CP‐93,129, a potent and selective 5‐HT_1B receptor agonist blocks neurogenic plasma extravasation within rat but not guinea‐pig dura mater

Pretreatment with CP‐93,129 blocked plasma extravasation in rat dura mater induced by electrical trigeminal ganglion stimulation when administered at ≥140 nmol kg⁻¹, i.v. but did not affect plasma leakage in guinea‐pig at 460 or 1400 nmol kg⁻¹. Sumatriptan, a 5‐HT_1D‐like receptor agonist, blocked plasma extravasation in the guinea‐pig model when administered at 7 nmol kg⁻¹. In as much as CP‐93,129 binds with micromolar affinities to 5‐HT_1A, 5‐HT_1C, 5‐HT_1D, and 5‐HT₂ recognition sites, and with nanomolar affinity to the 5‐HT_1B receptor subtype, blockade of plasma extravasation in the rat dura mater may be mediated by 5‐HT_1B receptors whereas the 5‐HT_1D receptor may be more relevant to the guinea‐pig.

DOI: 10.1111/j.1476-5381.1991.tb12374.x

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