BCTC is a orally effective vanilloid receptor 1 (TRPV1 receptor) antagonist. BCTC is also a potent and specific inhibitor of transient receptor potential cation channel subfamily M member 8 (TRPM8) in prostate cancer (PCa) DU145 cells. BCTC inhibits acid- and capsaicin-induced activation of rat TRPV1 receptors (IC50 values are 6.0 and 35 nM respectively). BCTC displays analgesic properties in rat models of inflammatory and neuropathic pain.
|Animal models||Jugular-cannulated male Sprague-Dawley rats (200-300 g)|
|Formulation||using 25% hydroxypropyl-β-cyclodextrin as vehicle|
|Dosages||3, 10, and 40 mg/kg p.o. or 3 mg/kg i.v.|
|Administration||p.o. or i.v.|
|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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
|Solubility||DMSO ≥ 38 mg/mL|
Anti-tumor activity of the TRPM8 inhibitor BCTC in prostate cancer DU145 cells
Tao Liu, et al. Oncol Lett. 2016 Jan;11(1):182-188. PMID: 26870186.
N-(4-tertiarybutylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine -1(2H)-carbox-amide (BCTC), a novel, orally effective vanilloid receptor 1 antagonist with analgesic properties: I. in vitro characterization and pharmacokinetic properties
Kenneth J Valenzano, et al. J Pharmacol Exp Ther. 2003 Jul;306(1):377-86. PMID: 12721338.
Activity of cytisine and its brominated isoteres on recombinant human α7, α4β2 and α4β4 nicotinic acetylcholine receptors.
Houlihan, et al. J Neurochem. 2001;78: 1029. PMID: 11553677.
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