Kurennaia G S, Chekneva E E, Grigorian G Iu, Tkachuk V A
Biull Eksp Biol Med. 1987 Nov;104(11):590-4.
The effect of cardio- and neurotropic drugs was studied on beta 2-adrenergic receptors and coupled adenylate cyclase (AC) from rat reticulocytes. Trifluperazine, chlorpromazine, levomepromazine, metaphenazine, haloperidol, (+) and (-) isomers of butaclamol, as well as imipramine, vinblastine and verapamil, at a concentration of 10(-4) M failed to influence AC stimulation by isoproterenol. Thioproperazine and trifluperidol inhibited isoproterenol-stimulated AC with Ki = 4.0.10(-5) M and Ki = 4.5.10(-5) M, respectively. This inhibitory effect was due to the direct action of thioproperazine and trifluperidol on the beta-adrenergic receptors, since this drugs displace the receptor-bound (3H) dihydroalprenolol with Ki = 5.10(-6) M and 9.10(-6) M, respectively. The results obtained suggest that adrenolytic effect of trifluperidol and thioproperazine might play a significant role in their side effects.
研究了心血管和神经otropic药物对大鼠网织红细胞β2 - 肾上腺素能受体和偶联腺苷酸环化酶（AC）的影响。三氟拉嗪、氯丙嗪、左美丙嗪、美吩嗪、氟哌啶醇、布他拉莫的（+）和（-）异构体，以及丙咪嗪、长春碱和维拉帕米，在浓度为10（-4）M时未能影响异丙肾上腺素对AC的刺激。硫丙嗪和三氟哌多抑制异丙肾上腺素刺激的AC，其Ki分别为4.0×10（-5）M和4.5×10（-5）M。这种抑制作用是由于硫丙嗪和三氟哌多对β - 肾上腺素能受体的直接作用，因为这些药物分别以Ki = 5×10（-6）M和9×10（-6）M取代与受体结合的（3H）二氢心得舒。所得结果表明，三氟哌多和硫丙嗪的抗肾上腺素作用可能在其副作用中起重要作用。
