Stubbs C M, Connor H E, Feniuk W
Department of Neuropharmacology, Glaxo Group Research Limited, Ware, Hertfordshire, U.K.
Eur J Pharmacol. 1991 May 2;197(1):113-6. doi: 10.1016/0014-2999(91)90373-x.
The putative 5-HT1A receptor antagonist BMY 7378 (3-100 micrograms.kg-1 i.v.) caused reductions in blood pressure, heart rate and efferent renal nerve activity in anaesthetised cats. Similar effects were produced by the selective 5-HT1A receptor agonist, 8-hydroxy-2(di-n-propylamino)tetralin (8-OH-DPAT 1-10 micrograms.kg-1 i.v.). The sympatho-inhibitory effects of BMY 7378 and 8-OH-DPAT, but not those of clonidine were reversed by the non-selective 5-HT1A receptor antagonist, spipirone (1 mg.kg-1 i.v.). It is concluded that BMY 7378 is an agonist at 5-HT1A receptors mediating hypotension and renal sympatho-inhibition in anaesthetised cats.
假定的5-羟色胺1A受体拮抗剂BMY 7378(静脉注射剂量为3 - 100微克·千克-1)可使麻醉猫的血压、心率和肾传出神经活动降低。选择性5-羟色胺1A受体激动剂8-羟基-2(二正丙基氨基)四氢萘(8-OH-DPAT,静脉注射剂量为1 - 10微克·千克-1)也产生类似作用。非选择性5-羟色胺1A受体拮抗剂螺哌隆(静脉注射剂量为1毫克·千克-1)可逆转BMY 7378和8-OH-DPAT的交感抑制作用,但不能逆转可乐定的交感抑制作用。结论是,BMY 7378是麻醉猫中介导低血压和肾交感抑制的5-羟色胺1A受体激动剂。