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Changes of mu and kappa opioid receptors in cathartic colon of rat
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作者 刘宝华 莫平 +2 位作者 贾后军 李春穴 张胜本 《Journal of Medical Colleges of PLA(China)》 CAS 2004年第5期282-284,共3页
Objective: To observe the changes of mu and kappa opioid receptors in the cathartic colon of rat, and to clarify that whether opioid receptors accounts for the occurrence of slow transit constipation (STC). Methods: T... Objective: To observe the changes of mu and kappa opioid receptors in the cathartic colon of rat, and to clarify that whether opioid receptors accounts for the occurrence of slow transit constipation (STC). Methods: The cathartic colon model of rat was made by feeding with laxatives. The activity of mu and kappa opioid receptors in the cathartic colon of rat was measured by radio-ligand binding assay. Results: Compared with the control group, the maximal binding capacity (Bmax) and affinity(Kd) of mu opioid receptor in cathartic colon group were significantly increased (207.00±22.90 fmol/mg·p vs 82.00±14.23 fmol/mg·p, P < 0.01;3.30±0.45 mmol/L vs 2.40±0.57 mmol/L,P < 0.05). The maximal binding capacity of kappa opioid receptor also showed a great increase (957.00±102.41 fmol/mg·p vs 459.00±52.41 fmol/mg·p, P<0.01), but no significant difference of affinity was found between the two groups. Conclusion: The mu and kappa opioid receptors may be involved in the functional disorders of cathartic colon. 展开更多
关键词 cathartic colon mu opioid receptor kappa opioid receptor
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YFa and analogs:Investigation of opioid receptors in smooth muscle contraction
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作者 Krishan Kumar Ritika Goyal +2 位作者 Annu Mudgal Anita Mohan Santosh Pasha 《World Journal of Gastroenterology》 SCIE CAS CSCD 2011年第40期4523-4531,共9页
AIM:To study the pharmacological profile and inhibition of smooth muscle contraction by YFa and its analogs in conjunction with their receptor selectivity. METHODS:The effects of YFa and its analogs (D-Ala2) YFa, Y (D... AIM:To study the pharmacological profile and inhibition of smooth muscle contraction by YFa and its analogs in conjunction with their receptor selectivity. METHODS:The effects of YFa and its analogs (D-Ala2) YFa, Y (D-Ala2) GFMKKKFMRF amide and Des-Phe-YGGFMKKKFMR amide in guinea pig ileum (GPI) and mouse vas deferens (MVD) motility were studied using an isolated tissue organ bath system, and morphine and DynA (1-13) served as controls. Acetylcholine was used for muscle stimulation. The observations were validated by specific antagonist pretreatment experiments using naloxonazine, naltrindole and norbinaltor-phimine norBNI. RESULTS:YFa did not demonstrate significant inhibition of GPI muscle contraction as compared with mor-phine (15% vs 62%, P = 0.0002), but moderate inhibition of MVD muscle contraction, indicating the role of κ opioid receptors in the contraction. A moderate inhibition of GPI muscles by (Des-Phe) YFa revealed the role of anti-opiate receptors in the smooth muscle contraction. (D-Ala-2) YFa showed significant inhibition of smooth muscle contraction, indicating the involvement of mainly δ receptors in MVD contraction. These results were supported by specific antagonist pretreatment assays. CONCLUSION:YFa revealed its side-effect-free analgesic properties with regard to arrest of gastroin-testinal transit. The study provides evidences for the involvement of κ and anti-opioid receptors in smooth muscle contraction. 展开更多
关键词 opioid receptor Guinea pig ileum Mousevas deferens Smooth muscle contraction Gastrointestinal motility
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A Functional Balance between Spinal Mu and Kappa Opioid Receptors in Itch Regulation
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作者 Ming Chen Cheng Liu +2 位作者 Xue-hai Guan Lin-tao Qu Hong-bing Xiang 《麻醉与监护论坛》 2012年第5期335-337,共3页
关键词 阿片受体 皮肤瘙痒症 脊柱 平衡 规例 神经系统 神经传递 动物模型
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Expression of mu-opioid receptors in human chronic inflamed knee joint synovium tissue 被引量:3
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作者 袁红斌 何星颖 +3 位作者 徐海涛 朱秋峰 王亚华 石学银 《Journal of Medical Colleges of PLA(China)》 CAS 2006年第6期397-400,共4页
Objective: To examine the changes of mu-opioid receptors (MORs) expression in human chronic inflamed knee joint synovium tissue. Methods:Knee joint synovium tissues were taken from 21 patients with chronic arthritis (... Objective: To examine the changes of mu-opioid receptors (MORs) expression in human chronic inflamed knee joint synovium tissue. Methods:Knee joint synovium tissues were taken from 21 patients with chronic arthritis (inflamed group) and 6 fresh bodies with normal knee joints (control group). And the expression of MORs was detected by using immunohistochemistry. flow cytometry(FCM) and reverse-transcription polymerase chain reaction (RT-PCR). Results: The expression of MORs in the inflamed group was significantly higher than that in the normal group by using the 3 techniques(P<0. 05). Conclusion: Chronic inflammation enhances the up-regulation of MORs in human knee joint synovium tissue. 展开更多
