A nonpeptide NK2 receptor antagonist; binds to NK2 receptors (Ki = 0.32 nM); selective for NK2 over NK1 and NK3 receptors in radioligand binding assays (Kis = 5

GR159897 – 5 mg

Brand:
Cayman
CAS:
158848-32-9
Storage:
-20
UN-No:
- /

GR159897 is a nonpeptide antagonist of the neurokinin-2 (NK2) receptor.{60141} It binds to NK2 receptors (Ki = 0.32 nM) and is selective for NK2 over NK1 and NK3 receptors in radioligand binding assays (Kis = 5,010 and >1,000 nM, respectively). GR159897 inhibits contractions induced by the NK2 receptor agonist GR64349 in isolated guinea pig trachea (pA2 = 8.7). In vivo GR159897 (0.12 mg/kg) inhibits GR64349-induced bronchoconstriction in anesthetized guinea pigs. GR159897 (0.2-50 µg/kg) increases the amount of time spent in the front of the cage during confrontation with a human observer, a marker of anxiolytic-like activity, in marmosets.{60142}  

 

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SKU: 32774 - 5 mg Category:

Description

A nonpeptide NK2 receptor antagonist; binds to NK2 receptors (Ki = 0.32 nM); selective for NK2 over NK1 and NK3 receptors in radioligand binding assays (Kis = 5,010 and >1,000 nM, respectively); inhibits GR64349-induced contractions in isolated guinea pig trachea (pA2 = 8.7); inhibits GR64349-induced bronchoconstriction in anesthetized guinea pigs at 0.12 mg/kg; increases the amount of time spent in the front of the cage during confrontation with a human observer in marmosets from 0.2-50 µg/kg

Formal name: 5-fluoro-3-[2-[4-methoxy-4-[[(R)-phenylsulfinyl]methyl]-1-piperidinyl]ethyl]-1H-indole

Synonyms: 

Molecular weight: 414.5

CAS: 158848-32-9

Purity: ≥98%

Formulation: A solid

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