Receptor specificity and trigemino-vascular inhibitory actions of a novel 5-HT(1B/1D) receptor partial agonist, 311C90 (zolmitriptan)

British Journal of Pharmacology

Volumn 121, Issue 2, 1997, Pages 157-164

  Martin, G R ^a,b   Robertson, A D ^a,c   MacLennan, S J ^a,b   Prentice, D J ^a,d   Barrett, V J ^a,e   Buckingham, J ^a   Honey, A C ^a,e   Giles, H ^a,e   Moncada, S ^a,f  

^a WELLCOME RESEARCH LABORATORIES   (United Kingdom)

^b ROCHE BIOSCIENCE   (United States)

^c Zenyth Therapeutics Limited Australia   (Australia)

^d UNIVERSITY OF SURREY   (United Kingdom)

^e GLAXOSMITHKLINE   (United Kingdom)

^f Cruciform Project   (United Kingdom)

Author keywords

311C90; 5 HT receptors; Migraine; Neurogenic extravasation; Zolmitriptan; Zomig

Indexed keywords

ADENYLATE CYCLASE; ANTIMIGRAINE AGENT; FORSKOLIN; PARTIAL AGONIST; PLASMA PROTEIN; RECEPTOR; SEROTONIN; SEROTONIN 1B RECEPTOR; SEROTONIN 1D RECEPTOR; SEROTONIN 2A RECEPTOR; SUMATRIPTAN; ZOLMITRIPTAN;

ADULT; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BASILAR ARTERY; CASE REPORT; CELL MEMBRANE; COMPARATIVE STUDY; CONCENTRATION RESPONSE; CONDUCTANCE; CONTROLLED STUDY; CORONARY ARTERY; DRUG POTENCY; DURA MATER; ELECTROSTIMULATION; ENZYME INHIBITION; EXTRAVASATION; FEMALE; GENETIC TRANSFECTION; GUINEA PIG; HUMAN; HUMAN TISSUE; LASER DOPPLER FLOWMETRY; MALE; MIGRAINE; NONHUMAN; PRIMATE; PRIORITY JOURNAL; RABBIT; RECEPTOR AFFINITY; SAPHENOUS VEIN; TRIGEMINUS GANGLION; VASOCONSTRICTION;

EID: 0030899908     PISSN: 00071188     EISSN: None     Source Type: Journal    
DOI: 10.1038/sj.bjp.0701041     Document Type: Article

References (51)

