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类阿片肽(Opioid peptides)的镇痛作用机制
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作者 吴银生 《中国医院药学杂志》 CAS 1984年第4期27-28,共2页
改变吗啡骨架合成麻醉性镇痛药的报道已很多,就其结构活性研究成果发现,具天然吗啡相同的R~((-))这一立体特异性,确认了它们有强力的镇痛活性.麻醉性镇痛药设想有特异结合能的阿片受体,1973年已被实验证实脑内存在。但其分布不均一,在... 改变吗啡骨架合成麻醉性镇痛药的报道已很多,就其结构活性研究成果发现,具天然吗啡相同的R~((-))这一立体特异性,确认了它们有强力的镇痛活性.麻醉性镇痛药设想有特异结合能的阿片受体,1973年已被实验证实脑内存在。但其分布不均一,在调节痛觉深部的脊髓后角,兰斑核,三叉神经下行核的罗氏胶质区、中脑导水管周围灰质等高密度地存在阿片受体。有关阿片受体的内在性活性物质,已从一组含多肽哺乳动物的脑、下垂体分离出两种脑啡肽(蛋-脑啡肽和亮-脑啡肽)及β-内啡肽的单体.从类阿片肽的发现推测可能存在调节内在性疼痛的机能. 展开更多
关键词 镇痛作用 吗啡 阿片 opioid peptides
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Beta-endorphin in serum and seminal plasma in infertile men 被引量:1
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作者 Shawky El-Haggar Salah El-Ashmawy +6 位作者 Ahmed Attia Taymour Mostafa M.M.Farid Roaiah Ashraf Fayez Sherif Ghazi Wael Zohdy Nagwa Roshdy 《Asian Journal of Andrology》 SCIE CAS CSCD 2006年第6期709-712,共4页
Aim: To access beta-endorphin levels in serum as well as seminal plasma in different infertile male groups. Methods: Beta-endorphin was estimated in the serum and seminal plasma by enzyme-linked immunosorbent assay ... Aim: To access beta-endorphin levels in serum as well as seminal plasma in different infertile male groups. Methods: Beta-endorphin was estimated in the serum and seminal plasma by enzyme-linked immunosorbent assay (ELISA) method in 80 infertile men equally divided into four groups: non-obstructive azoospermia (NOA), obstructive azoospermia (OA), congenital bilateral absent vas deferens (CBVAD) and asthenozoospermia. The results were compared to those of 20 normozoospermic proven fertile men. Results: There was a decrease in the mean levels of betaendorphin in the seminal plasma of all successive infertile groups (mean ± SD: NOA 51.30 ± 27.37, OA 51.88 ± 9.47, CBAVD 20.36 ± 13.39, asthenozoospermia 49.26 ± 12.49 pg/mL, respectively) compared to the normozoospermic fertile control (87.23 ± 29.55 pg/mL). This relation was not present in mean serum level of beta-endorphin between four infertile groups (51.09 ± 14.71, 49.76 ± 12.4, 33.96 ± 7.2, 69.1 ± 16.57 pg/mL, respectively) and the fertile control group (49.26 ± 31.32 pg/mL). The CBVAD group showed the lowest seminal plasma mean level of beta-endorphin. Testicular contribution of seminal beta-endorphin was estimated to be approximately 40%. Seminal beta-endorphin showed significant correlation with the sperm concentration (r = 0.699, P = 0.0188) and nonsignificant correlation with its serum level (r = 0.375, P = 0.185) or with the sperm motility percentage (r = 0.470, P = 0.899). Conclusion: The estimation of beta-endorphin alone is not conclusive to evaluate male reproduction as there are many other opiates acting at the hypothalamic pituitary gonadal axis. 展开更多
关键词 AZOOSPERMIA BETA-ENDORPHIN male infertility opioid peptides SEMEN seminal plasma
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Characteristic fragmentation behavior of the analogs of endomorphin-2 with phenylglycine in position 3 or 4 by ESI-FT tandem mass spectrometry
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作者 Chang Feng Hu Chuan Jun Zhu +3 位作者 Yan Feng Gao Xuan Shao Rui Wang Yu Xin Cui 《Chinese Chemical Letters》 SCIE CAS CSCD 2008年第12期1479-1482,共4页
A series of analogs of endomorphin-2 (EM-2) with phenylglycine (Phg) in position 3 or 4 were synthesized. In electrospray ionization Fourier transform ion cyclotron resonance (ESI-Fr-ICR) MS/MS spectra of these ... A series of analogs of endomorphin-2 (EM-2) with phenylglycine (Phg) in position 3 or 4 were synthesized. In electrospray ionization Fourier transform ion cyclotron resonance (ESI-Fr-ICR) MS/MS spectra of these compounds, some b, y, a, and internal ions were observed and slight mass differences between the calculated and observed results are obtained. Their sequences were derived successfully. However, the MS/MS patterns of these analogs with Dphg and Lphg were very similar. It is hard to distinguish them by MS/MS spectra. Moreover, if the third position was substituted by phenylglycine (L or D), a rearrangement could occur in MS/MS experiment to lose proline residue. 展开更多
关键词 Endomorphin-2 opioid peptide analogs PHENYLGLYCINE ESI-FT MS
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Enzymatic clickable functionalization of peptides via computationally engineered peptide amidase
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作者 Tong Zhu Lu Song +1 位作者 Ruifeng Li Bian Wu 《Chinese Chemical Letters》 SCIE CAS CSCD 2018年第7期1116-1118,共3页
Directed peptides C-terminal modification enabled by the engineered biomolecular catalyst-peptide amidase 12 B has been achieved via computational protein engineering. The engineered enzyme exhibits great promising po... Directed peptides C-terminal modification enabled by the engineered biomolecular catalyst-peptide amidase 12 B has been achieved via computational protein engineering. The engineered enzyme exhibits great promising potential in the C-terminal modification of opioid peptides using prop-2-yn-1-amine(PYA) or prop-2-en-l-amine(PEA) as the nucleophile. A variety of opioid peptides could be readily functionalized at the C-terminal chain in high yield in a mild and selective manner. Notably, modified opioid peptides bearing alkynyl moiety could be further functionalized through well-established click reaction. 展开更多
关键词 peptide amidase opioid peptides C-terminal modification Click reaction FUNCTIONALIZATION
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