关键词 HUMAN INFLAMMATION knee joint opioid receptors mu
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Dopamine D<sub>1</sub>- and D<sub>2</sub>-Receptors in Immunostimulation under Activation of Mu-Opioid Receptors in Mice with Different Psychoemotional States
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作者 Margarita Cheido Galina Idova Elizaveta Alperina 《Pharmacology & Pharmacy》 2014年第1期43-48,共6页
The purpose of the present study was to analyze the effect of activation of mu-opioid receptors (mu-OR) on the immune response under blockade of postsynaptic D1-and D2-receptors in mice of the C57BL/6J strain displayi... The purpose of the present study was to analyze the effect of activation of mu-opioid receptors (mu-OR) on the immune response under blockade of postsynaptic D1-and D2-receptors in mice of the C57BL/6J strain displaying either aggressive or depressive-like behaviors in the social conflict model. It is shown that activation of activation of mu-OR with a highly selective agonist DAGO (100 μg/kg) increased significantly IgM-immune response not only in C57BL/6J mice with an unchanged psychoemotional state but also in mice displaying aggressive or depressive-like behaviors in the social stress model (10 days of agonistic confrontations). Selective blockade of DA receptors of the D1-type with SCH-23390 (1.0 mg/kg with DAGO administration) caused a more pronounced elevation of IgM-immune response than DAGO alone while DAGO effect was completely blocked by prior administration of D2-receptor antagonist haloperidol (1.0 mg/kg). At the same time, both SCH-23390 and haloperidol prevented the immune response increase induced by DAGO injection in mice engaged in aggressive or depressive-like behaviors. Thus, in animals not subjected to social stress DAGO-induced immunostimulation is provided only by D2-receptors, whereas in animals with altered psychoemotional state mu-opioid immunostimulation is mediated by both types of DA receptors—D1 and D2. These data provide evidence for different impacts of the main subtypes of DA receptors in the mediation of immunomodulating effects of mu-opioid system under normal and stressful conditions. 展开更多
关键词 mu-opioid and Dopamine receptors Social Stress AGGRESSION Depressive-Like Behavior Immunomodulation
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Analgesic and anti-inflammatory potential of aerial parts of the Daphne mucronata Royle extract in mice: Opioid-independent action
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作者 Zohreh Khodadadian Majid Hassanpour-Ezatti +1 位作者 Seyed Zahra Mousavi Jinous Asgarpanah 《Asian Pacific Journal of Tropical Biomedicine》 SCIE CAS 2016年第3期198-201,共4页
Objective: To investigate the analgesic and anti-inflammatory property and possible involvement of opioid receptors of ethyl acetate extract from aerial parts of Daphne mucronata(D. mucronata) in mice by formalin test... Objective: To investigate the analgesic and anti-inflammatory property and possible involvement of opioid receptors of ethyl acetate extract from aerial parts of Daphne mucronata(D. mucronata) in mice by formalin test.Methods: Single doses of 2.5, 5.0 and 10.0 mg/kg of body weight of ethyl acetate extract of D. mucronata were intraperitoneally administered to the mice 30 min before analgesic test. The anti-nociceptive effect of preparations was evaluated based on the formalin in mice.Results: The results indicated that the extract(2.5, 5.0 and 10.0 mg/kg) increased the pain threshold of mice and induced analgesia in both phases of formalin test. Like morphine sulfate(5.0 mg/kg, i.p.), the extract also showed more effective analgesic effect on the late phase of formalin test. Pre-treatment of animals with naloxone(5.0 mg/kg i.p.)did not inhibit the effects of the extract.Conclusions: Our findings suggest that D. mucronata contains potential analgesic and anti-inflammatory compounds which support its traditional use. Moreover, it seems that the analgesic and anti-inflammatory effects of the extract is mediated by non-opioid mechanisms. Further pharmacological studies are required to determine whether the analgesic mechanisms are actually responsible for such properties. 展开更多
关键词 DAPHNE mucronata ANALGESIA opioid receptors MICE
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Corelation Between Single Nucleotide Polymorphisms in Mu Opioid Receptor Exon 2 and Stereotypic Behaviour in Sows
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作者 LI Jianhong BAO Jun CUI Weiguo 《Journal of Northeast Agricultural University(English Edition)》 CAS 2008年第4期20-27,共8页
