The relevance of preclinical research models for the development of antimigraine drugs: focus on 5-HT(1B/1D) and CGRP receptors

Pharmacology & Therapeutics
S Gupta, C M Villalón

Abstract

Migraine is a complex neurovascular syndrome, causing a unilateral pulsating headache with accompanying symptoms. The past four decades have contributed immensely to our present understanding of migraine pathophysiology and have led to the introduction of specific antimigraine therapies, much to the relief of migraineurs. Pathophysiological factors culminating into migraine headaches have not yet been completely deciphered and, thus, pose an additional challenge for preclinical research in the absence of any direct experimental marker. Migraine provocation experiments in humans use a head-score to evaluate migraine, as articulated by the volunteer, which cannot be applied to laboratory animals. Therefore, basic research focuses on different symptoms and putative mechanisms, one at a time or in combination, to validate the hypotheses. Studies in several species, utilizing different preclinical approaches, have significantly contributed to the two antimigraine principles in therapeutics, namely: 5-HT(1B/1D) receptor agonists (known as triptans) and CGRP receptor antagonists (known as gepants). This review will analyze the preclinical experimental models currently known for the development of these therapeutic principles, which ar...Continue Reading

References

Sep 1, 1977·Agents and Actions·E Müller-Schweinitzer, H Weidmann
May 1, 1992·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·H E ConnorP P Humphrey
May 1, 1992·The American Journal of Psychiatry·E A WorkmanD Short
Dec 1, 1991·Trends in Pharmacological Sciences·P P Humphrey, W Feniuk
Jan 1, 1990·Journal of Cardiovascular Pharmacology·P R Saxena, C M Villalón
Jan 1, 1990·European Journal of Clinical Pharmacology·K JägerJ A Fischer
Mar 1, 1989·Cephalalgia : an International Journal of Headache·K KovácsS Komoly
Sep 1, 1989·Neurology·M D FerrariG W Bruyn
Jan 1, 1989·British Journal of Pharmacology·W FeniukM J Perren
Apr 1, 1987·Headache·F SicuteriA Bonazzi
Feb 1, 1985·Pflügers Archiv : European journal of physiology·P R Saxena, P D Verdouw
Jul 1, 1995·Nature Medicine·C WeillerH C Diener
Nov 1, 1993·Stroke; a Journal of Cerebral Circulation·D W Busija, W Meng
Oct 1, 1996·Brain : a Journal of Neurology·K L HoskinP J Goadsby
Jan 1, 1997·Neuroepidemiology·M Abdul Jabbar, A Ogunniyi
Jan 1, 1997·Journal of Receptor and Signal Transduction Research·D Hoyer, P P Humphrey

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Citations

Nov 16, 2013·CNS Drugs·Inger Jansen-OlesenJes Olesen
Mar 22, 2014·European Journal of Pharmacology·Alexey Y SokolovSergey S Panteleev
Jun 3, 2014·The Journal of Headache and Pain·Flóra Gölöncsér, Beáta Sperlágh
Aug 22, 2013·Expert Opinion on Drug Discovery·Sieneke LabruijereAntoinette Maassenvandenbrink
Sep 4, 2012·Pharmacology & Therapeutics·Lars EdvinssonAntoinette MaassenVanDenBrink
Jan 23, 2015·Cephalalgia : an International Journal of Headache·Enriqueta Muñoz-IslasCarlos M Villalón
Nov 12, 2016·Acupuncture in Medicine : Journal of the British Medical Acupuncture Society·Hui ZhangHui Zheng
Jun 3, 2011·Headache·Saurabh GuptaB Lee Peterlin
Mar 29, 2014·Current Opinion in Supportive and Palliative Care·Greg Dussor
Jun 19, 2019·International Journal of Molecular Sciences·Giuseppe TardioloEmanuela Mazzon
Jan 21, 2021·Expert Opinion on Drug Metabolism & Toxicology·Abimael González-HernándezCarlos M Villalón
Apr 6, 2020·Journal of Vascular Research·Bruno A Marichal-CancinoCarlos M Villalón

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