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Items: 39

1.

A novel series of benzimidazole NR2B-selective NMDA receptor antagonists.

Davies DJ, Crowe M, Lucas N, Quinn J, Miller DD, Pritchard S, Grose D, Bettini E, Calcinaghi N, Virginio C, Abberley L, Goldsmith P, Michel AD, Chessell IP, Kew JN, Miller ND, Gunthorpe MJ.

Bioorg Med Chem Lett. 2012 Apr 1;22(7):2620-3. doi: 10.1016/j.bmcl.2012.01.108. Epub 2012 Feb 6.

PMID:
22366657
2.

The spectrum of anticonvulsant efficacy of retigabine (ezogabine) in animal models: implications for clinical use.

Large CH, Sokal DM, Nehlig A, Gunthorpe MJ, Sankar R, Crean CS, Vanlandingham KE, White HS.

Epilepsia. 2012 Mar;53(3):425-36. doi: 10.1111/j.1528-1167.2011.03364.x. Epub 2012 Jan 5.

3.

The mechanism of action of retigabine (ezogabine), a first-in-class K+ channel opener for the treatment of epilepsy.

Gunthorpe MJ, Large CH, Sankar R.

Epilepsia. 2012 Mar;53(3):412-24. doi: 10.1111/j.1528-1167.2011.03365.x. Epub 2012 Jan 5. Review.

4.

Ototrauma induces sodium channel plasticity in auditory afferent neurons.

Fryatt AG, Mulheran M, Egerton J, Gunthorpe MJ, Grubb BD.

Mol Cell Neurosci. 2011 Sep;48(1):51-61. doi: 10.1016/j.mcn.2011.06.005. Epub 2011 Jun 25.

5.

The efficacy of sodium channel blockers to prevent phencyclidine-induced cognitive dysfunction in the rat: potential for novel treatments for schizophrenia.

Large CH, Bison S, Sartori I, Read KD, Gozzi A, Quarta D, Antolini M, Hollands E, Gill CH, Gunthorpe MJ, Idris N, Neill JC, Alvaro GS.

J Pharmacol Exp Ther. 2011 Jul;338(1):100-13. doi: 10.1124/jpet.110.178475. Epub 2011 Apr 12.

PMID:
21487071
6.

Voltage-gated sodium channel expression in rat spiral ganglion neurons.

Fryatt AG, Vial C, Mulheran M, Gunthorpe MJ, Grubb BD.

Mol Cell Neurosci. 2009 Dec;42(4):399-407. doi: 10.1016/j.mcn.2009.09.001. Epub 2009 Sep 16.

PMID:
19765660
7.

Targeting gut T cell Ca2+ release-activated Ca2+ channels inhibits T cell cytokine production and T-box transcription factor T-bet in inflammatory bowel disease.

Di Sabatino A, Rovedatti L, Kaur R, Spencer JP, Brown JT, Morisset VD, Biancheri P, Leakey NA, Wilde JI, Scott L, Corazza GR, Lee K, Sengupta N, Knowles CH, Gunthorpe MJ, McLean PG, MacDonald TT, Kruidenier L.

J Immunol. 2009 Sep 1;183(5):3454-62. doi: 10.4049/jimmunol.0802887. Epub 2009 Jul 31.

8.

Allosteric modulators of NR2B-containing NMDA receptors: molecular mechanisms and therapeutic potential.

Mony L, Kew JN, Gunthorpe MJ, Paoletti P.

Br J Pharmacol. 2009 Aug;157(8):1301-17. doi: 10.1111/j.1476-5381.2009.00304.x. Epub 2009 Jul 8. Review.

9.

Clinical development of TRPV1 antagonists: targeting a pivotal point in the pain pathway.

Gunthorpe MJ, Chizh BA.

Drug Discov Today. 2009 Jan;14(1-2):56-67. doi: 10.1016/j.drudis.2008.11.005. Epub 2008 Dec 26. Review.

