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Effects of kappa, sigma, and phencyclidine receptors agonists in rat tail arteries of spontaneously hypertensive rats

  
@article{APS6107,
	author = {Jun Bao and Wei-li Bao and Feng-yan Sun and An-zhong Zhang},
	title = {Effects of kappa, sigma, and phencyclidine receptors agonists in rat tail arteries of spontaneously hypertensive rats},
	journal = {Acta Pharmacologica Sinica},
	volume = {15},
	number = {2},
	year = {2016},
	keywords = {},
	abstract = {The effects of the kappa receptor agonist trans-4-dichloro-N-methyl-N-(2-(1-pyrrolidin)cyclohexyl)-benzen eacefamide methane sulfonate (U-50 488H), etorphine, the sigma (sigma) receptor agonists (+)-3-(3-hydroxychenyl)-N-(1-propyl) piperidine ((+)-3-PPP), 1, 3-di-o-tolyl-guanidine (DTG), and the phencyclidine (Phe) receptor agonists Phe, N-(1-(2-thienyl)cyclohexyl) piperidine (TCP), and dizocilipine maleate (MK-801) on electrically stimulated constriction (ESC) were investigated in the rat tail arteries (RTA) of spontaneously hypertensive rats (SHR) and normotensive Wistar-Kyoto (WKY) rats. Etorphine and U-50 488H inhibited the response to ESC in SHR more than that in WKY. The effects of U-50 488H were greater than those of etorphine. The IC50 and Kact of U-50 488H in SHR were 2.5 +/- 2.0 and 0.43 +/- 0.22 mumol.L-1, respectively, while the corresponding figures in WKY were 23 +/- 15 and 2.3 +/- 1.0 mumol.L-1, respectively (P < 0.05). The inhibitory effects of (+)-3-PPP on ESC in RTA of SHR were weaker than those in WKY. Its IC50 and Kact in SHR were 11.6 +/- 5.4 and 0.87 +/- 0.30 mumol.L-1, respectively, while the corresponding figures in WKY were 0.63 +/- 0.16 and 0.35 +/- 0.18 mumol.L-1, respectively (P < 0.05). But the inhibitory effect of DTG was very slight and the difference of Kact between WKY and SHR was not significant. The enhancing effects of Phe, TCP, and MK-801 in SHR were not at all different from those in WKY at each concentration tested.(ABSTRACT TRUNCATED AT 250 WORDS)},
	issn = {1745-7254},	url = {http://www.chinaphar.com/article/view/6107}
}