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Volumn 18, Issue 16, 2008, Pages 4569-4572

Discovery of piperidine carboxamide TRPV1 antagonists

Author keywords

Capsaicin; TRPV1; VR1

Indexed keywords

1 ACETYL 2,3 DIHYDROINDOL 5 YL; 1 ACETYL 2,3 DIHYDROINDOL 6 YL; 1 ACETYL 2,3 DIHYDROINDOL 7 YL; 3 OXO 3,4 DIHYDROBENZO[1,4]OXAZIN 6 YL; AMIDE; INDOL 4 YL; INDOL 5 YL; INDOL 6 YL; PIPERIDINE DERIVATIVE; QUINOLIN 3 YL; UNCLASSIFIED DRUG; VANILLOID RECEPTOR 1;

EID: 48849099961     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.07.035     Document Type: Article
Times cited : (20)

References (16)
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    • note
    • 2 (0.122 mmol) and triethylamine (0.183 mmol) were added sequentially into the acyl chloride solution at 0 °C. The reaction mixture was warmed to 25 °C and stirred for 20 min. Concentration of the solvent provided the residue, which was then purified by flash column chromatography with hexanes and ethyl acetate to afford the product. Spectral data have been reported: Calvo, Raul R.; Cheung, Wing S.; Player, Mark R. WO 06/058338.
  • 9
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    • note
    • 3H]-RTX binding assay used hVR1/HEK293 cell membranes. Both assays were carried out under conditions previously reported. Jetter, M. C.; Youngman, M. A.; McNally, J. J.; Zhang, S. -P.; Dubin, A. E.; Nasser, N.; Dax, S. L. Bioorg. Med. Chem. Lett. 2004, 14, 3053-3056.
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    • note
    • Complete Freunds adjuvant (CFA; 100 mL emulsion of saline and heat-killed Mycobacterium tuberculosis in mineral oil) was injected into a single hind paw of male Sprague-Dawley rats. Each rat was placed in a test chamber directly on a warm glass surface and acclimated for 10 min. Response latencies to the heat stimulus were recorded for each animal before and 24 h after the injection of CFA. Directly following the post-CFA latency measurement, test compound or hydroxymethylcellulose vehicle was administered orally to the animals. Post-treatment withdrawal latencies were assessed at 0, 30, 60, 100, and 180 min post-dose.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.