AIM: To examine the acute actions of the CB1cannabinoid receptor antagonist SR141716A [N-piperidino-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methylpyrazole-3-carbowamide] on typical behavioralpattern of psychoactiv...AIM: To examine the acute actions of the CB1cannabinoid receptor antagonist SR141716A [N-piperidino-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methylpyrazole-3-carbowamide] on typical behavioralpattern of psychoactive cannabinoids in rats.METHODS:At different time after injection the tail-flick response latency,the rectal temperature,thelocomotor activity,and the immobility on a ring as wellas the numbers of rears,self-grooming episodes(lasting 5 s),and fecal pellets were measured.RESULTS:Achte administration of SR141716A(3 mg/kg ip) induced a significant increase inhorizontal locomotor activity assayed by an activitymeter,in stereotypic activity(such as rearing and self-展开更多
AIM: To study the potential role of dependence statuson CB_1-mediated blockade of ethanol self-administra-tion. METHODS: We examined the effects of thecannabinoid antagonist SR141716A (0, 0.03, 0.3,and 3 mg/kg) on ppe...AIM: To study the potential role of dependence statuson CB_1-mediated blockade of ethanol self-administra-tion. METHODS: We examined the effects of thecannabinoid antagonist SR141716A (0, 0.03, 0.3,and 3 mg/kg) on pperant ethanol (10 ％ v/v) self-administration in male Wistar rats that were madeethanol-dependent by chronic (14 d ) exposure toethanol vapor-chambers or exposed to air in identicalvapor chambers.RESULTS: Dependent animalsresponded more for ethanol than did air controlnondependent tats. The acute administration of a 3mg/kg dose of SR141716A almost suppressed ethanolself-administration ouly in ethanol dependent animals.展开更多
A novel and efficient method was developed for the synthesis of diarylpyrazole derivatives as cannabinoid CB1 receptor antagonist via four step reactions. The key step was the synthesis of a diarylpyrazole skeleton, w...A novel and efficient method was developed for the synthesis of diarylpyrazole derivatives as cannabinoid CB1 receptor antagonist via four step reactions. The key step was the synthesis of a diarylpyrazole skeleton, which involved initial condensation of the sodium salt of compound 12 with diazonium compounds, and further cyclization by heating at reflux in acetic acid. Eight diarylpyrazole derivatives and nine new synthesized compounds were characterized by 1H NMR, IR, MS, and elemental analysis. The reaction conditions were mild and the overall yields of the target compounds ranged from 26% to 44%.展开更多
文摘AIM: To examine the acute actions of the CB1cannabinoid receptor antagonist SR141716A [N-piperidino-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methylpyrazole-3-carbowamide] on typical behavioralpattern of psychoactive cannabinoids in rats.METHODS:At different time after injection the tail-flick response latency,the rectal temperature,thelocomotor activity,and the immobility on a ring as wellas the numbers of rears,self-grooming episodes(lasting 5 s),and fecal pellets were measured.RESULTS:Achte administration of SR141716A(3 mg/kg ip) induced a significant increase inhorizontal locomotor activity assayed by an activitymeter,in stereotypic activity(such as rearing and self-
基金DGICYT PM 96/0047,Comunidad de Madrid and Plan Nacional Sobre Drogas (MN,FRF)National Institutes of Health grants AA 06420AA 08459 from the National Institute on Alcohol Abuse and Alcoholism (GFK and AJR)
文摘AIM: To study the potential role of dependence statuson CB_1-mediated blockade of ethanol self-administra-tion. METHODS: We examined the effects of thecannabinoid antagonist SR141716A (0, 0.03, 0.3,and 3 mg/kg) on pperant ethanol (10 ％ v/v) self-administration in male Wistar rats that were madeethanol-dependent by chronic (14 d ) exposure toethanol vapor-chambers or exposed to air in identicalvapor chambers.RESULTS: Dependent animalsresponded more for ethanol than did air controlnondependent tats. The acute administration of a 3mg/kg dose of SR141716A almost suppressed ethanolself-administration ouly in ethanol dependent animals.
基金Supported by the Program for New Century Excellent Talents in University of China(NosNCET-08-0668, 1154-NCET-002)the Outstanding Youth Foundation of Heilongjiang Province, China(NoJC200706)
文摘A novel and efficient method was developed for the synthesis of diarylpyrazole derivatives as cannabinoid CB1 receptor antagonist via four step reactions. The key step was the synthesis of a diarylpyrazole skeleton, which involved initial condensation of the sodium salt of compound 12 with diazonium compounds, and further cyclization by heating at reflux in acetic acid. Eight diarylpyrazole derivatives and nine new synthesized compounds were characterized by 1H NMR, IR, MS, and elemental analysis. The reaction conditions were mild and the overall yields of the target compounds ranged from 26% to 44%.
