Skip to main content
British Journal of Pharmacology logoLink to British Journal of Pharmacology
. 1993 Jan;108(1):11–12. doi: 10.1111/j.1476-5381.1993.tb13432.x

The non-peptide neurokinin1 receptor antagonist, RP 67580, blocks neurogenic plasma extravasation in the dura mater of rats.

S L Shepheard 1, D J Williamson 1, R G Hill 1, R J Hargreaves 1
PMCID: PMC1907730  PMID: 7679023

Abstract

A non-peptide neurokinin1 (NK1) receptor antagonist, RP 67580, that is selective for the rodent subtype of the NK1 receptor, dose-dependently reduced plasma extravasation in the dura mater produced by electrical stimulation of the trigeminal ganglion in rats, with an ID50 of 0.6 micrograms kg-1. Its enantiomer RP 68651 was some 400 fold less active. The results indicate that neurogenic plasma extravasation within the dura mater is NK1 receptor-mediated and suggest that NK1 receptor antagonists may have a role as antimigraine agents.

Full text

PDF
11

Selected References

These references are in PubMed. This may not be the complete list of references from this article.

  1. Beresford I. J., Birch P. J., Hagan R. M., Ireland S. J. Investigation into species variants in tachykinin NK1 receptors by use of the non-peptide antagonist, CP-96,345. Br J Pharmacol. 1991 Oct;104(2):292–293. doi: 10.1111/j.1476-5381.1991.tb12423.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  2. Buzzi M. G., Dimitriadou V., Theoharides T. C., Moskowitz M. A. 5-Hydroxytryptamine receptor agonists for the abortive treatment of vascular headaches block mast cell, endothelial and platelet activation within the rat dura mater after trigeminal stimulation. Brain Res. 1992 Jun 26;583(1-2):137–149. doi: 10.1016/s0006-8993(10)80017-4. [DOI] [PubMed] [Google Scholar]
  3. Buzzi M. G., Moskowitz M. A. The antimigraine drug, sumatriptan (GR43175), selectively blocks neurogenic plasma extravasation from blood vessels in dura mater. Br J Pharmacol. 1990 Jan;99(1):202–206. doi: 10.1111/j.1476-5381.1990.tb14679.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  4. Moskowitz M. A. Neurogenic versus vascular mechanisms of sumatriptan and ergot alkaloids in migraine. Trends Pharmacol Sci. 1992 Aug;13(8):307–311. doi: 10.1016/0165-6147(92)90097-p. [DOI] [PubMed] [Google Scholar]
  5. Saito K., Markowitz S., Moskowitz M. A. Ergot alkaloids block neurogenic extravasation in dura mater: proposed action in vascular headaches. Ann Neurol. 1988 Dec;24(6):732–737. doi: 10.1002/ana.410240607. [DOI] [PubMed] [Google Scholar]

Articles from British Journal of Pharmacology are provided here courtesy of The British Pharmacological Society

RESOURCES