Cloning of another human serotonin receptor (5-HT1F): a fifth 5-HT1 receptor subtype coupled to the inhibition of adenylate cyclase. | Zendy

Nika Adham | Zendy; HungTeh Kao | Zendy; L E Schecter | Zendy; Jonathan Bard | Zendy; Michael A. Olsen | Zendy; Deborah A. Urquhart | Zendy; Margaret M. Durkin | Zendy; Paul Hartig | Zendy; Richard L. Weinshank | Zendy; T. A. Branchek | Zendy

Open Access

Cloning of another human serotonin receptor (5-HT1F): a fifth 5-HT1 receptor subtype coupled to the inhibition of adenylate cyclase.

Author(s) -

Nika Adham,

HungTeh Kao,

L E Schecter,

Jonathan Bard,

Michael A. Olsen,

Deborah A. Urquhart,

Margaret M. Durkin,

Paul Hartig,

Richard L. Weinshank,

T. A. Branchek

Publication year - 1993

Publication title -

proceedings of the national academy of sciences

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 5.011

H-Index - 771

eISSN - 1091-6490

pISSN - 0027-8424

DOI - 10.1073/pnas.90.2.408

Subject(s) - 5 ht1 receptor , spiperone , 5 ht2a receptor , receptor , biology , cyclase , 5 ht7 receptor , 5 ht receptor , serotonin , adenylate kinase , microbiology and biotechnology , medicine , biochemistry

An intronless gene encoding an additional human serotonin (5-HT) 5-HT1-like receptor subtype was isolated from a human genomic library with probes obtained from degenerate PCR primers used to amplify 5-HT-receptor-specific sequences. The highest degree of homology was found with the 5-HT1E subtype (70%) and the 5-HT1D alpha (63%) and 5-HT1D beta (60%) receptors. RNA for this gene was detected in the human brain but was not detected in kidney, liver, spleen, heart, pancreas, and testes. High-affinity (Kd = 9.2 nM) 3H-labeled 5-HT binding was detected. Competition studies revealed the following rank order of potencies for serotonergic ligands: 5-HT > sumatriptan >> 5-carboxyamidotryptamine > 8-hydroxy-2(di-1-propylamino)tetralin > spiperone. 5-HT produced a dose-dependent inhibition of forskolin-stimulated cAMP accumulation (EC50 = 7.9 nM) in transfected cells. These properties distinguish this receptor from any previously characterized and establish a fifth 5-HT1-like receptor subtype (5-HT1F) coupled to the inhibition of adenylate cyclase.

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