Three breeds of sows were observed to investigate the relationship between Single Nucleotide Polymorphisms(SNPs) in Mu Opioid Receptor(MOR)and stereotypic behaviour,such as,sham-chewing,bar biting and standing sti... Three breeds of sows were observed to investigate the relationship between Single Nucleotide Polymorphisms(SNPs) in Mu Opioid Receptor(MOR)and stereotypic behaviour,such as,sham-chewing,bar biting and standing still in order to better understand the mechanism of stereotypic development of the animals in restrained conditions.MOR exon 2 partial sequences were amplified to analyze single nucleotide polymorphisms by PCR-SSCP.One SNP,a silence mutant was found.A significant difference (P〈0.01)was found in the frequency of genotypes in these 3 breeds where only the BB genotype,which was identical to that published in GenBank,was found in the Duroc breed,while no AA genotype was found in Landrace,3 genotypes AA,BB and AB were found in Yorkshire.The result also indicated that the individuals with AA and AB genotypes tended to be more active in sham-chewing than those with the BB genotype(P〈0.05).The overall results of this study suggested that sham-chewing of sows may be subjected to both genetic control and environmental conditions,but activity level was more likely to be affected by their environment.We can putatively draw the conclusion that MOR gene has effect on the sham-chewing behavioral traits of sow. 展开更多
关键词 mu opioid Receptor(MOR) Single Nucleotide Polymorphism(SNP) stereotypic behaviour SOWS
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Effects of Peripherally Acting Opioid Ligands on Central Opioid Receptors and <i>β</i>-Endorphin Release in Stressed Rats
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作者 Sergey K. Sudakov Valentina G. Bashkatova +1 位作者 Tatiyana V. Proskuriakova Alexey E. Umriukhin 《Journal of Behavioral and Brain Science》 2012年第2期162-166,共5页
Using the radioreceptor binding assay, μ-opioid receptor (MOR) affinity in the midbrain of stressed rats was higher than in naive controls. MOR density in the rat frontal cortex was reduced after stress. Intragastric... Using the radioreceptor binding assay, μ-opioid receptor (MOR) affinity in the midbrain of stressed rats was higher than in naive controls. MOR density in the rat frontal cortex was reduced after stress. Intragastric administration of the MOR antagonist naloxone methiodide was followed by an increase in the number of MORs in the frontal cortex. However, the MOR agonist loperamide significantly decreased the density of MORs in the frontal cortex and midbrain of naive animals. Loperamide and naloxone methiodide were shown to prevent an increase in MOR affinity and a decrease in MOR density in the midbrain of rats after restraint stress. The restraint stress was accompanied by an increase in the release of β-endorphin (BE) in the ventral tegmental area (VTA) of control rats. After administration, loperamide slightly decreased the release of BE, naloxone methiodide significantly increased the release of BE in the cingulate cortex (CC) of untreated animals, while drugs had no effect on the release of BE in the VTA. The drugs significantly increased the extracellular level of BE in the CC of stressed animals. Loperamide abolished the increase in the stress-induced release of BE in the VTA. By contrast, naloxone methiodide significantly increased the release of BE in the VTA of stressed rats. Our data indicated that activation of peripheral MORs induces depression of the central part of the μ-opioid system, but suppression of peripheral MOR activity induces activation of the central μ-opioid system, the interaction of which can be modulated by stress. 展开更多
关键词 Peripheral opioid receptors Emotional Stress Β-ENDORPHIN Microdialysis RADIOLIGAND Binding Density of μ-opioid receptors
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MODULATION OF A δ-AND C-FIBER EVOKED RESPONSES OF NOCICEPTIVE NEURONS IN THE SUPERFICIAL AND THE DEEPER DORSAL HORN OF THE MEDULLA:ROLE OF OPIOID RECEPTORS(μ, δ_1, δ_2)
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作者 王小民 《Journal of Pharmaceutical Analysis》 CAS 1995年第2期202-203,共2页
The present study was designed to investigate the effects of intravenously administered agonists and antagonists at μ(DAMGO, naloxone,)δ1 (DPDPE,BNTX)andδ2(DELT, NTB)opioid receptors on the Aδ-and C-fiber evoked r... The present study was designed to investigate the effects of intravenously administered agonists and antagonists at μ(DAMGO, naloxone,)δ1 (DPDPE,BNTX)andδ2(DELT, NTB)opioid receptors on the Aδ-and C-fiber evoked responses of nociceptive neurons in the superficial and the deeper dorsal horn of the rat medulla.Extracellular single unit recording were made from 70 nociceptive neurons(28 NS,42 WDR) in the superficial dorsal horn and 37 nociceptive neurons(4 NS,33 WDR)in the deeper dorsal horn.All these neurons had an ipsilateral orofacial mechanoreceptive field and majority of these neurons had no spontaneous activity. The latencies for