title: A potential calcium antagonist and its antihypertensive effects.
abstract: Imperatorin (Imp) as a hypotensive active ingredient, its hypotensive effect was evaluated in the SHRs, its calcium antagonism and affinity to L-type calcium channel was also confirmed. The results showed that the blood pressure was decreased in the SHRs treated with Imp, the aortic ring was relaxed with Imp, L-type calcium channel currents and intracellular calcium free ion rise was nearly disappeared when adding Imp. In addition, Imp displayed a chromatographic peak similar to nitrendipine and verapamil by the cell membrane chromatography, same results from protein-drug docking approaches. Hence, Imp target the L-type calcium channel, and may be used as a novel antihypertensive drug.
authors.affiliation: School of Medicine, Xi'an Jiaotong University, Xi'an, PR China; The Mental Health Center of Xi'an, Xi'an, PR China.
authors.forename: Yan
authors.initials: Y
authors.lastname: Zhang
authors.forename: YanJun
authors.initials: Y
authors.lastname: Cao
authors.forename: QunLi
authors.initials: Q
authors.lastname: Wang
authors.forename: Lei
authors.initials: L
authors.lastname: Zheng
authors.forename: Jie
authors.initials: J
authors.lastname: Zhang
authors.forename: LangChong
authors.initials: L
authors.lastname: He
mesh_terms: D000818:Animals; D000959:Antihypertensive Agents / Q000737:chemistry / Q000494:pharmacology*; D001011:Aorta / Q000187:drug effects; D019661:Apiaceae / Q000737:chemistry*; D001794:Blood Pressure / Q000187:drug effects*; D002118:Calcium / Q000037:antagonists & inhibitors*; D002121:Calcium Channel Blockers / Q000737:chemistry / Q000494:pharmacology; D020746:Calcium Channels, L-Type / Q000378:metabolism*; D002462:Cell Membrane; D002845:Chromatography; D011564:Furocoumarins / Q000737:chemistry / Q000494:pharmacology*; D009568:Nitrendipine / Q000737:chemistry; D010936:Plant Extracts / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D017208:Rats, Wistar; D014664:Vasodilation / Q000187:drug effects; D014700:Verapamil / Q000737:chemistry
chemical_list: D000959:Antihypertensive Agents; D002121:Calcium Channel Blockers; D020746:Calcium Channels, L-Type; D011564:Furocoumarins; D010936:Plant Extracts; D009568:Nitrendipine; D014700:Verapamil; C031534:imperatorin; D002118:Calcium