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NK-1受体拮抗剂GR 82,334对反射性诱发膀胱收缩的影响。

Effect of the NK-1 receptor antagonist GR 82,334 on reflexly-induced bladder contractions.

作者信息

Lecci A, Giuliani S, Maggi C A

机构信息

Pharmacological Research Department, A. Menarini Pharmaceuticals, Florence, Italy.

出版信息

Life Sci. 1992;51(26):PL277-80. doi: 10.1016/0024-3205(92)90165-l.

Abstract

The effect of intrathecal administration of the novel tachykinin NK-1 receptor antagonist GR 82,334 has been tested in three reflexes which excite urinary bladder motility. GR 82,334 at 1 but not at 0.1 nmol/rat blocked the chemonociceptive micturition reflex induced by the topical application of capsaicin (4 micrograms/50 microliters) onto the urinary bladder. At the same dose proven effective in the chemonociceptive reflex, GR 82,334 did not affect either micturition reflex induced by bladder filling or the urinary bladder contraction induced by perineal pinching. These results suggest that, in urethane-anesthetized rats, specific stimuli applied in the periphery activate NK-1 receptors at spinal cord level facilitating urinary bladder reflex contractions.

摘要

新型速激肽NK-1受体拮抗剂GR 82,334鞘内给药对三种激发膀胱运动的反射作用进行了测试。GR 82,334以1 nmol/大鼠而非0.1 nmol/大鼠的剂量阻断了通过向膀胱局部应用辣椒素(4微克/50微升)诱导的化学伤害性排尿反射。在对化学伤害性反射有效的相同剂量下,GR 82,334既不影响膀胱充盈诱导的排尿反射,也不影响会阴夹捏诱导的膀胱收缩。这些结果表明,在乌拉坦麻醉的大鼠中,外周施加的特定刺激在脊髓水平激活NK-1受体,促进膀胱反射性收缩。

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