the C fiber evoked responses ranged from 34~105 msec whereas for Aδfiber-evoked responses it ranged from 3~22msec. A clear separation was observed between early and late responses of evoked by Cand Aδ-fiber.Application of DPDPE,DELT and DAMGO produced inhibitory effects on the Aδ-and C-fiber evoked responses of nociceptive neurons in the superficial and thedeeper dorsal horn.By comparison,the inhibition was more pronounced on the C-fiber evoked response than on the Aδ-fiber evoked response,and DAMGO produced a stronger inhibitory action than both DELT and DPDPE. Additionally,DPDPE produced facilitation, or inhibition followed by facilitation on the Aδ-and C-response and the effect had longer latency and longer time course.DPDPE also induced completely oppsite effects on the Aδ-and C-fiber evoked responses.Although the facilitation was observed,the effect was not dose-dependent. Application of BNTX (0.4~1mg/kg),a δ1 receptor antagonist,produced antagonism of DPDPE in 88%(7/8) neurons. Application of the doses (0.7~1mg/kg) of BTB,δ2-receptor antagonist,resulted in antagonism of both DELT and DPDPE. The inhibition of DELT on Aδ-response was antagonized by doses (0.3~1mg/kg)of NTB in 100% (14/14)neurons while the antagonism on C-response was in 79%(11/14) neurons.The effect produced by DPDPE was antagonized by the doses (0.7~1mg/kg) of NTB in 100%(4/4) neurons. However,a smaller dose of NTB(0.3mg/kg)which and antagonize the effect of DELT,did not antagonize the effect of DPEPE in 100%(4/4) neurons. The inhibitory action of DAMGO on Aδ-and C-fiber evoked responses was completely antagonized by naloxone(0. 2mg/kg) in 100% (6/6) neurons. These results suggest that:①μ-and δ-opioid receptors play an important role in modulating Aδ-and Cfiber evoked responses of nociceptive neurons in the superficial and the deeper dorsal horn of the rat medulla; ② The inhibitory action produced by DPDPE, DELT and DAMGO was more pronounced on the C-fiber evoked excitation and indicates that the agonists produce more predominant inhibition on the responses of dorsal horn neurons to noxious stimuli; ③ activation of either δ1-orδ2-opioid receptors produces inhibitory actions on Aδ- and C-response of nociceptive neurons in the superficial and the deeper dorsal horn of the medullal;DPDPE and DELT act at different δ-opioid receptor subtypes in the rat rnedulla; ⑤i.v.-administered NTB can distinguish δ-opioid receptor subtypes in a limited dose range.When administered i. v., 0. 3mg/kg of NTB is selective for δ2-opioid receptor. 展开更多
关键词 pain trigeminal dorsal horn opioid receptor DPDPE DELT DAMGO NTB BNTX NALOXONE
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Low-dose morphine elicits ventilatory excitant and depressant responses in conscious rats: Role of peripheral <i>µ</i>-opioid receptors 被引量:1
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作者 Fraser Henderson Jr. Walter J. May +4 位作者 Ryan B. Gruber Alex P. Young Lisa A. Palmer Benjamin Gaston Stephen J. Lewis 《Open Journal of Molecular and Integrative Physiology》 2013年第3期111-124,共14页
The systemic administration of morphine affects ventilation via a mixture of central and peripheral actions. The aims of this study were to characterize the ventilatory responses elicited by a low dose of morphine in ... The systemic administration of morphine affects ventilation via a mixture of central and peripheral actions. The aims of this study were to characterize the ventilatory responses elicited by a low dose of morphine in conscious rats;to determine whether tolerance develops to these responses;and to determine the potential roles of peripheral μ-opioid receptors (μ-ORs) in these responses. Ventilatory parameters were monitored via unrestrained whole-body plethysmography. Conscious male Sprague-Dawley rats received an intravenous injection of vehicle or the peripherally-restricted μ-OR antagonist, naloxone methiodide (NLXmi), and then three successive injections of morphine (1 mg/kg) given 30 min apart. The first injection of morphine in vehicle-treated rats elicited an array of ventilatory excitant (i.e., increases in frequency of breathing, minute volume, respiratory drive, peak inspiratory and expiratory flows, accompanied by decreases in inspiratory time and end inspiratory pause) and inhibitory (i.e., a decrease in tidal volume and an increase in expiratory time) responses. Subsequent injections of morphine elicited progressively and substantially smaller responses. The pattern of ventilatory responses elicited by the first injection of morphine was substantially affected by pretreatment with NLXmi whereas NLXmi minimally affected the development of tolerance to these responses. Low-dose morphine elicits an array of ventilatory excitant and depressant effects in conscious rats that are subject to the development of tolerance. Many of these initial actions of morphine appear to involve activation of peripheral μ-ORs whereas the development of tolerance to these responses does not. 展开更多
