Rawlow A, King R G
Department of Pharmacology, Monash University, Clayton, Victoria, Australia.
J Neural Transm Gen Sect. 1991;84(1-2):85-94. doi: 10.1007/BF01249112.
In the spinalized and decerebrate rat, electrically evoked flexor reflex activity (FRA) of the right anterior tibialis muscle was facilitated by DMI (0.1-3 mg/kg i.v.). DMI (3 mg/kg i.v.) had not effect on twitches of the left ant. tib. muscle evoked by electrical stimulation of the distal stump of the severed sciatic nerve (directly evoked twitches). The alpha-1 adrenoceptor antagonist prazosin (300 micrograms/kg i.v.) and the alpha-2 adrenoceptor agonists clonidine (5 and 10 micrograms/kg i.v.) and BHT-920 (100 micrograms/kg i.v.) all suppressed FRA facilitated by DMI (3 mg/kg i.v.). The alpha-2 adrenoceptor antagonists yohimbine (100 micrograms/kg i.v.) and mianserin (30 micrograms/kg i.v.) antagonized the suppressant effect of clonidine (5 micrograms/kg i.v.) on DMI-facilitated FRA. Clonidine (10 micrograms/kg i.v.) had no effect on directly evoked twitches, and at 3-300 micrograms/kg i.v. had no effect on FRA facilitated by L-DOPA (100 mg/kg i.p.). It is suggested that DMI-facilitated FRA can be used as a test for alpha-2 adrenoceptor agonists which may act at presynaptic alpha-2 adrenoceptors in the spinal cord.
在脊髓横断和去大脑的大鼠中,静脉注射地马唑啉(DMI,0.1 - 3毫克/千克)可增强右侧胫前肌的电诱发屈肌反射活动(FRA)。静脉注射DMI(3毫克/千克)对切断坐骨神经远侧端电刺激诱发的左侧胫前肌抽搐(直接诱发抽搐)无影响。α1肾上腺素能受体拮抗剂哌唑嗪(静脉注射300微克/千克)、α2肾上腺素能受体激动剂可乐定(静脉注射5和10微克/千克)以及BHT - 920(静脉注射100微克/千克)均能抑制由DMI(3毫克/千克静脉注射)增强的FRA。α2肾上腺素能受体拮抗剂育亨宾(静脉注射100微克/千克)和米安色林(静脉注射30微克/千克)可拮抗可乐定(静脉注射5微克/千克)对DMI增强的FRA的抑制作用。可乐定(静脉注射10微克/千克)对直接诱发的抽搐无影响,且在静脉注射3 - 300微克/千克时对左旋多巴(腹腔注射100毫克/千克)增强的FRA也无影响。提示DMI增强的FRA可作为一种检测方法,用于检测可能作用于脊髓突触前α2肾上腺素能受体的α2肾上腺素能受体激动剂。