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 11:46:48 GMT 2023
Edited
by admin
on Sat Dec 16 11:46:48 GMT 2023
Protein Sub Type
Sequence Type COMPLETE
Record UNII
NQI5D806LC
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
5-HYDROXYTRYPTAMINE RECEPTOR 2A
Common Name English
5-HT2A
Common Name English
HTR2
Common Name English
5-HT-2
Common Name English
SEROTONIN RECEPTOR 2A
Common Name English
5-HT2A RECEPTOR
Common Name English
5HT2A
Common Name English
Code System Code Type Description
UNIPROT
P28223
Created by admin on Sat Dec 16 11:46:58 GMT 2023 , Edited by admin on Sat Dec 16 11:46:58 GMT 2023
PRIMARY
FDA UNII
NQI5D806LC
Created by admin on Sat Dec 16 11:46:58 GMT 2023 , Edited by admin on Sat Dec 16 11:46:58 GMT 2023
PRIMARY
PHAROS
P28223
Created by admin on Sat Dec 16 11:46:58 GMT 2023 , Edited by admin on Sat Dec 16 11:46:58 GMT 2023
PRIMARY
From To
1_148 1_227
1_349 1_353
Glycosylation Type HUMAN
Glycosylation Link Type Site
N 1_8
N 1_38
N 1_44
N 1_51
N 1_54
Related Record Type Details
WEAK AGONIST->TARGET
IC50
AGONIST -> TARGET
Moderate selectivity over related serotonin receptors. It has lower 5-HT2 affinity and efficacy than the related compound AL-37350A, but higher lipophilicity.
Ki
INVERSE AGONIST->TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
LIGAND->TARGET
INHIBITOR -> TARGET
INHIBITOR
Ki
AGONIST -> TARGET
AGONIST -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
Ki
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
MAJOR
Ki
AGONIST -> TARGET
EC50
AGONIST -> TARGET
AGONIST -> TARGET
EC50
RADIOLIGAND->TARGET
AGONIST -> TARGET
AGONIST -> TARGET
INHIBITOR -> TARGET
Ki
RADIOLIGAND->TARGET
AGONIST -> TARGET
INHIBITOR -> TARGET
Ki
INHIBITOR -> TARGET
AGONIST -> TARGET
Ki
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
AGONIST -> TARGET
Designed specifically as a peripherally selective drug, which does not cross the blood–brain barrier. AL-34662 has been shown to be potent and effective in the treatment of symptoms of glaucoma, with minimal side effects.
INHIBITOR -> TARGET
AGONIST -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
AGONIST -> TARGET
all of the tryptamines, including DMT but with the exception of psilocin, were more potent agonists at the 5-HT2A receptor than LSD in the assay that was used in the present study. LSD and psilocin were 5-HT2A receptor partial agonists, with 28% and 16% activation efficacy, respectively, whereas all of the other compounds presented higher 5-HT2A receptor activation efficacies (up to >80% for DiPT and 5-MeO-MiPT). DMT has 40 maximal receptor activation.
EC50
AGONIST -> TARGET
Ki
AGONIST -> TARGET
ANTAGONIST->TARGET
AGONIST -> TARGET
PARTIAL AGONIST->TARGET
INHIBITOR -> TARGET
RADIOLIGAND->TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
AGONIST -> TARGET
Ki
AGONIST -> TARGET
AGONIST -> TARGET
[125I]DOI was the radioligand.
