Literature DB >> 8107508

Is migraine prophylactic activity caused by 5-HT2B or 5-HT2C receptor blockade?

H O Kalkman1.   

Abstract

It has been suggested that activation of 5-HT2C receptors is involved in the initiation of a migraine attack. The 5-HT2C receptor and the newly cloned rat fundus 5-HT2B receptor show close pharmacological and structural resemblance. Antagonist pA2 values from the rat stomach and pKD values from a 5-HT2C receptor binding assay correlated both highly significantly (p < 0.005) with the daily dose of eight migraine prophylactic compounds. Although the small difference in antimigraine potency between the enantiomers of propranolol agrees with the lack of stereo-selectivity found on the rat fundus 5-HT2B receptor but not with the 5-HT2C receptor, the evidence available does not allow one to distinguish between 5-HT2C and 5-HT2B receptor blockade as possible mechanisms for prophylactic activity.

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Year:  1994        PMID: 8107508     DOI: 10.1016/0024-3205(94)00546-x

Source DB:  PubMed          Journal:  Life Sci        ISSN: 0024-3205            Impact factor:   5.037


  14 in total

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Review 3.  Primary headache disorders and neuro-ophthalmologic manifestations.

Authors:  Daniel P Schwartz; Matthew S Robbins
Journal:  Eye Brain       Date:  2012-09-13

4.  Endothelial 5-HT receptors mediate relaxation of porcine pulmonary arteries in response to ergotamine and dihydroergotamine.

Authors:  E Glusa; A Roos
Journal:  Br J Pharmacol       Date:  1996-09       Impact factor: 8.739

5.  Psilocybin dose-dependently causes delayed, transient headaches in healthy volunteers.

Authors:  Matthew W Johnson; R Andrew Sewell; Roland R Griffiths
Journal:  Drug Alcohol Depend       Date:  2011-11-29       Impact factor: 4.492

Review 6.  Current Prophylactic Medications for Migraine and Their Potential Mechanisms of Action.

Authors:  Till Sprenger; M Viana; C Tassorelli
Journal:  Neurotherapeutics       Date:  2018-04       Impact factor: 7.620

7.  Agonist actions of dihydroergotamine at 5-HT2B and 5-HT2C receptors and their possible relevance to antimigraine efficacy.

Authors:  B Schaerlinger; P Hickel; N Etienne; L Guesnier; L Maroteaux
Journal:  Br J Pharmacol       Date:  2003-08-11       Impact factor: 8.739

8.  Prophylactic Therapy for Migraine.

Authors:  Shazia Afridi; Holger Kaube
Journal:  Curr Treat Options Neurol       Date:  2003-11       Impact factor: 3.598

Review 9.  Current and prospective pharmacological targets in relation to antimigraine action.

Authors:  Suneet Mehrotra; Saurabh Gupta; Kayi Y Chan; Carlos M Villalón; David Centurión; Pramod R Saxena; Antoinette MaassenVanDenBrink
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2008-07-15       Impact factor: 3.000

Review 10.  Cardiovascular responses produced by 5-hydroxytriptamine:a pharmacological update on the receptors/mechanisms involved and therapeutic implications.

Authors:  Carlos M Villalón; David Centurión
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2007-08-17       Impact factor: 3.000

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