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Items: 11

1.

Design and synthesis of 6-phenylnicotinamide derivatives as antagonists of TRPV1.

Westaway SM, Thompson M, Rami HK, Stemp G, Trouw LS, Mitchell DJ, Seal JT, Medhurst SJ, Lappin SC, Biggs J, Wright J, Arpino S, Jerman JC, Cryan JE, Holland V, Winborn KY, Coleman T, Stevens AJ, Davis JB, Gunthorpe MJ.

Bioorg Med Chem Lett. 2008 Oct 15;18(20):5609-13. doi: 10.1016/j.bmcl.2008.08.105. Epub 2008 Aug 31.

PMID:
18809327
2.

Characterization of SB-705498, a potent and selective vanilloid receptor-1 (VR1/TRPV1) antagonist that inhibits the capsaicin-, acid-, and heat-mediated activation of the receptor.

Gunthorpe MJ, Hannan SL, Smart D, Jerman JC, Arpino S, Smith GD, Brough S, Wright J, Egerton J, Lappin SC, Holland VA, Winborn K, Thompson M, Rami HK, Randall A, Davis JB.

J Pharmacol Exp Ther. 2007 Jun;321(3):1183-92. Epub 2007 Mar 28.

PMID:
17392405
3.

N-Tetrahydroquinolinyl, N-quinolinyl and N-isoquinolinyl biaryl carboxamides as antagonists of TRPV1.

Westaway SM, Chung YK, Davis JB, Holland V, Jerman JC, Medhurst SJ, Rami HK, Stemp G, Stevens AJ, Thompson M, Winborn KY, Wright J.

Bioorg Med Chem Lett. 2006 Sep 1;16(17):4533-6. Epub 2006 Jun 27.

PMID:
16806913
4.

Discovery of SB-705498: a potent, selective and orally bioavailable TRPV1 antagonist suitable for clinical development.

Rami HK, Thompson M, Stemp G, Fell S, Jerman JC, Stevens AJ, Smart D, Sargent B, Sanderson D, Randall AD, Gunthorpe MJ, Davis JB.

Bioorg Med Chem Lett. 2006 Jun 15;16(12):3287-91. Epub 2006 Mar 31.

PMID:
16580202
5.

3,4-Dihydro-2H-benzoxazinones are 5-HT(1A) receptor antagonists with potent 5-HT reuptake inhibitory activity.

Atkinson PJ, Bromidge SM, Duxon MS, Gaster LM, Hadley MS, Hammond B, Johnson CN, Middlemiss DN, North SE, Price GW, Rami HK, Riley GJ, Scott CM, Shaw TE, Starr KR, Stemp G, Thewlis KM, Thomas DR, Thompson M, Vong AK, Watson JM.

Bioorg Med Chem Lett. 2005 Feb 1;15(3):737-41.

PMID:
15664848
6.

Evidence for a molecular mechanism of teratogenicity of SB-236057, a 5-HT1B receptor inverse agonist that alters axial formation.

Augustine-Rauch KA, Zhang QJ, Leonard JL, Chadderton A, Welsh MJ, Rami HK, Thompson M, Gaster L, Wier PJ.

Birth Defects Res A Clin Mol Teratol. 2004 Oct;70(10):789-807.

PMID:
15472891
7.

Discovery of small molecule antagonists of TRPV1.

Rami HK, Thompson M, Wyman P, Jerman JC, Egerton J, Brough S, Stevens AJ, Randall AD, Smart D, Gunthorpe MJ, Davis JB.

Bioorg Med Chem Lett. 2004 Jul 16;14(14):3631-4.

PMID:
15203132
8.

Identification and characterisation of SB-366791, a potent and selective vanilloid receptor (VR1/TRPV1) antagonist.

Gunthorpe MJ, Rami HK, Jerman JC, Smart D, Gill CH, Soffin EM, Luis Hannan S, Lappin SC, Egerton J, Smith GD, Worby A, Howett L, Owen D, Nasir S, Davies CH, Thompson M, Wyman PA, Randall AD, Davis JB.

Neuropharmacology. 2004 Jan;46(1):133-49. Erratum in: Neuropharmacology. 2004 May;46(6):905.

PMID:
14654105
9.

Non-thiazolidinedione antihyperglycaemic agents. Part 3: The effects of stereochemistry on the potency of alpha-methoxy-beta-phenylpropanoic acids.

Haigh D, Allen G, Birrell HC, Buckle DR, Cantello BC, Eggleston DS, Haltiwanger RC, Holder JC, Lister CA, Pinto IL, Rami HK, Sime JT, Smith SA, Sweeney JD.

Bioorg Med Chem. 1999 May;7(5):821-30.

PMID:
10400335
10.

The contribution of classical (beta1/2-) and atypical beta-adrenoceptors to the stimulation of human white adipocyte lipolysis and right atrial appendage contraction by novel beta3-adrenoceptor agonists of differing selectivities.

Sennitt MV, Kaumann AJ, Molenaar P, Beeley LJ, Young PW, Kelly J, Chapman H, Henson SM, Berge JM, Dean DK, Kotecha NR, Morgan HK, Rami HK, Ward RW, Thompson M, Wilson S, Smith SA, Cawthorne MA, Stock MJ, Arch JR.

J Pharmacol Exp Ther. 1998 Jun;285(3):1084-95. Erratum in: J Pharmacol Exp Ther 1998 Dec;287(3):1135.

PMID:
9618411
11.

Bioreductive fluorescent markers for hypoxic cells: a study of 2-nitroimidazoles with 1-substituents containing fluorescent, bridgehead-nitrogen, bicyclic systems.

Hodgkiss RJ, Middleton RW, Parrick J, Rami HK, Wardman P, Wilson GD.

J Med Chem. 1992 May 15;35(10):1920-6.

PMID:
1588568

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