Baranauskas G, Nistri A
Biophysics Sector, International School for Advanced Studies (S.I.S.S.A.), Trieste, Italy.
Peptides. 1995;16(2):357-9. doi: 10.1016/0196-9781(94)00194-4.
The effect of RP 67580, a recently developed antagonist selective for the NK1 tachykinin receptors of peripheral tissues, was studied with intracellular recording from motoneurones of the rat isolated spinal cord. In the presence of RP 67580 (1-2 microM), membrane depolarization induced by the putative transmitter substance P (SP) was either unchanged or enhanced (an effect prevented by tetrodotoxin; TTX). Neither short nor long excitatory synaptic potentials (EPSPs) were antagonized by RP 67580. Sustained synaptically evoked depolarizations (mimicking noxious stimuli and thus presumed to be at least partly mediated by SP) were also insensitive to RP 67580. These data suggest the existence of a pharmacologically distinct NK1 receptor population insensitive to RP 67580) in the neonatal rat spinal cord.
采用细胞内记录法,对从大鼠离体脊髓运动神经元上获取的标本进行研究,以探究RP 67580(一种最新研发的、对周围组织的NK1速激肽受体具有选择性的拮抗剂)的作用。在存在RP 67580(1 - 2微摩尔)的情况下,由假定的递质P物质(SP)诱导的膜去极化要么未改变,要么增强(该效应可被河豚毒素;TTX阻断)。RP 67580既不拮抗短时间的兴奋性突触后电位(EPSP),也不拮抗长时间的EPSP。持续的突触诱发去极化(模拟有害刺激,因此推测至少部分由SP介导)对RP 67580也不敏感。这些数据表明,新生大鼠脊髓中存在一个对RP 67580不敏感的药理学上不同的NK1受体群体。