CP 376395是一种CRF1受体选择性拮抗剂。

CP 376395 is an effective and specific Corticotropin-releasing factor 1 (CRF1) receptor antagonist.

It is highly selective for the human CRF1 receptor subtype,and exhibits affinities against 40 neurotransmitter receptor and ion channels(>1 μM).

Pretreatment with CP 376395 (ID50=17.8 mg/kg, p.o.) reverses the excitation of locus coeruleus neurons induced by icv CRF (3 μg) completely blocked the enhanced startle response, while pretreatment with CP 376395(10 mg/kg, p.o.) induced by icv CRF (1 μg) is partially blocked.

In supernatants from cells, which are incubated in OSS_128167 (100 μM) for 18 hours,TNF-a levels are measured .

Beagle dogs weighing between 8 and 15 kg are administered with CP 376395 hydrochloride salt (1.0 mg/kg) into the cephalic vein of the foreleg. Beagle dogs are treated with CP 376395(10 mg/mL) prepared in 0.1% methyl cellulose at pH 2 by oral.

175140-00-8

C21H30N2O

326.484

CP-316311

H2O:< 0.1 mg/mL (insoluble)
DMSO:100 mg/mL (306.30 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years