BCTC is a orally effective vanilloid receptor 1 (TRPV1 receptor) antagonist. Inhibits acid- and capsaicin-induced activation of rat TRPV1 receptors (IC50 values are 6.0 and 35 nM respectively). Displays analgesic properties in rat models of inflammatory and neuropathic pain. CNS penetrant.
|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.
|Solubility||DMSO ≥ 38 mg/mL|
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.
|Related TRP Channel Products|
AC1903 is a specific inhibitor of TRPC5 channel.
MK6-83 is an agonist of the transient receptor potential channel ML3 (TRPML3).
Nonivamide (also called pelargonic acid vanillylamide or PAVA) can activate the TRPV1 receptor, thus, stimulate the firing rate of dopaminergic neurons in the ventral tegmental area of the brain and to increase the expression of the serotonin receptor gene HTR2A.
HC-067047 is a potent, selective inhibitor of hTRPV4.
Capsazepine is a specific vanilloid receptor antagonist; synthetic analog of capsaicin.
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