1. 1F receptor to multiple signal; transduction pathways. Naunyn-Schmiedeberg's Arch. Pharmacol., 348, 566-575.
2. 1 receptor subtype coupled to the inhibition of adenylate cyclase. Proc. Natl. Acad. Sci. U.S.A., 90, 408-412.
3. BAXTER, G.S., CRAIG, D.A. & CLARKE, D.E. (1991). 5-Hydroxytryptamine receptors mediate relaxation of the rat oesophageal tunica muscularis mucosae. Naunyn-Schmiedeberg's Arch Pharmacol., 343, 439-446.
4. BLACK, J.W. & LEFF, P. (1983). Operational models of pharmacological agonism. Proc. R. Soc. Lond (B), 220, 141-162.
5. BROWN, E.G., ENDERSBY, C.A., SMITH, R.N. & TALBOT, J.C. (1991). The safety and tolerability of sumatriptan: an overview. Eur. Neurol., 31, 339-344.
6. BUZZI, M.G., MOSKOWITZ, M.A., PEROUTKA, S.J. & BYUN, B. (1991). Further characterisation of the putative 5-HT receptor which mediates blockade of neurogenic plasma extravasation in rat dura mater. Rr. J. Pharmacol., 103, 1421-1428.
7. 1-like receptors in guinea-pig basilar arteries. Acta Physiol. Scand. 136, 59-67.
8. 50) of an enzymatic reaction. Biochem. Pharmacol., 22, 3099-3108.
9. CHESTER, A., MARTIN, G.R., BODELSSON, M., ARNEKLO-NOBIN, B., TADJKARIMI, S., TÖRNEBRANDT, K. & YACOUB, M. (1990). 5-Hydroxytryptamine receptor profile in healthy and diseased human epicardial coronary arteries. Cardiovasc. Res., 24, 932-937.
10. 2-receptor agonist. U-46619. Br. J. Pharmacol., 110, 360-368.
11. 1-adenosine receptor in the guinea-pig atrium. Br. J. Pharmacol., 78, 207-212.
12. 1D receptor subtypes mediating cerebral vasoconstriction. Cephalalgia, 15 (Suppl 14), 99.
13. 1-like receptor agonist. Br. J. Pharmacol., 96, 379-387.
14. 1D receptors of 5-hydroxytryptamine-induced contractions of rabbit middle and posterior cerebral arteries. Br. J. Pharmacol., 112, 939-945.
15. 1-like receptors in the reduction of porcine cranial arterio-venous anastomotic shunting by sumatriptan. Br. J. Pharmacol., 102, 323-330.
16. EARL, N.L. (1995). 311C90, a new acute treatment for migraine: an overview of safety. Cephalalgia, 15 (Suppl. 14), 217.
17. EARL, N.L. (1997). Zolmitriptan (311C90), a new acute treatment for migraine: An overview of safety. In Headache Treatment: Trial Methodology and New Drugs, Frontiers in Headache Research, Vol. 6. ed. Olesen, J. & Tfelt-Hansen, P. pp 267-272. Lippincott: Raven.
18. FENIUK, W., HUMPHREY, P.P.A. & WATTS, A.D. (1979). Pre-synaptic inhibitory action of 5-hydroxytryptamine in dog isolated saphenous vein. Br. J. Pharmacol., 67, 247-254.
19. FENIUK, W., HUMPHREY, P.P.A., PERREN, M.J. & WATTS, A.D. (1985). A comparison of 5-hydroxytryptamine receptors mediating contraction in rabbit isolated aorta and dog saphenous vein. Evidence for different receptor types obtained by the use of selective agonists and antagonists. Br. J. Pharmacol., 86, 697-704.
20. FRIBERG, L., OLESEN, J., IVERSEN, H.K. & SPERLING, B. (1991). Migraine pain associated with middle cerebral artery dilatation: reversal by sumatriptan. Lancet, 338, 13-17.
21. GOADSBY, P.J. & EDVINSSON, L. (1994). Peripheral and central trigeminovascular activation in cat is blocked by the serotonin (5-HT)-1D receptor agonist 311C90. Headache, 34, 394-399.
22. 1Dβ receptor subtype in human and bovine cerebral arteries. Mol. Pharmacol., 44, 242-246.
23. 1D receptor subtypes. Trends Pharmacol. Sci., 17, 103-105.
24. HUMPHREY, P.P.A., APPERLEY, E., FENIUK, W. & PERREN, M.J. (1990). A rational approach it identifying a fundamentally new drug for the treatment of migraine. In Cardiovascular Pharmacology of 5-hydroxytryptamine. ed. Saxena, P.R., Wallis, D.I., Wouters, W. & Bevan, P. pp. 417-431. Dordrecht: Kluwer.
25. HUMPHREY, P.P.A. & FENIUK, W. (1991). Mode of action of the antimigraine drug sumatriptan. Trends Pharmacol. Sci., 12, 444-446.
26. HUMPHREY, P.P.A., FENIUK, W., MOTEVALIAN, M., PARSONS, A.A. & WHALLEY, E.T. (1991). The vasoconstrictor action of sumatriptan on human isolated dura mater. In Serotonin: Molecular Biology, Receptors and Functional Effects, ed. Fozard, J.R. & Saxena, P.R. pp. 421-429. Basel: Birkhäuser Verlag.