关键词 MORPHINE Minute Ventilation Tolerance PERIPHERAL and Central opioid receptors CONSCIOUS Rats
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Immunohistochemical identification of dynorphin A and Kappa opioid receptor-1 in the digestive system of scallop Chlamys farreri
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作者 SUN Hushan WANG Yiyan +1 位作者 LIU Xiaoli LIU Dongwu 《Journal of Oceanology and Limnology》 SCIE CAS CSCD 2018年第6期2288-2296,共9页
Little is known about the roles of dynorphin and Kappa opioid receptor(KOR) in mollusks. In this study, we aim to determine the distribution of dynorphin A and KOR-1 in the digestive system of the scallop Chlamys farr... Little is known about the roles of dynorphin and Kappa opioid receptor(KOR) in mollusks. In this study, we aim to determine the distribution of dynorphin A and KOR-1 in the digestive system of the scallop Chlamys farreri. Using immunohistochemical staining, we confirmed the expression of dynorphin A and KOR-1 in the digestive system of C. farreri. Dynorphin A immunopositive cells were identified in intestine and hepatopancreas. In intestine, small and spherical dynorphin A immunopositive cells(4–9 μm in diameter) were scattered among the long columnar epithelial cells(ECs). In hepatopancreas, cells containing masses(5–14 μm in diameter) of dynorphin A immunopositive products were observed in epithelium of acinis. These immunopositive cells may be synthetic and/or secretory cells of dynorphin A. Dynorphin A immunoreactive products were commonly observed in epithelium and connective tissue(CT) of labial palps, mouth labia and stomach, which presented in forms of grains, fibers or flakes. KOR-1 immunoreactive material was observed in ECs and CTs of labial palps, mouth labia and stomach, intestine and hepatopancreas. The distribution of both dynorphin A and KOR-1 in the digestive organs suggests an involvement of dynorphin via KOR-1 in the functional regulation of the digestive system of C. farreri. 展开更多
关键词 CHLAMYS FARRERI DYNORPHIN DIGESTIVE system kappa opioid receptors immunohistochemistry
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Role of opioid receptor heterodimerization in pain modulation and tolerance development
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作者 Annu Mudgal Santosh Pasha 《World Journal of Pharmacology》 2015年第1期144-159,共16页
Protein to protein interactions leading to homo/heteromerization of receptor is well documented in literature. These interactions leading to dimeric/oligomers formation of receptors are known to modulate their functio... Protein to protein interactions leading to homo/heteromerization of receptor is well documented in literature. These interactions leading to dimeric/oligomers formation of receptors are known to modulate their function, particularly in case of G-protein coupled receptors. The opioid receptor heteromers having changed pharmacological properties than the constituent protomers provides preferences for novel drug targets that could lead to potential analgesicactivity devoid of tolerance and physical dependence. Heterodimerization of opioid receptors appears to generate novel binding properties with improved specificity and lack of side effects. Further the molecules which can interact simultaneously to both the protomers of the heteromer, or to both the binding sites(orthosteric and allosteric) of a receptor protein could be potential therapeutic molecules. This review highlights the recent advancements in exploring the plausible role of heteromerization of opioid receptors in induction of tolerance free antinociception. 展开更多
关键词 opioid receptors Receptor heterodimers G-protein coupled receptors oligomerization G protein coupled receptors opioid tolerance G-protein coupled receptors Allosteric regulation ANTINOCICEPTION
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Determination of structure-activity relationships between fentanyl analogs and human μ-opioid receptors based on active binding site models 被引量:3
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作者 Ming Liu Xiaoli Liu +2 位作者 Ping Wan Qiangsan Wu Wenxiang Hu 《Neural Regeneration Research》 SCIE CAS CSCD 2011年第4期267-276,共10页
