25CN-NBOH

Agonist of HTR2A, HTR2C, HTR2B

Structure

Information

Protein target names: HTR2A HTR2C HTR2B

Mechanism of action: Agonist

Recommended in-cell concentration:
up to 500 nM

In Vitro Validations

Uniprot ID: P28223
Target Class: GPCR
Target SubClass: Serotonin Receptor
Potency: Ki
Potency Value: 0.81 nM
Potency Assay: Radioligand competition binding assay performed using: [3H]LSD (data shown), [3H]Cimbi-36, ([3H]ketanserin), ([3H]mesulergine)
PDB ID for probe-target interaction (3D structure): 6WHA
Target aliases:
5-hydroxytryptamine receptor 2A, HTR2, HTR2A, 5HT2 ...

DOI Reference: 10.1021/cn400216u

In Cell Validations

In Vivo Data

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SERP ratings and comments


SERP Ratings

In Cell Rating
In Model Organisms

Comments:

Need to be aware compound is active on multiple targets - HTR2A, HTR2B, and HTR2C - when drawing biological conclusions from studies carried out with this compound.
Important to measure drug concentrations in any efficacy studies to put other pharmacology into context:  sigma-1 (Ki = 284 nM), α2C (Ki = 543 nM), 5-HT6 (Ki = 573 nM), sigma-2 (Ki = 575 nM), α2A (Ki = 803 nM)

(last updated: 25 Jul 2020 )

SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 4 Aug 2020 )

SERP Ratings

In Cell Rating
In Model Organisms

Comments:

Mode of in vivo delivery i.p or s.c. @ 1.5 mg/kg is indicated by Buchborn 2018.  Note potential for rapid desensitization in mouse models

(last updated: 13 Aug 2020 )