[The beta-adrenergic receptor and adenylate cyclase of rat reticulocytes as a test system for screening pharmacologic preparations].
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.
Kurennaia
G S
GS
Chekneva
E E
EE
Grigorian
G Iu
GIu
Tkachuk
V A
VA
D000262:Adenylyl Cyclases / Q000378:metabolism*; D000818:Animals; D004353:Drug Evaluation, Preclinical / Q000379:methods*; D051381:Rats; D011943:Receptors, Adrenergic, beta / Q000187:drug effects*; D012156:Reticulocytes / Q000187:drug effects*; D013268:Stimulation, Chemical
D011943:Receptors, Adrenergic, beta; D000262:Adenylyl Cyclases
Beta-adrenergicheskiĭ retseptor i adenilattsiklaza retikulotsitov krysy kak test-sistema dlia skrininga farmakologicheskikh preparatov.