【摘要】 用生物鉴定法研究苯环利定Phe受体的配体Phe,TCP,Diz及δ受体的配体dl-SK&F-10047 dl-pentazocine,DTG在兔耳中动脉的作用。结果表明:Phe受体配体均能剂量依赖地增强电场刺激引起的动脉收缩;而δ受体配体无此作用,右旋的δ受体配体能抑制Phe的作用;它的异构体却是增强Phe作用。提示:在外周血管上主要存在Phe受体更多还原

【Abstract】 Several ligands of phencyclidine ( Phe ) receptors; Phe, dizocilpine maleate (Diz, MK-801),- 1-[1-(2-thionyl)cyclohexyl] piperidine (TCP), and ligands of sigma (σ) 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 a receptors had no effect on ESV of the arteries, but 5 μmol·L-1 reduced or increased the effect of Phe (5 μmol·L-1) on ESV. d-SK&F-10047, d-pentazocine, and DTG inhibited the effect of Phe on ESV from 364 μ 22 mg to 142 μ 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 a receptors in the arteries.更多还原