PMID:
19063991
10.

Characterisation of 5-HT3C, 5-HT3D and 5-HT3E receptor subunits: evolution, distribution and function.

Holbrook JD, Gill CH, Zebda N, Spencer JP, Leyland R, Rance KH, Trinh H, Balmer G, Kelly FM, Yusaf SP, Courtenay N, Luck J, Rhodes A, Modha S, Moore SE, Sanger GJ, Gunthorpe MJ.

J Neurochem. 2009 Jan;108(2):384-96. doi: 10.1111/j.1471-4159.2008.05775.x. Epub 2008 Nov 29.

11.

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
12.

TRPA1 receptor localisation in the human peripheral nervous system and functional studies in cultured human and rat sensory neurons.

Anand U, Otto WR, Facer P, Zebda N, Selmer I, Gunthorpe MJ, Chessell IP, Sinisi M, Birch R, Anand P.

Neurosci Lett. 2008 Jun 20;438(2):221-7. doi: 10.1016/j.neulet.2008.04.007. Epub 2008 Apr 8.

PMID:
18456404
13.

Peripheral TRPV1 receptors as targets for drug development: new molecules and mechanisms.

Gunthorpe MJ, Szallasi A.

Curr Pharm Des. 2008;14(1):32-41. Review.

PMID:
18220816
14.

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
15.

Effects of pan- and subtype-selective N-methyl-D-aspartate receptor antagonists on cortical spreading depression in the rat: therapeutic potential for migraine.

Peeters M, Gunthorpe MJ, Strijbos PJ, Goldsmith P, Upton N, James MF.

J Pharmacol Exp Ther. 2007 May;321(2):564-72. Epub 2007 Jan 31.

PMID:
17267580
16.

The voltage-gated sodium channel Na(v)1.9 is an effector of peripheral inflammatory pain hypersensitivity.

Amaya F, Wang H, Costigan M, Allchorne AJ, Hatcher JP, Egerton J, Stean T, Morisset V, Grose D, Gunthorpe MJ, Chessell IP, Tate S, Green PJ, Woolf CJ.

J Neurosci. 2006 Dec 13;26(50):12852-60.

17.

TRPV1 antagonist, SB-366791, inhibits glutamatergic synaptic transmission in rat spinal dorsal horn following peripheral inflammation.

Lappin SC, Randall AD, Gunthorpe MJ, Morisset V.

Eur J Pharmacol. 2006 Jul 1;540(1-3):73-81. Epub 2006 May 6.

PMID:
16737693
18.

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
19.

An animal model of chronic inflammatory pain: pharmacological and temporal differentiation from acute models.

Wilson AW, Medhurst SJ, Dixon CI, Bontoft NC, Winyard LA, Brackenborough KT, De Alba J, Clarke CJ, Gunthorpe MJ, Hicks GA, Bountra C, McQueen DS, Chessell IP.

Eur J Pain. 2006 Aug;10(6):537-49. Epub 2005 Sep 30.

PMID:
16199187
20.

Conservation of functional and pharmacological properties in the distantly related temperature sensors TRVP1 and TRPM8.

Weil A, Moore SE, Waite NJ, Randall A, Gunthorpe MJ.

Mol Pharmacol. 2005 Aug;68(2):518-27. Epub 2005 May 23.

PMID:
15911692
21.

Effects of piperine, the pungent component of black pepper, at the human vanilloid receptor (TRPV1).

McNamara FN, Randall A, Gunthorpe MJ.

Br J Pharmacol. 2005 Mar;144(6):781-90.

22.

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
23.

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
24.

TRPV channels as temperature sensors.

Benham CD, Gunthorpe MJ, Davis JB.

Cell Calcium. 2003 May-Jun;33(5-6):479-87. Review.

PMID:
12765693
25.

TRPV3 is a temperature-sensitive vanilloid receptor-like protein.

