Zobrazeno 1 - 10
of 33
pro vyhledávání: '"Jeffrey C. Jerman"'
Publikováno v:
Label-Free Technologies for Drug Discovery
Autor:
Kim Winborn, Sarah C. Lappin, James S. Wright, Vicky Holland, Martin J. Gunthorpe, Harshad Kantilal Rami, Andrew D. Randall, Sandra Arpino, Graham D Smith, Julie Egerton, Stephen J. Brough, Mervyn Thompson, Jeffrey C. Jerman, Sara Luis Hannan, Darren Smart, John B. Davis
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 321:1183-1192
Vanilloid receptor-1 (TRPV1) is a nonselective cation channel, predominantly expressed by sensory neurons, which plays a key role in the detection of noxious painful stimuli such as capsaicin, acid, and heat. TRPV1 antagonists may represent novel the
Autor:
Jeffrey C. Jerman, Darren Smart, Andrew D. Randall, Becky Sargent, Steve Fell, Geoffrey Stemp, Harshad Kantilal Rami, Alexander J. Stevens, Dominic Sanderson, Martin J. Gunthorpe, John B. Davis, Mervyn Thompson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:3287-3291
Small molecule antagonists of the vanilloid receptor TRPV1 (also known as VR1) are disclosed. Pyrrolidinyl ureas such as 8 and 15 (SB-705498) emerged as lead compounds following optimisation of the previously described urea SB-452533. Pharmacological
Autor:
S. Nasir, Angela Worby, Catherine H. Gill, Harshad Kantilal Rami, Wyman Paul Adrian, Jeffrey C. Jerman, Andrew D. Randall, John B. Davis, Mervyn Thompson, Darren Smart, Julie Egerton, Ellen M. Soffin, Davina E. Owen, Graham D Smith, Ceri H. Davies, Sarah C. Lappin, Martin J. Gunthorpe, L. Howett, S. Luis Hannan
Publikováno v:
Neuropharmacology. 46:133-149
Vanilloid receptor-1 (TRPV1) is a non-selective cation channel, predominantly expressed by peripheral sensory neurones, which is known to play a key role in the detection of noxious painful stimuli, such as capsaicin, acid and heat. To date, a number
Autor:
Rosemary E. Kelsell, Andrew D. Randall, K. J. Charles, Jeffrey C. Jerman, James Wright, P. Reilly, Darren Smart, Praveen Anand, Julie Egerton, Paul Facer, Lezanne Ooi, Graham D Smith, Philip David Hayes, John B. Davis, Martin J. Gunthorpe, Jean-Philippe Walhin
Publikováno v:
Nature. 418:186-190
Vanilloid receptor-1 (VR1, also known as TRPV1) is a thermosensitive, nonselective cation channel that is expressed by capsaicin-sensitive sensory afferents and is activated by noxious heat, acidic pH and the alkaloid irritant capsaicin. Although VR1
Autor:
Martyn C. Coldwell, Jeffrey C. Jerman, Wai N. Chan, Phillip Jeffrey, Roderick A. Porter, Amanda Johns, Widdowson Katherine L, Nigel E. Austin, F Jewitt, Darren Smart, Steven Coulton, Michael S. Hadley, Stephen J. Brough
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:1907-1910
This communication reports SARs for the first orexin-1 receptor antagonist series of 1-aryl-3-quinolin-4-yl and 1-aryl-3-naphthyridin-4-yl ureas. One of these compounds, 31 (SB-334867), has excellent selectivity for the orexin-1 receptor, blood-brain
Publikováno v:
European Journal of Pharmacology. 424:211-219
The effects of three structurally related cannabinoids on human and rat recombinant vanilloid VR1 receptors expressed in human embryonic kidney (HEK293) cells and at endogenous vanilloid receptors in the rat isolated mesenteric arterial bed were stud
Autor:
Roderick A. Porter, Jeffrey C. Jerman, Stephen J. Brough, Darren Smart, C Sabido-David, A Johns, F Jewitt
Publikováno v:
British Journal of Pharmacology. 132:1179-1182
The pharmacology of various peptide and non-peptide ligands was studied in Chinese hamster ovary (CHO) cells stably expressing human orexin-1 (OX1) or orexin-2 (OX2) receptors by measuring intracellular calcium ([Ca2+]i) using Fluo-3AM. Orexin-A and
Autor:
Jeffrey C. Jerman, Derek N. Middlemiss, Martyn C. Coldwell, Darren Smart, Stephen J. Brough, Tracey Gager, Martyn D. Wood
Publikováno v:
European Journal of Pharmacology. 414:23-30
Prompted by conflicting literature, this study compared the pharmacology of human 5-hydroxytryptamine2 (5-HT2) receptors expressed in SH-SY5Y cells using a fluorometric imaging plate reader (FLIPR) based Ca2+ assay. 5-Hydroxytryptamine (5-HT) increas
Publikováno v:
European Journal of Pharmacology. 409:259-263
Bombesin and its receptors have been shown to have a role regulating circadian rhythms in the hamster suprachiasmatic and dorsal raphe nuclei and have been implicated in the regulation of sleep. We have identified and characterised a bombesin recepto