Fentanyl is a potent and widely used clinical narcotic analgesic, as well as a highly selective IJ-opioid agonist. The present study established a homologous model of the human μ-opioid receptor; an intercomparison o... Fentanyl is a potent and widely used clinical narcotic analgesic, as well as a highly selective IJ-opioid agonist. The present study established a homologous model of the human μ-opioid receptor; an intercomparison of three types of μ-opioid receptor protein sequence homologous rates was made. The secondary receptor structure was predicted, the model reliability was assessed and verified using the Ramachandran plot and ProTab analysis. The predictive ability of the CoMFA model was further validated using an external test set. Using the Surflex-Dock program, a series of fentanyl analog molecules were docked to the receptor, the calculation results from Biopolymer/SitelD showed that the receptor had a deep binding area situated in the extracellular side of the transmembrane domains (TM) among TM3, TM5, TM6, and TMT. Results suggested that there might be 5 active areas in the receptor. The important residues were Asp147, Tyr148, and Tyr149 in TM3, Trp293, and His297 in TM6, and Trp318, His319, Ile322, and Tyr326 in TM7, which were located at the 5 active areas. The best fentanyl docking orientation position was the piperidine ring, which was nearly perpendicular to the membrane surface in the 7 TM domains. Molecular dynamic simulations were applied to evaluate potential relationships between ligand conformation and fentanyl substitution. 展开更多
关键词 μ-opioid receptor fentanyl analogs AGONIST active site structure-activity relationship
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Subtype of Opioid Receptor in Airway SmoothMuscle and the Role of the Receptor in Asthmatic Attacks
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作者 沈健藩 吴倩萍 +1 位作者 林雅芳 刘存明 《The Journal of Biomedical Research》 CAS 1998年第2期84-88,共5页
In order to elucidate the behavior of opioid receptor in the airway smooth muscle (ASM) and potential role of the receptor in asthmatic attacks electrical field stimulation (EFS) was used to evaluate the effects of di... In order to elucidate the behavior of opioid receptor in the airway smooth muscle (ASM) and potential role of the receptor in asthmatic attacks electrical field stimulation (EFS) was used to evaluate the effects of different narcotics and naloxine (Nal) on isolated rabbit ASM and biochemical methods were used to assay the influences of morphine (Mor) and pethidine(Pet) on the activities of adenylcyclase (AAC) and phosphodiesterase(APDE) in homogenate derived from rabbit ASM.Nal was used to treat the bronchospasm during anesthesia. It shows that Mor increased the rabbit ASM contraction and Nal reversed this effect, while Nal itself did not affect ASM. Fentanyl(Fen) decreased the contraction and Pet not only decreased the contraction but relaxed the ASM. Mor decreased the AAC in the rabbit ASM but didn't affect the APDE in the rabbit ASM. Pet had no influence on both the AAC and the APDE. Nal effectively relieved the bronchospasm which failed to the traditional treatment during anesthsia. These indicate that the opioid receptor in the ASM is a new subtype one.Mor exhibits satuable binding the subtype receptor and exerts strong agonistic activity to induce bronchospasm, while Nal antagonizes this effect. Yet Fen and Pet don's bind this subtype receptor. Endogenous opioid-like peptides may also bind this subtype receptor. In patients with airway hyperreactivity (PAHR) Mor is contraindicated, Fen and Pet may be used. and the latter may be the best choice.Asthma or bronchospasm may be treated with Nal. 展开更多
关键词 opioid receptor MORPHINE FENTANYL PETHIDINE naloxine BRONCHOSPASM
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RNA interference targeting mu-opioid receptors reverses the inhibition of fentanyl on glucose-evoked insulin release of rat islets 被引量:1
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作者 QIAN Tao-lai ZHANG Lei +3 位作者 WANG Xin-hua LIU Sheng MA Liang LU Ying 《Chinese Medical Journal》 SCIE CAS CSCD 2010年第24期3652-3657,共6页
Background Mu opioid receptor plays an important role in many physiological functions. Fentanyl is a widely used opioid receptor agonist for analgesia. This study was conducted to test the role of mu-opioid receptor o... Background Mu opioid receptor plays an important role in many physiological functions. Fentanyl is a widely used opioid receptor agonist for analgesia. This study was conducted to test the role of mu-opioid receptor on insulin release by determining whether fentanyl affected insulin release from freshly isolated rat pancreatic islets and if small interfering RNAs (siRNA) targeting mu-opioid receptor in the islets could knock down mu-opioid receptor expression.Methods Islets were isolated from ripe SD rats' pancreas by common bile duct intraductal collagenase V digestion and purified by discontinuous Ficoll density gradient centrifugation. The siRNA knock-down of mu-opioid receptor mRNA and protein in islet cells was analyzed by semi-quantitative real time-PCR and Western blotting. After siRNA-transfection for 48 hours, the islets were co-cultured with fentanyl as follows: 0 ng/ml, 3 ng/ml and 30 ng/ml for 48 hours. Then glucose-evoked insulin release was performed. As a control, the insulin release was also analyzed in islets without siRNA-trasfection after being co-cultured with fentanyl for 48 hours.Results After 48 hours of transfections, specific siRNA targeting of mu-opioid receptors produced significant reduction of mu-opioid receptor mRNA and protein (P <0.01). Fentanyl significantly inhibited glucose-evoked insulin release in islets in a concentration dependent manner (P <0.01). But after siRNA-transfection for 48 hours, the inhibition on glucose-evoked insulin reiease was reversed (P <0.01).Conclusions RNA interference specifically reduces mu-opioid receptor mRNA and protein expression, leading to reversal of the fentanyl-induced inhibition on glucose-evoked insulin release of rat islets. The activation of opioid receptor induced by fentanyl functions to inhibit insulin release. The use of RNAi presents a promising tool for future research in diabetic mechanisms and a novel therapy for diabetes. 展开更多
