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Comparative Study
. 2012 Apr;153(4):830-838.
doi: 10.1016/j.pain.2012.01.005. Epub 2012 Feb 4.

mRNA expression of 5-hydroxytryptamine 1B, 1D, and 1F receptors and their role in controlling the release of calcitonin gene-related peptide in the rat trigeminovascular system

Dipak V Amrutkar  1 , Kenneth B Ploug, Anders Hay-Schmidt, Frank Porreca, Jes Olesen, Inger Jansen-Olesen
Affiliations
Comparative Study

mRNA expression of 5-hydroxytryptamine 1B, 1D, and 1F receptors and their role in controlling the release of calcitonin gene-related peptide in the rat trigeminovascular system

Dipak V Amrutkar et al. Pain. 2012 Apr.

Abstract

Triptans, a family of 5-hydroxytryptamine (5-HT) 1B, 1D, and 1F receptor agonists, are used in the acute treatment of migraine attacks. The site of action and subtypes of the 5-HT(1) receptor that mediate the antimigraine effect have still to be identified. This study investigated the mRNA expression of these receptors and the role of 5-HT(1) receptor subtypes in controlling the release of calcitonin gene-related peptide (CGRP) in rat dura mater, trigeminal ganglion (TG), and trigeminal nucleus caudalis (TNC). The mRNA for each receptor subtype was quantified by quantitative real-time polymerase chain reaction. A high potassium concentration was used to release CGRP from dura mater, isolated TG, and TNC in vitro. The immunoreactive CGRP (iCGRP) release was measured by enzyme-linked immunoassay. The mRNA transcripts of the 3 5-HT(1) receptor subtypes were detected in the trigeminovascular system. Sumatriptan inhibited iCGRP release by 31% in dura mater, 44% in TG, and 56% in TNC. This effect was reversed by a 5-HT(1B/1D) antagonist (GR127395). The 5-HT(1F) agonist (LY-344864) was effective in the dura mater (26% iCGRP inhibition), and the 5-HT(1D) agonist (PNU-142633) had a significant effect in the TNC (48%), whereas the 5-HT(1B) agonist (CP-94253) was unable to reduce the iCGRP release in all tissues studied. We found that sumatriptan reduced the iCGRP release via activation of 5-HT(1D) and 5-HT(1F) receptor subtypes. The 5-HT(1F) receptor agonist was effective only in peripheral terminals in dura mater, whereas the 5-HT(1D) agonist had a preferential effect on central terminals in the TNC.

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References

    1. Adell A, Celada P, Artigas F. The role of 5-HT1B receptors in the regulation of serotonin cell firing and release in the rat brain. J Neurochem. 2001;79:172-182.
    1. Adham N, Kao HT, Schecter LE, Bard J, Olsen M, Urquhart D, Durkin M, Hartig PR, Weinshank RL, Branchek TA. Cloning of another human serotonin receptor (5-HT1F): a fifth 5-HT1 receptor subtype coupled to the inhibition of adenylate cyclase. Proc Natl Acad Sci USA. 1993;90:408-412.
    1. Ahn SK, Khalmuratova R, Jeon SY, Kim JP, Park JJ, Hur DG, Kim DW, Balaban CD. Colocalization of 5-HT1F receptor and glutamate in neurons of the vestibular nuclei in rats. Neuroreport. 2009;20:111-115.
    1. Amrutkar DV, Ploug KB, Olesen J, Jansen-Olesen I. Role for voltage gated calcium channels in calcitonin gene-related peptide release in the rat trigeminovascular system. Neuroscience. 2011;172:510-517.
    1. Bonaventure P, Voorn P, Luyten WH, Leysen JE. 5HT1B and 5HT1D receptor mRNA differential co-localization with peptide mRNA in the guinea pig trigeminal ganglion. Neuroreport. 1998;9:641-645.

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