Kajekar R, Gupta P, Shepperson N B, Brain S D
Pharmacology Group, King's College, London.
Br J Pharmacol. 1995 May;115(1):1-2. doi: 10.1111/j.1476-5381.1995.tb16310.x.
Neurogenic oedema formation in the rat hind paw skin induced by electrical stimulation of the saphenous nerve and measured by extravasation of [125I]-albumin, was inhibited by the 5-HT1B receptor agonist, CP-93,129, and the novel tryptamine analogue, CP-122,288. Significant inhibition of up to 66% of control was observed with CP-122,288 (2 x 10(-14) - 2 x 10(-7) mol kg-1) and CP-93,129 (5 x 10(-7) - 5 x 10(-6) mol kg-1), with the minimum effective dose for CP-122,288 being about 10(7) fold less than that for CP-93,129. Oedema formation induced by the intradermal administration of exogenous mediators (substance P and histamine) in rat dorsal skin was not inhibited by CP-122,288 (2 x 10(-10) mol kg-1). These results suggest that CP-122,288 is a potent inhibitor of neurogenic inflammation in rat skin and that the effect may be due to a prejunctional inhibition of neuropeptide release.
通过电刺激大鼠隐神经并以[125I] - 白蛋白外渗来测量，大鼠后爪皮肤中由神经源性引起的水肿形成，受到5 - HT1B受体激动剂CP - 93,129和新型色胺类似物CP - 122,288的抑制。CP - 122,288（2×10（-14） - 2×10（-7）mol kg-1）和CP - 93,129（5×10（-7） - 5×10（-6）mol kg-1）可观察到高达对照66%的显著抑制，CP - 122,288的最小有效剂量比CP - 93,129小约10（7）倍。大鼠背部皮肤中由皮内注射外源性介质（P物质和组胺）诱导的水肿形成未被CP - 122,288（2×10（-10）mol kg-1）抑制。这些结果表明，CP - 122,288是大鼠皮肤神经源性炎症的有效抑制剂，且该作用可能是由于对神经肽释放的节前抑制所致。
