An inverse agonist of 5-HT receptor subtypes 5-HT2CINI and 5-HT2CVSV (Ki = 6.6 and 8.9 nM

S 32212 (hydrochloride) – 5 mg

Brand:
Cayman
CAS:
847871-78-7
Storage:
-20
UN-No:
Non-Hazardous - /

S 32212 is an inverse agonist of the serotonin (5-HT) receptor subtypes 5-HT2CINI and 5-HT2CVSV (Kis = 6.6 and 8.9 nM, respectively).{42934} It is also an antagonist of the 5-HT2A receptor and the α2B-adrenergic receptor (Ki = 5.8 nM for both). S 32212 is greater than 70-fold selective for these receptors in a panel of 80 receptors, enzymes, and ion channels. S 32212 reduces binding of GTPγS to Gαq and decreases the activity of phospholipase C (PLC) in HEK293 cells expressing 5-HT2CINI receptors (EC50s = 38 and 18.6 nM, respectively) and in CHO cells expressing 5-HT2CVSV receptors (EC50s = 38 and 18.6 nM, respectively). S 32212 (2.5 mg/kg) decreases head twitching, penile erections, and drug discrimination induced by 5-HT receptor agonists in mice and rats. It reduces immobility time in the forced swim test and decreases marble burying in mice and rats when administered at doses of 10 and 40 mg/kg, indicating anti-depressant-like and anxiolytic activities.{42934,42935}  

 

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Description

An inverse agonist of 5-HT receptor subtypes 5-HT2CINI and 5-HT2CVSV (Ki = 6.6 and 8.9 nM, respectively); an antagonist of the 5-HT2A receptor and the α2B-adrenergic receptors (Ki = 5.8 nM for both receptors); is greater than 70-fold selective for these receptors in a panel of 80 receptors, enzymes, and ion channels; reduces binding of GTPγS to Gαq and decreases the activity of PLC in HEK293 cells expressing 5-HT2CINI receptors (EC50s = 38 and 18.6 nM, respectively) and in CHO cells expressing 5-HT2CVSV receptors (EC50s = 38 and 18.6 nM, respectively); S 32212 (2.5 mg/kg) decreases head twitching, penile erections, and drug discrimination induced by 5-HT receptor agonists in mice and rats; reduces immobility in the forced swim test and decreases marble burying in mice and rats at 10 and 40 mg/kg, indicating anti-depressant-like and anxiolytic activities.

Formal name: 1,2-dihydro-N-[4-methoxy-3-(4-methyl-1-piperazinyl)phenyl]-3H-benz[e]indole-3-carboxamide, monohydrochloride

Synonyms: 

Molecular weight: 453

CAS: 847871-78-7

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Product Type|Biochemicals|Receptor Pharmacology|Inverse Agonists||Research Area|Neuroscience|Behavioral Neuroscience|Addiction Research||Research Area|Neuroscience|Behavioral Neuroscience|Anxiety||Research Area|Neuroscience|Behavioral Neuroscience|Depression

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