Effects of alkyl-1, 2, 5, 6-tetrahydro-3-substitutedPyridine derivatives on the functions of vascular endothelial cells and its structure-activity relationship

Abstract

Abstract: AIM: To observe the influence of alkyl-1,2,5,6-tetrahydro-3-substitutedPyridine analogy compounds on the function of endothelial cells.METHODS: The effects ofl-NAME,indomethacin,pilocarpine and atropine on the novel compounds were observed using the isolated rat aorta and guineaPig ileum model.RESULTS: Among 100 compounds,4leading compounds were found,which included HH91,HH95,HH98,and HH103.The endothelium-dependent relaxation mediated by HH103 could be blocked byl-NAME,but not by indomethacin,pilocarpine and atropine.CONCLUSION: The novel compounds can mediate endothelium-dependent relaxation and had unique structure-activity relationship.The function of endothelium-dependent relaxation mediated by HH103 isPerformed byPromoting the secrete of NO,but different from that of ACh.

Key words: pharmacology, endothelial cells, muscarinic receptor, acetylcholine, arecoline, structure-activity relationship

CLC Number:

R965
R971.92

SHI Cui-Ge1, HU Guo-Qiang, HU Gang, HUANG Wen-Long, WANG Hai. Effects of alkyl-1, 2, 5, 6-tetrahydro-3-substitutedPyridine derivatives on the functions of vascular endothelial cells and its structure-activity relationship[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2003, 8(6): 613-617.

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