Papir-Kricheli D, Gilon C, Chorev M, Selinger Z, Devor M
Department of Zoology, Hebrew University of Jerusalem, Israel.
Neuropharmacology. 1990 Nov;29(11):1055-65. doi: 10.1016/0028-3908(90)90112-5.
Recently, two compounds have been developed, designated septide and senktide, which are highly selective agonists for the substance P receptor, types NK-1 and NK-3, respectively. Each of these, when injected intrathecally in awake rats, produced a distinct and non-overlapping constellation of sensory and behavioural effects which were subsets of the symptoms evoked by intrathecal administration of substance P. Prior systemic administration of 5-hydroxytryptamine (5-HT), alpha-adrenergic and opiate receptor antagonists, at doses sufficient to block the behavioural effects of the corresponding receptor agonists, did not alter responses to intrathecally injected septide or senktide. This was so, even for symptoms which suggested inhibitory mediation, hypoalgesia and (transient) motor flaccidity. Septide and senktide, administered by lumbar puncture and by indwelling catheter, produced identical results. Finally, in contrast to some other peptides, flaccid paralysis induced by senktide was not accompanied by spinal necrosis.
最近,已研发出两种化合物,分别命名为septide和senktide,它们分别是P物质受体NK - 1型和NK - 3型的高度选择性激动剂。将它们各自鞘内注射到清醒大鼠体内时,会产生一系列独特且不重叠的感觉和行为效应,这些效应是鞘内注射P物质所诱发症状的子集。事先全身给予5 - 羟色胺(5 - HT)、α - 肾上腺素能和阿片受体拮抗剂,剂量足以阻断相应受体激动剂的行为效应,但这并未改变对鞘内注射septide或senktide的反应。即便对于那些提示有抑制性介导、痛觉减退和(短暂的)运动弛缓的症状也是如此。通过腰椎穿刺和留置导管给予septide和senktide产生了相同的结果。最后,与其他一些肽不同,senktide诱导的弛缓性麻痹并未伴有脊髓坏死。