5-hydroxytryptamine receptor 1B

UniProt P28222 Organism Homo sapiens Gene HTR1B, HTR1DB

Also known as: HTR1B, HTR1DB

Function

G protein-coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive substances, such as lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of downstream effectors, such as adenylate cyclase. HTR1B is coupled to G(i)/G(o) G alpha proteins and mediates inhibitory neurotransmission by inhibiting adenylate cyclase activity. Arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Regulates the release of 5-hydroxytryptamine, dopamine and acetylcholine in the brain, and thereby affects neural activity, nociceptive processing, pain perception, mood and behavior. Besides, plays a role in vasoconstriction of cerebral arteries.

Classification

Family (Pfam): PF00001 7tm_1
InterPro: 5HT1B_rcpt, 5HT_rcpt, GPCR_Rhodpsn, GPCR_Rhodpsn_7TM
Functional cluster: G Protein-Coupled Receptors

Experimental structures · PDB · 5

4IAQ X-ray 2.80A
4IAR X-ray 2.70A
5V54 X-ray 3.90A
6G79 EM 3.78A
7C61 X-ray 3.00A

A predicted model is available from AlphaFold.

Gene Ontology · 23

Drugs targeting this protein · 16

Related proteins · sequence + function similarity

Co-cited proteins · studied together in the literature

5-hydroxytryptamine receptor 1D 4 shared papers
5-hydroxytryptamine receptor 2B 4 shared papers
5-hydroxytryptamine receptor 1F 3 shared papers
5-hydroxytryptamine receptor 1E 3 shared papers
5-hydroxytryptamine receptor 1A 3 shared papers
Guanine nucleotide-binding protein G(o) subunit alpha 1 shared papers
5-hydroxytryptamine receptor 5A 1 shared papers
Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2 2 shared papers
5-hydroxytryptamine receptor 2A 2 shared papers
Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1 2 shared papers
5-hydroxytryptamine receptor 2C 1 shared papers
Guanine nucleotide-binding protein G(i) subunit alpha-1 1 shared papers

Literature · 20 cited papers

Structural insights into the ligand binding and Gi coupling of serotonin receptor 5-HT5A. Cell Discov. · 2022
Cryo-EM structure of the serotonin 5-HT1B receptor coupled to heterotrimeric Go. Nature · 2018
Structural features for functional selectivity at serotonin receptors. Science · 2013
Structural basis for molecular recognition at serotonin receptors. Science · 2013
Serotonin receptors - from molecular biology to clinical applications. Physiol. Res. · 2011
Serotonin receptors. Chem. Rev. · 2008
Triptan-induced contractile (5-HT1B receptor) responses in human cerebral and coronary arteries: relationship to clinical effect. Clin. Sci. · 2005
The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC). Genome Res. · 2004
Human-specific amino acid changes found in 103 protein-coding genes. Mol. Biol. Evol. · 2004
The DNA sequence and analysis of human chromosome 6. Nature · 2003
Serotonin 5-HT1B and 5-HT1D receptors form homodimers when expressed alone and heterodimers when co-expressed. FEBS Lett. · 1999
Human serotonin1B receptor expression in Sf9 cells: phosphorylation, palmitoylation, and adenylyl cyclase inhibition. Biochemistry · 1993
… and 8 more in the literature graph

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