393514-24-4 Usage
Description
BCTC (393514-24-4) is a vanilloid receptor I (TRPV1) blocker, IC50 = 35 nM for capsaicin-induced and 6 nM for acid-induced TRPV1 activation. Displays analgesic activity in rat models of neuropathic pain. BCTC is orally active and cell permeable.
Uses
BCTC is a antagonists of TRPA1 and TRPV1, a non-selective cation channel gated by noxious heat, vanilloids and extracellular protons. BCTC inhibits both capsaicin and proton activation.
References
1) Valenzano et al. (2003), 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; J. Pharmacol. Exp. Ther., 306 377
2) Pomonis et al. (2003), N-(4-Tertiarybutylphenyl)-4-(3-cholorphyridin-2-yl)tetrahydropyrazine -1(2H)-carbox-amide (BCTC), a novel, orally effective vanilloid receptor 1 antagonist with analgesic properties: II. in vivo characterization in rat models of inflammatory and neuropathic pain; J. Pharmacol. Exp. Ther., 306 387
Check Digit Verification of cas no
The CAS Registry Mumber 393514-24-4 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 3,9,3,5,1 and 4 respectively; the second part has 2 digits, 2 and 4 respectively.
Calculate Digit Verification of CAS Registry Number 393514-24:
(8*3)+(7*9)+(6*3)+(5*5)+(4*1)+(3*4)+(2*2)+(1*4)=154
154 % 10 = 4
So 393514-24-4 is a valid CAS Registry Number.
393514-24-4Relevant articles and documents
4-(2-Pyridyl)piperazine-1-carboxamides: Potent vanilloid receptor 1 antagonists
Sun, Qun,Tafesse, Laykea,Islam, Khondaker,Zhou, Xiaoming,Victory, Sam F.,Zhang, Chongwu,Hachicha, Mohamed,Schmid, Lori A.,Patel, Aniket,Rotshteyn, Yakov,Valenzano, Kenneth J.,Kyle, Donald J.
, p. 3611 - 3616 (2007/10/03)
A series of 4-(2-pyridyl)piperazine-1-carboxamide analogues based on the lead compound 1 was synthesized and evaluated for VR1 antagonist activity in capsaicin-induced (CAP) and pH (5.5)-induced (pH) FLIPR assays in a rat VR1-expressing HEK293 cell line. Potent VR1 antagonists were identified through SAR studies. From these studies, 18 was found to be very potent in the in vitro assay [IC50=4.8 nM (pH) and 35 nM (CAP)] and orally available in rat (F%=15.1).