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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.
Pain. 2012 Apr; 153(4):830-8.PAIN

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.

Authors+Show Affiliations

Department of Neurology and Danish Headache Center, Glostrup Research Institute, Glostrup Hospital, Faculty of Health Sciences, University of Copenhagen, Glostrup, Denmark.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

22305629

Citation

Amrutkar, Dipak V., et al. "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." Pain, vol. 153, no. 4, 2012, pp. 830-8.
Amrutkar DV, Ploug KB, Hay-Schmidt A, et al. 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. Pain. 2012;153(4):830-8.
Amrutkar, D. V., Ploug, K. B., Hay-Schmidt, A., Porreca, F., Olesen, J., & Jansen-Olesen, I. (2012). 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. Pain, 153(4), 830-8. https://doi.org/10.1016/j.pain.2012.01.005
Amrutkar DV, et al. 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. Pain. 2012;153(4):830-8. PubMed PMID: 22305629.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - 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. AU - Amrutkar,Dipak V, AU - Ploug,Kenneth B, AU - Hay-Schmidt,Anders, AU - Porreca,Frank, AU - Olesen,Jes, AU - Jansen-Olesen,Inger, Y1 - 2012/02/04/ PY - 2011/08/29/received PY - 2011/12/21/revised PY - 2012/01/06/accepted PY - 2012/2/7/entrez PY - 2012/2/7/pubmed PY - 2012/9/13/medline SP - 830 EP - 8 JF - Pain JO - Pain VL - 153 IS - 4 N2 - 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. SN - 1872-6623 UR - https://www.unboundmedicine.com/medline/citation/22305629/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_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0304-3959(12)00006-1 DB - PRIME DP - Unbound Medicine ER -