TARGETID

T31204

FORMERID

TTDS00104

UNIPROID

5HT2B_HUMAN

TARGNAME

5-HT 2B receptor (HTR2B)

GENENAME

HTR2B

TARGTYPE

Successful target

SYNONYMS

Serotonin receptor 2B; 5-hydroxytryptamine receptor 2B; 5-HT2B; 5-HT-2B; 5-HT 2B

FUNCTION

Functions as a receptor for various ergot alkaloid derivatives and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors. Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Signaling activates a phosphatidylinositol-calcium second messenger system that modulates the activity of phosphatidylinositol 3-kinase and down-stream signaling cascades and promotes the release of Ca(2+) ions from intracellular stores. Plays a role in the regulation of dopamine and 5-hydroxytryptamine release, 5-hydroxytryptamine uptake and in the regulation of extracellular dopamine and 5-hydroxytryptamine levels, and thereby affects neural activity. May play a role in the perception of pain. Plays a role in the regulation of behavior, including impulsive behavior. Required for normal proliferation of embryonic cardiac myocytes and normal heart development. Protects cardiomyocytes against apoptosis. Plays a role in the adaptation of pulmonary arteries to chronic hypoxia. Plays a role in vasoconstriction. Required for normal osteoblast function and proliferation, and for maintaining normal bone density. Required for normal proliferation of the interstitial cells of Cajal in the intestine. G-protein coupled receptor for 5-hydroxytryptamine (serotonin).

PDBSTRUC

6DS0; 6DRZ; 6DRY; 6DRX; 5TVN

BIOCLASS

GPCR rhodopsin

SEQUENCE

MALSYRVSELQSTIPEHILQSTFVHVISSNWSGLQTESIPEEMKQIVEEQGNKLHWAALLILMVIIPTIGGNTLVILAVSLEKKLQYATNYFLMSLAVADLLVGLFVMPIALLTIMFEAMWPLPLVLCPAWLFLDVLFSTASIMHLCAISVDRYIAIKKPIQANQYNSRATAFIKITVVWLISIGIAIPVPIKGIETDVDNPNNITCVLTKERFGDFMLFGSLAAFFTPLAIMIVTYFLTIHALQKKAYLVKNKPPQRLTWLTVSTVFQRDETPCSSPEKVAMLDGSRKDKALPNSGDETLMRRTSTIGKKSVQTISNEQRASKVLGIVFFLFLLMWCPFFITNITLVLCDSCNQTTLQMLLEIFVWIGYVSSGVNPLVYTLFNKTFRDAFGRYITCNYRATKSVKTLRKRSSKIYFRNPMAENSKFFKKHGIRNGINPAMYQSPMRLRSSTIQSSSIILLDTLLLTENEGDKTEEQVSYV

DRUGINFO

Metergolin

DRUGINFO

Minaprine

DRUGINFO

Triflupromazine

DRUGINFO

SPN-812

DRUGINFO

PRX-08066

DRUGINFO

Vabicaserin

DRUGINFO

Pyrazole-3-carboxamide derivative 1

DRUGINFO

Pyrimidine derivative 23

DRUGINFO

Pyrimidine derivative 24