关键词 RNA interference mu-opioid receptor FENTANYL INHIBITION insulin release
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Endorphinergic Attenuation of Distress by Concomitantly Enhancing Endogenous Opioid Release and Switching Opioid Receptor Signaling from an Excessively Excitatory to a Normal Inhibitory Mode
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作者 Steven Crain Stanley M. Crain 《Journal of Behavioral and Brain Science》 2013年第7期497-508,共12页
The endogenous opioid system plays a significant role in the modulation of distress in many psychiatric, neurologic, and neurodevelopmental disorders. Many clinical distress symptoms show similarities to the excitator... The endogenous opioid system plays a significant role in the modulation of distress in many psychiatric, neurologic, and neurodevelopmental disorders. Many clinical distress symptoms show similarities to the excitatory autonomic withdrawal effects in chronic opioid-dependent animals and humans, as well as to the “quasi-morphine withdrawal syndrome” evoked in naive rodents shortly after acute systemic injection of cyclic AMP-phosphodiesterase (cAMP-PDE) inhibitors. These symptoms result from excessive excitatory opioid receptor signaling and increased endorphin release. Pharmacologic analyses of the remarkably plastic bimodal (excitatory/inhibitory) signaling functions of opioid receptors have utilized microelectrode recordings from opioid-sensitive neurons in tissue cultures of mouse sensory ganglia and hot-water tail-flick assays in mice. These studies led to development of specific chemical formulations that switch opioid receptor signaling from an excessively excitatory to a normal inhibitory mode. Critical combinations of cAMP-PDE inhibitors that release endorphins plus specific agents that switch opioid receptors from excitatory Gs-coupled to inhibitory Gi/Go-coupled signaling were shown to attenuate hyperalgesia and distress evoked by diverse chemical stressors in mouse tail-flick assays. Both the “quasi-morphine withdrawal syndrome” in naive rodents as well as the excitatory withdrawal effects in chronic, opioid-dependent animals and humans may be manifestations of a common Endorphinergic Distress Syndrome (EDS). We suggest that many distress symptoms are caused by EDS, a dysfunctional imbalance in the endogenous opioid system, consisting of abnormal endorphin levels, together with opioid receptors predominately in their excitatory mode. Therefore, concomitantly enhancing endogenous opioid release and switching excessive excitatory opioid receptor signaling to inhibitory signaling can attenuate these distress symptoms. Trials of a critically formulated oral preparation, containing both endorphin enhancers and opioid receptor switchers, have resulted in long-term anxiolytic efficacy and enhanced calm and mental clarity in large numbers of individuals with distress symptoms. These endorphinergic formulations may provide treatment for the emotional and physical distress associated with many psychiatric, neurologic, and neurodevelopmental disorders. 展开更多
关键词 ENDORPHINS Bimodal opioid receptors DISTRESS opioid ANALGESIA HYPERALGESIA Tolerance Dependence Endorphinergic DISTRESS Disorder
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“New-Look” Opioids: Biased Ligands
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作者 Joseph V. Pergolizzi Michael H. Ossipov +1 位作者 Robert Taylor Robert B. Raffa 《Pharmacology & Pharmacy》 2018年第7期242-249,共8页
Between the illicit use of opioids and attendant overdoses, and accidental overdoses with prescribed drugs, overuse of opioids has become a serious problem. At the same time, finding that fine balance between minimizi... Between the illicit use of opioids and attendant overdoses, and accidental overdoses with prescribed drugs, overuse of opioids has become a serious problem. At the same time, finding that fine balance between minimizing the risk of opioid misuse and abuse while at the same time providing access to treatment for patients who need pain control presents an ongoing challenge. Efforts to discover and develop better agents have led to what we term “new-look” opioids. We summarize here one such approach—known as biased ligands. By targeting a subset of GPCR signal transduction, this approach attempts to increase the separation between therapeutic and adverse effects. 展开更多
