An antagonist of the 5-HT6 receptor (Ki = 0.09 nM); selectively inhibits the 5-HT6 receptor over the 5-HT2B receptor (IC50s = 0.19 and 268 nM

AVN-492 – 10 mg

Brand:
Cayman
CAS:
1220646-23-0
Storage:
-20
UN-No:
Non-Hazardous - /

AVN-492 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT6 (Ki = 0.09 nM).{52052} It selectively inhibits the 5-HT6 receptor over the 5-HT2B receptor (IC50s = 0.19 and 268 nM, respectively, in a radioligand binding assay). AVN-492 inhibits increases in cAMP levels induced by 5-HT in HEK293 cells expressing the 5-HT6 receptor (IC50 = 1.5 nM). It increases the time spent in the open arms of the elevated plus maze in rats, indicating anxiolytic activity, when administered at a dose of 0.2 mg/kg. AVN-492 (1 mg/kg) also prevents memory deficits induced by the NMDA receptor antagonist MK-801 in a passive avoidance test.  

 

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SKU: 28079 - 10 mg Category:

Description

An antagonist of the 5-HT6 receptor (Ki = 0.09 nM); selectively inhibits the 5-HT6 receptor over the 5-HT2B receptor (IC50s = 0.19 and 268 nM, respectively, in a radioligand binding assay); inhibits increases in cAMP levels induced by 5-HT in HEK293 cells expressing the 5-HT6 receptor (IC50 = 1.5 nM); increases the time spent in the open arms of the elevated plus maze in rats, indicating anxiolytic activity, at 0.2 mg/kg; prevents memory deficits induced by MK-801 in a passive avoidance test at 1 mg/kg

Formal name: N2,N6,N6,5,7-pentamethyl-3-(phenylsulfonyl)-pyrazolo[1,5-a]pyrimidine-2,6-diamine

Synonyms: 

Molecular weight: 359.4

CAS: 1220646-23-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Neuroscience

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