Effects of sigma and phencyclidine receptor ligands on electric field-stimulated rabbit ear artery constriction in vitro.
Several ligands of phencyclidine (Phe) receptors: Phe, dizocilpine maleate (Diz, MK-801), 1-[1-(2-thionyl)cyclohexyl] piperidine (TCP), and ligands of sigma (sigma) receptors: dl-N-allylnormetazocine (dl-SK&F-10047), 1, 3-di-ortho-tylyl-guanidine (DTG), dl-pentazocine, were tested on rabbit ear arteries in vitro. It was found that the ligands of Phe receptors enhanced the electric field stimulated vasoconstriction (ESV). Their concentration-effect curves of these compounds were parallel in the order of potencies: Phe > Diz > TCP. The ligands of sigma receptors had no effect on ESV of the arteries, but 5 mumol.L-1 reduced or increased the effect of Phe (5 mumol.L-1) on ESV. d-SK&F-10047, d-pentazocine, and DTG inhibited the effect of Phe on ESV from 364 +/- 22 mg to 142 +/- 49 mg (n = 5, P < 0.01), 262 +/- 95 mg (n = 5, P < 0.05), and 291 +/- 80 mg (n = 5, P > 0.05), respectively. The levoisomers: l-SK&F-10047 and l-pentazocine enhanced the effect of Phe on ESV from 364 +/- 22 mg to 484 +/- 78 mg (n = 5, P < 0.05), and 466 +/- 95 mg (n = 5, P < 0.05), respectively. These results revealed that there were mainly Phe receptors but hardly any sigma receptors in the arteries.
Bao
W L
WL
Department of Neurobiology, Shanghai Medical University, China.
Zhen
F C
FC
Sun
F Y
FY
Zhang
A Z
AZ
D000818:Animals; D001158:Arteries; D016291:Dizocilpine Maleate / Q000494:pharmacology; D004423:Ear / Q000098:blood supply*; D004558:Electric Stimulation; D005260:Female; D066298:In Vitro Techniques; D008024:Ligands; D008297:Male; D010423:Pentazocine / Q000494:pharmacology; D010620:Phenazocine / Q000031:analogs & derivatives / Q000494:pharmacology; D010622:Phencyclidine / Q000494:pharmacology; D011817:Rabbits; D017478:Receptors, Phencyclidine / Q000378:metabolism; D017480:Receptors, sigma / Q000378:metabolism; D014661:Vasoconstriction / Q000187:drug effects*
D008024:Ligands; D017478:Receptors, Phencyclidine; D017480:Receptors, sigma; D016291:Dizocilpine Maleate; C012134:SK&F 10047; D010620:Phenazocine; D010622:Phencyclidine; D010423:Pentazocine