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.
Evid Based Complement Alternat Med. 2022 Apr 13;2022:5731372.
Gallic Acid Inhibits Mesaconitine-Activated TRPV1-Channel-Induced Cardiotoxicity
BCTC purchased from AbMole
|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.|
|Solubility (25°C)||DMSO ≥ 38 mg/mL|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|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.
 Tao Liu, et al. Oncol Lett. Anti-tumor activity of the TRPM8 inhibitor BCTC in prostate cancer DU145 cells
 Kenneth J Valenzano, et al. J Pharmacol Exp Ther. 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
 Houlihan, et al. J Neurochem. Activity of cytisine and its brominated isoteres on recombinant human α7, α4β2 and α4β4 nicotinic acetylcholine receptors.
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