27. 1-like receptor in dog isolated saphenous vein. Br. J. Pharmacol., 94, 1123-1132.
28. HUMPHREY, P.P.A. & GOADSBY, P.J. (1994). The mode of action of sumatriptan is vascular? A debate. Cephalalgia, 14, 401-410.
29. KAUBE, H., HOSKIN, K.L. & GOADSBY, P.J. (1992). Activation of the trigemino-vascular system by mechanical distention of the superior sagittal sinus in the cat. Cephalalgia, 12, 133-136.
30. KAUBE, H., HOSKIN, K.L. & GOADSBY, P.J. (1993). Inhibition by sumatriptan of central trigeminal neurones only after blood-brain barrier disruption. Br. J. Pharmacol., 109, 788-792.
31. KAUMANN, A.J., PARSONS, A.A. & BROWN, A.M. (1993). Human arterial constrictor serotonin receptors. Cardiovasc. Res., 27, 2094-2103.
32. 1Dβ receptors. Circulation, 90, 1141-1153.
33. KLEIN, K.B. (1995). 311C90, a new acute treatment for migraine: an efficacy overview. Cephalalgia, 15 (Suppl. 14), 175.
34. KLEIN, K.B. (1997). A review of the efficacy of zolmitriptan (311C90): A new acute treatment for migraine. In Headache Treatment: Trial Methodology and New Drugs, Frontiers in Headache Research, Vol. 6. ed. Olesen, J. & Tfelt-Hansen, P. pp. 263-266. Lippincott: Raven.
35. 2-receptors: a problem of acute desensitisation? Br. J. Pharmacol., 95, 569-577.
36. LEFF, P., PRENTICE, D.J., GILES, H., MARTIN, G.R. & WOOD, J. (1990). Estimation of agonist affinity and efficacy by direct operational model-fitting. J. Pharmacol. Methods, 23, 225-237.
37. MARKOWITZ, S., SAITO, K. & MOSKOWITZ, M.A. (1987). Neurogenically mediated leakage of plasma protein occurs from blood vessels in dura mater but not brain. J. Neurosci., 7, 4129-4136.
38. MARTIN, G.R. (1994). Vascular receptors for 5-hydroxytryptamine. Distribution, function and classification. J. Pharmacol. Ther., 62, 283-324.
39. MARTIN, G.R . LEFF, P., CAMBRIDGE, D. & BARRETT, V.J. (1987). Comparative analysis of two types of 5-hydroxytryptamine receptor mediating vasorelaxation: differential classification using tryptamines. Naunyn-Schmiedeberg's Arch Pharmacol., 336, 365-373.
40. MARTIN, G.R. & MACLENNAN, S.J. (1990). Analysis of the 5-HT receptor in rabbit saphenous vein exemplifies the problems of using exclusion criteria for receptor classification. Naunyn-Schmiedeberg's Arch. Pharmacol., 342, 111-119.
41. 1D recognition site? Fund. Clin. Exp. Pharmacol., 5, 417.
42. 3H]sumatriptan binding in cat brainstem and spinal cord. Eur. J. Pharmacol., 280, 175-178.
43. MOSKOWITZ, M.A. (1992). Neurogenic vs vascular mechanisms of sumatriptan and ergot alkaloids in migraine. Trends Pharmacol. Sci., 13, 307-311.
44. NOZAKI, K., MOSKOWITZ, M.A. & BOCCALINI, P. (1992). CP-93,129, a sumatriptan, dihydroergotamine block c-fos expression within rat trigeminal nucleus caudalis caused by chemical stimulation of the meninges. Br. J. Pharmacol., 106, 409-415.
45. 1-like receptors mediate 5-hydroxytryptamine-induced contraction of human isolated basilar artery. Br. J. Pharmacol., 96, 434-449.
46. PERREN, M.J., FENIUK, W. & HUMPHREY, P.P.A (1989). The selective closure of feline carotid arterio-venous anatomoses by GR43175. Cephalalgia, 9 (Suppl. 9), 41-46.
47. 1Dα serotonin receptor gene expression in trigeminal ganglia: Implications for antimigraine drug development. Proc. Natl. Acad. Sci. U.S.A., 91, 3666-3669.
48. SAXENA, P.R. (1978). Arterio-venous shunting and migraine. Res. Clin. Stud. Headache, 6, 89-102.
49. SEABER, E., ON, N., DIXON, R. & POSNER, J. (1995). The metabolic disposition of the novel antimigraine compound 311C90. Cephalalgia, 15 (Suppl. 14), 215.
50. VISSER, W.H., KLEIN, K.B., COX, R., MARKS, S.J. & FERRARI, M.D. (1994). An in-patient, placebo-controlled, dose-ranging study of oral 311C90 in the acute treatment of migraine. In New Advances in Headache Research, Vol. 4. ed. Clifford Rose, F. pp. 15-16. Nishimura: Smith-Gordon.
51. 1B receptors: 5-CT and CP-122,288, but not sumatriptan or CP-93,129, block dural plasma protein extravasation. Cephalalgia, 15, (Suppl. 14), 59.