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Corticotropin-releasing hormone, also known as corticotropin-releasing factor (CRF) or corticoliberin, is a peptide hormone and neurotransmitter involved in the stress response. It is secreted from the hypothalamus and is the major regulator of pituitary corticotropin-release and consequent glucocorticoid secretion. NBI 35965 is a selective CRF receptor 1 (CRF1) antagonist with a Ki value of 4 nM. It does not inhibit CRF2 (Ki = >10,000 nM). NBI 35965 inhibits cAMP accumulation and adrenocorticotropic hormone (ACTH) production in vitro (pIC50s = 7.1 and 6.9, respectively) and reduces CRF- and stress-induced ACTH production in vivo. In animal models of stress, NBI 35965 administration produces anxiolytic effects.[Cayman Chemical] | [Uses]
NBI 35965 Hydrochloride is a potent and selective corticotropin-releasing factor 1 (CRF1) antagonist. | [Uses]
NBI 35965 Mesylate is a selective corticotropin-releasing factor (CRF1) receptor antagonist involved in stress response. | [in vivo]
NBI 35965 methanesulfonate (20 mg/kg; oral gavage; once) reduces stress induced ACTH production in mice[1].
In rats, NBI 35965 methanesulfonate (Compound 12a; 10 mg/kg) has a volume of distribution 17.8 L/kg, a plasma clearance of 17 mL/min/kg, and a half-life of 12 h. The estimated oral bioavailability is 34% with a mean maximal plasma concentration at 1 h of 560 ng/mL. NBI 35965 methanesulfonate also penetrated the blood-brain barrier, resulting in a mean maximal brain concentration of 700 ng/g[1]. | Animal Model: | Male CD-1 mice (24-26 g) bearing restraint stress[1] | | Dosage: | 20 mg/kg (10 mL/kg 5% mannitol-d (w/v) in water) | | Administration: | Oral gavage; 60 min prior to the initiation of the stressor | | Result: | Reduced stress induced ACTH production in vivo. |
| [IC 50]
CRFR1: 4 nM (Ki); CRFR1: 8.5 (pKi) | [storage]
Store at -20°C |
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