Smith GD, Gunthorpe MJ, Kelsell RE, Hayes PD, Reilly P, Facer P, Wright JE, Jerman JC, Walhin JP, Ooi L, Egerton J, Charles KJ, Smart D, Randall AD, Anand P, Davis JB.

Nature. 2002 Jul 11;418(6894):186-90. Epub 2002 Jun 23.

PMID:
12077606
26.

Ethanol elicits and potentiates nociceptor responses via the vanilloid receptor-1.

Trevisani M, Smart D, Gunthorpe MJ, Tognetto M, Barbieri M, Campi B, Amadesi S, Gray J, Jerman JC, Brough SJ, Owen D, Smith GD, Randall AD, Harrison S, Bianchi A, Davis JB, Geppetti P.

Nat Neurosci. 2002 Jun;5(6):546-51.

PMID:
11992116
27.

The diversity in the vanilloid (TRPV) receptor family of ion channels.

Gunthorpe MJ, Benham CD, Randall A, Davis JB.

Trends Pharmacol Sci. 2002 Apr;23(4):183-91. Review.

PMID:
11931994
28.

Characterisation of a human acid-sensing ion channel (hASIC1a) endogenously expressed in HEK293 cells.

Gunthorpe MJ, Smith GD, Davis JB, Randall AD.

Pflugers Arch. 2001 Aug;442(5):668-74.

PMID:
11512022
30.

Characterisation using FLIPR of human vanilloid VR1 receptor pharmacology.

Smart D, Jerman JC, Gunthorpe MJ, Brough SJ, Ranson J, Cairns W, Hayes PD, Randall AD, Davis JB.

Eur J Pharmacol. 2001 Apr 6;417(1-2):51-8.

PMID:
11301059
31.
32.

Cloning and functional expression of a human orthologue of rat vanilloid receptor-1.

Hayes P, Meadows HJ, Gunthorpe MJ, Harries MH, Duckworth DM, Cairns W, Harrison DC, Clarke CE, Ellington K, Prinjha RK, Barton AJ, Medhurst AD, Smith GD, Topp S, Murdock P, Sanger GJ, Terrett J, Jenkins O, Benham CD, Randall AD, Gloger IS, Davis JB.

Pain. 2000 Nov;88(2):205-15.

PMID:
11050376
33.

Voltage- and time-dependent properties of the recombinant rat vanilloid receptor (rVR1).

Gunthorpe MJ, Harries MH, Prinjha RK, Davis JB, Randall A.

J Physiol. 2000 Jun 15;525 Pt 3:747-59.

34.
35.

Vanilloid receptor-1 is essential for inflammatory thermal hyperalgesia.

Davis JB, Gray J, Gunthorpe MJ, Hatcher JP, Davey PT, Overend P, Harries MH, Latcham J, Clapham C, Atkinson K, Hughes SA, Rance K, Grau E, Harper AJ, Pugh PL, Rogers DC, Bingham S, Randall A, Sheardown SA.

Nature. 2000 May 11;405(6783):183-7.

PMID:
10821274
36.

The endogenous lipid anandamide is a full agonist at the human vanilloid receptor (hVR1).

Smart D, Gunthorpe MJ, Jerman JC, Nasir S, Gray J, Muir AI, Chambers JK, Randall AD, Davis JB.

Br J Pharmacol. 2000 Jan;129(2):227-30.

37.
38.

Diltiazem causes open channel block of recombinant 5-HT3 receptors.

Gunthorpe MJ, Lummis SC.

J Physiol. 1999 Sep 15;519 Pt 3:713-22.

39.

Direct inhibition of 5-hydroxytryptamine3 receptors by antagonists of L-type Ca2+ channels.

Hargreaves AC, Gunthorpe MJ, Taylor CW, Lummis SC.

Mol Pharmacol. 1996 Nov;50(5):1284-94.

PMID:
8913360

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