Ki
RADIOLIGAND->TARGET
PARTIAL AGONIST->TARGET
INHIBITOR -> TARGET
Ki
INHIBITOR -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
Ki
RADIOLIGAND->TARGET
AGONIST->OFF-TARGET
Ki
PARTIAL AGONIST->TARGET
PARTIAL AGONIST->TARGET
Emax=23%
INHIBITOR -> TARGET
INHIBITOR -> TARGET
AGONIST -> TARGET
PARTIAL AGONIST->TARGET
BINDING
Ki
AGONIST -> TARGET
Ki
INHIBITOR -> TARGET
PRECLINICAL
IC50
AGONIST -> TARGET
AGONIST -> TARGET
PARTIAL AGONIST->TARGET
INHIBITOR -> TARGET
WEAK INHIBITOR->TARGET
Ki
INHIBITOR -> TARGET
PARTIAL AGONIST->TARGET
Emax=25%
EC50
RADIOLIGAND->TARGET
Kd
AGONIST -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
PARTIAL AGONIST->TARGET
Emax=11%
EC50
AGONIST -> TARGET
INHIBITOR -> TARGET
INHIBITOR
Ki
AGONIST -> TARGET
Could be an active psychedelic in humans, although it is not known to have been tested in humans and could be dangerous due to its strong inhibition of MAO-A.
INHIBITOR -> TARGET
RADIOLIGAND->TARGET
Ki
RADIOLIGAND->TARGET
Ki
PARTIAL AGONIST->TARGET
INVERSE AGONIST->TARGET
Was under development for the treatment of insomnia. Development was halted in December 2008 because the substance did not meet the trial's effectiveness endpoints.recently, nelotanserin has been repurposed for the treatment of Lewy body disease.
INHIBITOR -> TARGET
WEAK AGONIST->TARGET
Ki
WEAK AGONIST->TARGET
Hallucinogenic, 31% of the stimulation of 5-hydroxytryptamine. Stimulation of phosphoinositide hydrolysis.
EC50
INHIBITOR -> TARGET
IC50
INHIBITOR -> TARGET
Ki
AGONIST -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
AGONIST -> TARGET
Assumed target
INHIBITOR -> TARGET
PARTIAL AGONIST->TARGET
Ki
INHIBITOR -> TARGET
BINDING
IC50
INHIBITOR -> TARGET
INHIBITOR -> TARGET
AGONIST -> TARGET
BINDING
IC50
AGONIST -> TARGET
INHIBITOR -> TARGET
AGONIST -> TARGET
INVERSE AGONIST->TARGET
Experimental drug for the treatment of insomnia.
AGONIST -> TARGET
INHIBITOR -> TARGET
INVERSE AGONIST->TARGET
AGONIST
Ki
RADIOLIGAND->TARGET
AGONIST -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
ANTAGONIST
INHIBITOR -> TARGET
INHIBITOR -> TARGET
Ki
AGONIST -> TARGET
May be an agonist
INHIBITOR -> TARGET
BINDING
IC50
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
Ki
AGONIST -> TARGET
Ki
ANTAGONIST->TARGET
BINDING
Ki
INHIBITOR -> TARGET
NON-AGONIST->OFF-TARGET
Pyr-T produces few to no effects in humans, but some behavioral changes were observed in animal tests.
INHIBITOR -> TARGET
AGONIST -> TARGET
INHIBITOR -> TARGET
BINDING
IC50
PARTIAL AGONIST->TARGET
AGONIST -> TARGET
INHIBITOR -> TARGET
WEAK AGONIST->OFF TARGET
EC50
INHIBITOR -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
INHIBITOR -> TARGET
AGONIST -> TARGET
PARTIAL AGONIST->TARGET
AGONIST -> TARGET
INHIBITOR -> TARGET
cell:CHO; ligand: 3-H-KETASERIN
BINDING
Ki
PARTIAL AGONIST->TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
Ki
INHIBITOR -> TARGET
Kd
INHIBITOR -> TARGET
PARTIAL AGONIST->TARGET
AGONIST -> TARGET
INHIBITOR -> TARGET
AGONIST -> TARGET
PARTIAL AGONIST->TARGET
Ki
INHIBITOR -> TARGET
LIGAND->TARGET
INHIBITOR -> TARGET
AGONIST -> TARGET
Retains reasonable potency, with a similar 5-HT2A receptor affinity to MiPT but better selectivity over the 5-HT1A and 5-HT2B subtypes.
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
RADIOLIGAND->TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
Kd
AGONIST -> TARGET
Ki
Name Property Type Amount Referenced Substance Defining Parameters References
MOL_WEIGHT CHEMICAL
Molecular Formula CHEMICAL