Post hoc analysis shows that the prototypic non-peptide CRF1 receptor antagonist NBI30775 (R121919) and Verucerfont are both significantly different from vehicle, CP-316 311, and pexacerfont (P<0.001 for all comparisons collapse across time-points); the latter three treatments in turn do not differ from each other. A differential effect of treatments over time is also shown by a significant treatment×time interaction (F[20,140]=6.4, P<0.001). Accordingly, detailed Post hoc analysis shows that both NBI30775 and Verucerfont inhibit ACTH release throughout the following 6 h of measurement (P<0.001 vs vehicle at each time-point, and vs the respective pretreatment baseline)
|Animal models||Male Sprague-Dawley rats|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
The CRF1 Antagonist Verucerfont in Anxious Alcohol-Dependent Women: Translation of Neuroendocrine, But not of Anti-Craving Effects.
Schwandt ML, et al. Neuropsychopharmacology. 2016 Nov;41(12):2818-2829. PMID: 27109623.
Behavioral, biological, and chemical perspectives on targeting CRF(1) receptor antagonists to treat alcoholism.
Zorrilla EP, et al. Drug Alcohol Depend. 2013 Mar 1;128(3):175-86. PMID: 23294766.
Acecainide HCl, also known as N-acetylprocainamide and ASL 601, is the N-acetylated metabolite of procainamide.
Sematilide (CK-1752) hydrochloride is a novel class III antiarrhythmic agent.
EBE-A22 is a derivative of PD 153035, has no effect on EGF-R TK but maintains a high cytotoxic profile.
NIH-12848 is a putative phosphatidylinositol 5-phosphate 4-kinase γ (PI5P4Kγ) inhibitor.
CHS-828 (GMX1778) is a potent and specific inhibitor of NAMPT with IC50 and Kd value of <25 nM and 120 nM, respectively.
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