Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C20H25ClN4O |
| Molecular Weight | 372.892 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)(C)C1=CC=C(NC(=O)N2CCN(CC2)C3=NC=CC=C3Cl)C=C1
InChI
InChIKey=ROGUAPYLUCHQGK-UHFFFAOYSA-N
InChI=1S/C20H25ClN4O/c1-20(2,3)15-6-8-16(9-7-15)23-19(26)25-13-11-24(12-14-25)18-17(21)5-4-10-22-18/h4-10H,11-14H2,1-3H3,(H,23,26)
| Molecular Formula | C20H25ClN4O |
| Molecular Weight | 372.892 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/12721338 | https://www.ncbi.nlm.nih.gov/pubmed/26689735Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/26870186
Sources: https://www.ncbi.nlm.nih.gov/pubmed/12721338 | https://www.ncbi.nlm.nih.gov/pubmed/26689735
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/26870186
BCTC is an orally effective mixed TRPV1/TRPM8 antagonist. Inhibits acid- and capsaicin-induced activation of rat TRPV1 receptors (IC50 values are 6.0 and 35 nM respectively). BCTC is shown to have robust antihyperalgesic properties
in rat models of inflammatory and neuropathic pain. TRPM8 specific antagonist BCTC demonstrated excellent anti-tumor activity in PCa DU145 cells, and therefore has the potential to become a targeted therapeutic strategy against PCa.
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| 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. | 2003 Jul |
|
| Anti-tumor activity of the TRPM8 inhibitor BCTC in prostate cancer DU145 cells. | 2016 Jan |
Sample Use Guides
Rats: Four groups of
rats (three per group) were dosed with BCTC under fasted conditions
at 3, 10, and 40 mg/kg p.o. or 3 mg/kg i.v. using 25% hydroxypropyl-
-cyclodextrin as vehicle. To study the CNS
permeability of BCTC, three rats received a single 10 mg/kg i.p.
administration of compound suspended in 20% hydroxypropyl--
cyclodextrin.
Route of Administration:
Other
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 15:20:12 GMT 2023
by
admin
on
Sat Dec 16 15:20:12 GMT 2023
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| Record UNII |
3HW474Y8YZ
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| Record Status |
Validated (UNII)
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