关键词 PAIN ANALGESIC Drugs opioidS G Protein-Coupled receptors Biased LIGANDS
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Effect of Synthetic Leucopyrokinin Analog [D-AlaS]-[2-8]-Leucopyrokinin ([D-AlaS]-[2-8]-LPK) on Opioid-lnduced Analgesia in Rats
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作者 Andrzej Plech Monika Rykaczewska-Czerwifiska +1 位作者 Adam Sipifiski Danuta Konopifiska 《Journal of Agricultural Science and Technology(A)》 2012年第5期682-689,共8页
The study was undertaken in order to evaluate effect of synthetic insect neuropeptide leucopyrokinin analog, [D-Ala5]-[2-8]-LPK, on analgesia induced by selective agonists of/a-, 6- and l〈-opioid receptors. The study... The study was undertaken in order to evaluate effect of synthetic insect neuropeptide leucopyrokinin analog, [D-Ala5]-[2-8]-LPK, on analgesia induced by selective agonists of/a-, 6- and l〈-opioid receptors. The study was performed on male Wistar rats, which a week before the experiments were implanted with polyethylene cannulas into the lateral brain ventricle (icv). Effect of prior administration of [D-Ala5]-[2-8]-LPK on analgesia induced in rats by next icv administration of equimolar dose of μ-, δ- and -opioid agonists: DAMGO, DPDPE and GR fumarate respectively, was evaluated. Antinociceptive effect was determined in rats by the test of the tail immersion. It was found that two doses of 5 and 10 nmols icv of [D-AlaS]-[2-8]-LPK inhibited analgesia in rats by equimolar doses of DAMGO. This analog also transiently (only in two time intervals) and in one dose of 10 nmols inhibited analgesia induced in rats by icv administration of equimolar DPDPE dose of 10 nmols icv. Obtained results indicate that [D-AlaS]-[2-8]-LPK inhibits antinociceptive effect of DAMGO and in part of DPDPE, i.e. mainly antagonized ~t-opioid receptors. These results correspond with results of our previous study that selective antagonists of μ- and δ-opioid receptors blocked antinociceptive effect of synthetic insect neuropeptide leucopyrokinin and of it active analog [2-8]-leucopyrokinin. We regard that [D-AIaS]-[2-8]-LPK, the first discovered antagonist of leucopyrokinin may be a useful as a probable tool substance in the study of biological effects of insect-derived peptides either in invertebrates or in mammals. 展开更多
关键词 [D-Ala5]-[2-8]-leucopyrokinin opioid receptors agonists antinociceptive effect rats.
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Binding properties of C-truncated delta opioid receptors 被引量:1
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作者 王春河 周德和 +3 位作者 陈洁 李桂芬 裴钢 池志强 《中国药理学报》 CSCD 1997年第4期337-340,共4页
目的:研究δ阿片受体C末端在受体结合配体的亲和力及选择性中的作用.方法:在中国苍鼠卵巢细胞(CHO细胞)中分别稳定表达C末端截短31个氨基酸残基及野生型δ阿片受体,用受体结合分析法研究表达产物与配体的结合特征.结果... 目的:研究δ阿片受体C末端在受体结合配体的亲和力及选择性中的作用.方法:在中国苍鼠卵巢细胞(CHO细胞)中分别稳定表达C末端截短31个氨基酸残基及野生型δ阿片受体,用受体结合分析法研究表达产物与配体的结合特征.结果:表达得到典型突变受体克隆CHOT及野生型受体克隆CHOW.CHOT结合[3H]diprenorphine(Dip)及[3H][DAla2,DLeu5]enkephalin(DADLE)的Kd值与CHOW一致,δ选择性激动剂对二者与[3H]Dip的结合均有很强的抑制作用,且Ki相似;而μ及κ选择性激动剂则对二者均无抑制作用.结论:δ阿片受体的C末端与受体结合配体的亲和力及选择性无关. 展开更多
关键词 Δ阿片受体 阿片 脑啡肽 结合位点 C-末端
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Molecular characterization and functional expression of opioid receptor-libe_1 receptor 被引量:2
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作者 WU YA LAN LU PU +4 位作者 KUN LING JIAN ZHAO ZHI JIE CHENG LAN MA GANG PEI(Shanghai Institute of Cell Biology, Chinese Academy of Sciences, Shanghai 200031, China)(Shanghai Medical University, Shanghai 200032, China) 《Cell Research》 SCIE CAS CSCD 1997年第1期69-77,共9页
The opioid receptor-libel receptor (ORL), an orphan receptor whose human and murine complementary DNAs,has been characterized recently. ORL transcripts are particularly abundant in the central nervous system. We demon... The opioid receptor-libel receptor (ORL), an orphan receptor whose human and murine complementary DNAs,has been characterized recently. ORL transcripts are particularly abundant in the central nervous system. We demonstrated that ORL expressed in human neuroblastoma SK-N-SH and SH-SY5Y cell lines by radioligand binding assay, reverse transcription polymerase chain reaction (RT-PCR) and Northern analysis in the present study. Stimulation with ORL1 specific agonist, nociceptin/orphanin Fo, increased [34S]GTPrγS binding to SK-N-SH cell membranes (EC50 = 14 ±0.45 nM), and attenuated forskolin-stimulated accumulation of cellular cAMP (EC50= 0.80 ±0.45 nM, indicative that activation of ORL1 activates G proteins and inhibits adenylyl cyclase. Activation of ORL1 receptor was also accessed using CHO:hORL1 cell line by microphysiometer. Treatment of nociceptin/orphanin FQ increased extracellular acidification rate significantly. 展开更多
关键词 opioid receptor-libe1 receptor (ORL1) nociceptin/orphanin FQ (N/OFQ) SK-N-SH cells extracellular acidification functional expression
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