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.
Definition
ChEBI: 1-piperazinecarboxamide, 4-(3-chloro-2-pyridinyl)-n-[4-(1,1-dimethylethyl)phenyl]- is a member of piperazines and a member of pyridines.
in vivo
BCTC (1-30 mg/kg; Oral gavage; Single dose) can inhibit inflammatory and neuropathic heat pain and mechanical hyperalgesia in Sprague-Dawley rats by targeting VR1, which has analgesic effect[2].
BCTC (10-100 mg/kg; Oral gavage, Twice daily for 4 weeks) improves the insulin resistance and systemic glucose and lipid metabolism, and increase insulin secretion in diabetic ob/ob mice[5].
| Animal Model: | Capsaicin-induced Sprague-Dawley rats model[2] |
| Dosage: | 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg |
| Administration: | Oral gavage (p.o.), Single dose. Before capsaicin (HY-10448) treatment (30 μg; intraplantar injection; Single dose) |
| Result: | Inhibited capsaicin-mediated thermal hyperalgesia in a dose-dependent manner. |
| Animal Model: | Freund’s complete adjuvant (FCA) Sprague-Dawley rats model[2] |
| Dosage: | 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg |
| Administration: | Oral gavage (p.o.), Single dose. After 100 % FAC treatment (50 μL; intraplantar injection; Single dose) |
| Result: | Significantly reduced FAC-induced inflammation-related thermal pain and mechanical hyperalgesia, and extended the inhibitory effect of mechanical hyperalgesia to 6 h at high doses (10 mg/kg, 30 mg/kg). |
| Animal Model: | Partial sciatic nerve ligation Sprague-Dawley rats model[2] |
| Dosage: | 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg |
| Administration: | Oral gavage (p.o.), Single dose. After partial sciatic nerve ligation. |
| Result: | Reduced post-operative abnormal tactile pain and mechanical hyperalgesia in a dose-dependent manner. |
| Animal Model: | Particularly strong insulin resistance and hyperinsulinemia ob/ob mice model[5] |
| Dosage: | 10 mg/kg, 30 mg/kg, 100 mg/kg |
| Administration: | Oral gavage (p.o.); Twice daily for 4 weeks |
| Result: | Reduced plasma triglyceride and glucose area under the curve (AUC) level.
Decreased calcitonin gene-related peptide (CGRP) levels in a dose-dependent manner.
|
References
[1] KENNETH J VALENZANO. 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]. Journal of Pharmacology and Experimental Therapeutics, 2003, 306 1: 377-386. DOI:
10.1124/jpet.102.045674[2] JAMES D POMONIS. 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]. Journal of Pharmacology and Experimental Therapeutics, 2003, 306 1: 387-393. DOI:
10.1124/jpet.102.046268
