C 49802-B-Ba和CGP 6085 A对去甲肾上腺素和5-羟色胺摄取的选择性抑制作用

Selective inhibition of noradrenaline and serotonin uptake by C 49802-B-Ba and CGP 6085 A.

作者信息

Waldmeier P C, Baumann P A, Wilhelm M, Bernasconi R, Maître L

出版信息

Eur J Pharmacol. 1977 Dec 15;46(4):387-91. doi: 10.1016/0014-2999(77)90234-5.

Abstract

The effects of two new compounds, 1-(1-methylamino-2-hydroxy-3-propyl)-dibenzo[b,e]bicyclo[2,2,2]octadiene-HCl (C 49802-B-Ba) and 4-(5,6-dimethyl-2-benzofuranyl) piperidine HCl (CGP 6085 A), on noradrenaline (NA) and serotonin (5-HT) uptake were investigated in different test systems, CGP 6085 A is a very potent and selective inhibitor of 5-HT uptake in rat brain (ED50 1-4 mg/kg p.o., depending on test system). Doses up to 1000 mg/kg p.o. did not inhibit NA uptake. C 49802-B-Ba is a potent and selective inhibitor of NA uptake in rat brain (ED50 5-10 mg/kg p.o. depending on test system) and heart (ED50 1.5 mg/kg p.o.). At 300 mg/kg p.o., this compound caused no inhibition of 5-HT uptake.

摘要

研究了两种新化合物1-(1-甲氨基-2-羟基-3-丙基)-二苯并[b,e]双环[2,2,2]辛二烯盐酸盐（C 49802-B-Ba）和4-(5,6-二甲基-2-苯并呋喃基)哌啶盐酸盐（CGP 6085 A）在不同测试系统中对去甲肾上腺素（NA）和5-羟色胺（5-HT）摄取的影响。CGP 6085 A是大鼠脑中5-HT摄取的一种非常强效且具选择性的抑制剂（口服半数有效剂量为1 - 4毫克/千克，具体取决于测试系统）。口服剂量高达1000毫克/千克时不会抑制NA摄取。C 49802-B-Ba是大鼠脑（口服半数有效剂量为5 - 10毫克/千克，具体取决于测试系统）和心脏（口服半数有效剂量为1.5毫克/千克）中NA摄取的强效且具选择性的抑制剂。口服剂量为300毫克/千克时，该化合物不会抑制5-HT摄取。