Discovery of small molecule antagonists of TRPV1

Bioorganic and Medicinal Chemistry Letters

Volumn 14, Issue 14, 2004, Pages 3631-3634

  Rami, Harshad K ^a   Thompson, Mervyn ^a   Wyman, Paul ^a   Jerman, Jeffrey C ^a   Egerton, Julie ^a   Brough, Stephen ^a   Stevens, Alexander J ^a   Randall, Andrew D ^a   Smart, Darren ^a   Gunthorpe, Martin J ^a   Davis, John B ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

Author keywords

SB 366791; SB 452533; TRPV1; Vanilloid antagonist; VR1

Indexed keywords

ACID; CALCIUM ION; CAPSAICIN; RECEPTOR BLOCKING AGENT; SB 452533; SODIUM CHLORIDE; UNCLASSIFIED DRUG; VANILLOID RECEPTOR 1;

ANIMAL CELL; ARTICLE; BINDING SITE; DRUG POTENCY; DRUG RECEPTOR BINDING; ELECTROPHYSIOLOGY; EMBRYO; FLUORESCENCE; HEAT; HUMAN; HUMAN CELL; NOCICEPTIVE STIMULATION; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION;

AMINOBIPHENYL COMPOUNDS; ANIMALS; BINDING SITES; CALCIUM; CAPSAICIN; CELL LINE; ELECTROPHYSIOLOGY; FLUORESCENCE; HEAT; HUMANS; HYDROGEN-ION CONCENTRATION; IMAGE ENHANCEMENT; PATCH-CLAMP TECHNIQUES; RATS; RECEPTORS, DRUG; STRUCTURE-ACTIVITY RELATIONSHIP; TRPV CATION CHANNELS;

EID: 2942620619     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2004.05.028     Document Type: Article

References (20)

1. Caterina M.J., Schumacher M.A., Tominaga M., Rosen T.A., Levine J.D., Julius D. Nature. 389:1997;816-824
2. Benham C.D., Davis J.B., Randall A.D. Neuropharamcology. 42:2002;873-888
3. Gunthorpe M.J., Benham C.D., Randall A., Davis J.B. Trends Pharmacol. Sci. 23:2002;183-191
4. Urban L., Campbell E.A., Panesar M., Patel S., Chaudhry N., Kane S., Buchheit K., Sandells B., James I.F. Pain. 89:2000;65-74
5. Forrest J.B., Camu F., Greer I.A., Kehlet H., Abdalla M., Bonnet F., Ebrahim S., Escolar G., Jage J., Pocock S., Velo S., Langman M.J.S., Bianchi Porro G., Samama M.M., Heitlinger E. Br. J. Anaesth. 88:2002;227-233
6. Bevan S., Hothi S., Hughes G., James I.F., Rang H.P., Shah K., Walpole C.S., Yeats J.C. Br. J. Pharmacol. 107:1992;544-552
7. Docherty R.J., Yeats J.C., Piper A.S. Br. J. Pharmacol. 121:1997;1461-1467
8. Liu L., Simon S.A. Neurosci. Lett. 228:1997;29-32
9. Gunthorpe M.J., Rami H.K., Jerman J.C., Smart D., Gill C.H., Soffin E.M., Luis Hannan S., Lappin S.C., Egerton J., Smith G.D., Worby A., Howett L., Owen D., Nasir S., Davies C.H., Thompson M., Wyman P.A., Randall A.D., Davis J.B. Neuropharmacology. 46:2004;133-149
10. Bakthavatchatam, R.; Blum, C. A.; Brielmann, H. L.; Caldwell, T. M.; De Lombaert, S. WO Patent 02/08221; Suh, H.; Oh, U. T.; Kim, H. D.; Lee, J. W.; Park, H. G.; Park, Y. H. WO Patent 02/16317, WO Patent 02/16318, WO Patent 02/16319; McIntyre, P.; James, I. F. U.S. Patent 6,406,908; Bo, Y. Y.; Chakrabarti, P. P.; Chen, N.; Doherty, E. M.; Fotsch, C. H. WO Patent 03/049702
11. Bakthavatchatam, R.; Blum, C. A.; Brielmann, H. L.; Caldwell, T. M.; De Lombaert, S. WO Patent 02/08221; Suh, H.; Oh, U. T.; Kim, H. D.; Lee, J. W.; Park, H. G.; Park, Y. H. WO Patent 02/16317, WO Patent 02/16318, WO Patent 02/16319; McIntyre, P.; James, I. F. U.S. Patent 6,406,908; Bo, Y. Y.; Chakrabarti, P. P.; Chen, N.; Doherty, E. M.; Fotsch, C. H. WO Patent 03/049702
12. Bakthavatchatam, R.; Blum, C. A.; Brielmann, H. L.; Caldwell, T. M.; De Lombaert, S. WO Patent 02/08221; Suh, H.; Oh, U. T.; Kim, H. D.; Lee, J. W.; Park, H. G.; Park, Y. H. WO Patent 02/16317, WO Patent 02/16318, WO Patent 02/16319; McIntyre, P.; James, I. F. U.S. Patent 6,406,908; Bo, Y. Y.; Chakrabarti, P. P.; Chen, N.; Doherty, E. M.; Fotsch, C. H. WO Patent 03/049702
13. Bakthavatchatam, R.; Blum, C. A.; Brielmann, H. L.; Caldwell, T. M.; De Lombaert, S. WO Patent 02/08221; Suh, H.; Oh, U. T.; Kim, H. D.; Lee, J. W.; Park, H. G.; Park, Y. H. WO Patent 02/16317, WO Patent 02/16318, WO Patent 02/16319; McIntyre, P.; James, I. F. U.S. Patent 6,406,908; Bo, Y. Y.; Chakrabarti, P. P.; Chen, N.; Doherty, E. M.; Fotsch, C. H. WO Patent 03/049702
14. Rami, H. K.; Thompson, M.; Wyman, P. WO Patent 02/072536
15. Smart D., Jerman J.C., Gunthorpe M.J., Brough S.J., Ranson J., Cairns W., Hayes P.D., Randall A.D., Davis J.B. Eur. J. Pharmacol. 417:2001;51-58
16. Jerman J.C., Gray J., Brough S.J., Ooi L., Owen D., Davis J.B., Smart D. Br. J. Anaesth. 89:2002;882-887
17. Jung J., Hwang S.W., Kwak J., Lee S., Kang C., Kim W.B., Kim D., Oh U. J. Neurosci. 19:1999;529-538
18. Vyklicky L., Lyfenko A., Kuffler D.P., Vlachova V. Neuroreport. 14:2003;1061-1065
19. Stevens, A. J. unpublished results. Intrinsic clearance rates in liver microsomes were rat >50 and human 41 mL/min/g liver
20. +=376, 378