U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Approval Year

Substance Class Protein
Created
by admin
on Sat Dec 16 12:03:50 GMT 2023
Edited
by admin
on Sat Dec 16 12:03:50 GMT 2023
Protein Type RECEPTOR
Protein Sub Type HYDROXYTRYPTAMINE RECEPTOR
Sequence Origin HUMAN
Sequence Type COMPLETE
Record UNII
6E2Z4UWILI
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
5-HYDROXYTRYPTAMINE RECEPTOR 2B
Common Name English
5-HT2B
Common Name English
5HT2B
Common Name English
Code System Code Type Description
UNIPROT
P41595
Created by admin on Sat Dec 16 12:03:52 GMT 2023 , Edited by admin on Sat Dec 16 12:03:52 GMT 2023
PRIMARY
FDA UNII
6E2Z4UWILI
Created by admin on Sat Dec 16 12:03:52 GMT 2023 , Edited by admin on Sat Dec 16 12:03:52 GMT 2023
PRIMARY
From To
1_128 1_207
1_350 1_353
Glycosylation Type HUMAN
Glycosylation Link Type Site
N 1_30
Related Record Type Details
PARTIAL AGONIST->TARGET
INHIBITOR -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
INHIBITOR -> TARGET
Ki
PARTIAL AGONIST->TARGET
INHIBITOR -> TARGET
AGONIST->OFF-TARGET
5-HT2B receptors, which were subsequently identified as the target for cardiac valvulopathy and pulmonary hypertension. Release of serotonin leads to 5-HT2B signaling.
WEAK AGONIST->OFF TARGET
Ki
RADIOLIGAND->TARGET
Ki
AGONIST -> TARGET
Eletriptan binds with high affinity to 5-HT1B, 5-HT1D and 5-HT1F receptors, has modest affinity for 5-HT1A, 5-HT1E, 5-HT2B and 5-HT7 receptors
INHIBITOR -> TARGET
Acts as a mixed antagonist for the 5-HT2B and 5-HT2C serotonin receptors, with good selectivity over other serotonin receptor subtypes and slight preference for 5-HT2C over 5-HT2B.
ANTAGONIST
AGONIST -> TARGET
A full agonist.
Ki
INHIBITOR -> TARGET
AGONIST -> TARGET
BINDING
IC50
INHIBITOR -> TARGET
ANTAGONIST
PARTIAL AGONIST->TARGET
INHIBITOR -> TARGET
Ki
INHIBITOR -> TARGET
BINDING
IC50
INHIBITOR -> TARGET
INHIBITOR -> TARGET
ANTAGONIST
INVERSE AGONIST->TARGET
IC50
AGONIST -> TARGET
BINDING
IC50
INVERSE AGONIST->TARGET
Ki
INHIBITOR -> TARGET
Ki
INHIBITOR -> TARGET
AGONIST -> TARGET
Ki
AGONIST -> TARGET
AGONIST -> TARGET
INHIBITOR -> TARGET
AGONIST -> TARGET
WEAK AGONIST->OFF TARGET
Emax,40%
AGONIST -> TARGET
INHIBITOR -> TARGET
AGONIST->OFF-TARGET
5-HT2B receptors, which were subsequently identified as the target for cardiac valvulopathy and pulmonary hypertension. Release of serotonin leads to 5-HT2B signaling.
INHIBITOR -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
Ki
INHIBITOR -> TARGET
Ki
RADIOLIGAND->TARGET
Kd
INHIBITOR -> TARGET
ANTAGONIST
AGONIST->OFF-TARGET
Responsible for valvular heart disease (VHD) with the administration of phentermine and fenfluramine (phen/fen) and dexfenfluramine1 led to the withdrawal of fenfluramine and dexfenfluramine from the marketplace in September 1997.
Ki
AGONIST->OFF-TARGET
We propose that preferential stimulation of valvular 5-HT2B receptors by norfenfluramine, ergot drugs, or 5-HT released from carcinoid tumors (with or without accompanying 5-HT2A receptor activation) may contribute to valvular fibroplasia in humans.
Ki
AGONIST->OFF-TARGET
Indeed all drugs and drug metabolites that induce heart valvular disease in humans activate 5-HT2B receptors in vivo and in vitro and this activity is thought to be important for the development of fibrotic lesions upon chronic human administration.
Ki
AGONIST -> TARGET
Ki
Name Property Type Amount Referenced Substance Defining Parameters References
Molecular Formula CHEMICAL
MOL_WEIGHT CHEMICAL