An antagonist of CRF1 (Ki = 2.7 nM); selective for CRF1 over CRF2 (Ki = >10 μM); inhibits CRF-induced increases in ACTH levels in rat plasma (ID50 = 10 mg/kg); increases the time spent in the open arms of the elevated plus maze in rats at 1 mg/kg; decreases immobility time in the forced swim test in a rat model of depressive-like behavior at 10 mg/kg

CP 154,526 (hydrochloride) – 1 mg

Brand:
Cayman
CAS:
257639-98-8
Storage:
-20
UN-No:
Non-Hazardous - /

CP 154,526 is an antagonist of corticotropin-releasing factor receptor 1 (CRF1; Ki = 2.7 nM).{49085,49086} It is selective for CRF1 over CRF2 (Ki = >10 μM).{49085} CP 154,526 inhibits CRF-induced increases in adrenocorticotropic hormone (ACTH) levels in rat plasma with an ID50 value of 10 mg/kg. It increases the time spent in the open arms of the elevated plus maze in rats when administered at a dose of 1 mg/kg.{49087} CP 154,526 (10 mg/kg, twice per day for 14 days) decreases immobility time in the forced swim test in a rat model of depressive-like behavior.{49088} It also decreases stress-induced reinstatement of cocaine or heroin self-administration in cocaine- and heroin-trained rats, respectively, when administered at doses of 15 and 30 mg/kg.{49090}  

 

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Description

An antagonist of CRF1 (Ki = 2.7 nM); selective for CRF1 over CRF2 (Ki = >10 μM); inhibits CRF-induced increases in ACTH levels in rat plasma (ID50 = 10 mg/kg); increases the time spent in the open arms of the elevated plus maze in rats at 1 mg/kg; decreases immobility time in the forced swim test in a rat model of depressive-like behavior at 10 mg/kg, twice per day for 14 days; decreases stress-induced reinstatement of cocaine or heroin self-administration in cocaine- and heroin-trained rats, respectively, at 15 and 30 mg/kg,

Formal name: N-butyl-N-ethyl-2,5-dimethyl-7-(2,4,6-trimethylphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine, monohydrochloride

Synonyms: 

Molecular weight: 401

CAS: 257639-98-8

Purity: ≥98%

Formulation: A crystalline solid

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

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