Stephen J Medhurst
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Explore the profile of Stephen J Medhurst including associated specialties, affiliations and a list of published articles.
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12
Citations
295
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Recent Articles
1.
Abberley L, Bebius A, Beswick P, Billinton A, Collis K, Dean D, et al.
Bioorg Med Chem Lett
. 2010 Oct;
20(22):6370-4.
PMID: 20934331
A backup molecule to compound 2 was sought by targeting the most likely metabolically vulnerable site in this molecule. Compound 18 was subsequently identified as a potent P2X(7) antagonist with...
2.
Abdi M, Beswick P, Billinton A, Chambers L, Charlton A, Collins S, et al.
Bioorg Med Chem Lett
. 2010 Aug;
20(17):5080-4.
PMID: 20673717
A computational lead-hopping exercise identified compound 4 as a structurally distinct P2X(7) receptor antagonist. Structure-activity relationships (SAR) of a series of pyroglutamic acid amide analogues of 4 were investigated and...
3.
Beswick P, Billinton A, Chambers L, Dean D, Fonfria E, Gleave R, et al.
Bioorg Med Chem Lett
. 2010 Jun;
20(15):4653-6.
PMID: 20579878
Structure-activity relationships (SAR) of analogues of lead compound 1 were investigated and compound 16 was selected for further study in animal models of pain. Compound 16 was shown to be...
4.
Westaway S, Thompson M, Rami H, Stemp G, Trouw L, Mitchell D, et al.
Bioorg Med Chem Lett
. 2008 Sep;
18(20):5609-13.
PMID: 18809327
6-Phenylnicotinamide (2) was previously identified as a potent TRPV1 antagonist with activity in an in vivo model of inflammatory pain. Optimization of this lead through modification of both the biaryl...
5.
Medhurst S, Hatcher J, Hille C, Bingham S, Clayton N, Billinton A, et al.
J Pain
. 2008 Apr;
9(7):580-7.
PMID: 18420461
Unlabelled: The role of specific nicotinic receptor (nAChR) subtypes in antinociception has not been fully elucidated because of the lack, until recently, of selective tool compounds. (R)-N-(1-azabicyclo[2.2.2]oct-3-yl)(5-(2-pyridyl)thiopene-2-carboxamide) (compound B) is...
6.
Medhurst S, Collins S, Billinton A, Bingham S, Dalziel R, Brass A, et al.
Pain
. 2008 Jan;
138(1):61-69.
PMID: 18164820
Several studies have implicated a potential role for histamine H(3) receptors in pain processing, although the data are somewhat conflicting. In the present study we investigated the effects of the...
7.
Medhurst A, Briggs M, Bruton G, Calver A, Chessell I, Crook B, et al.
Biochem Pharmacol
. 2007 Feb;
73(8):1182-94.
PMID: 17276409
GSK207040 (5-[(3-cyclobutyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)oxy]-N-methyl-2-pyrazinecarboxamide) and GSK334429 (1-(1-methylethyl)-4-({1-[6-(trifluoromethyl)-3-pyridinyl]-4-piperidinyl}carbonyl)hexahydro-1H-1,4-diazepine) are novel and selective non-imidazole histamine H(3) receptor antagonists from distinct chemical series with high affinity for human (pK(i)=9.67+/-0.06 and 9.49+/-0.09, respectively) and rat (pK(i)=9.08+/-0.16...
8.
N-Tetrahydroquinolinyl, N-quinolinyl and N-isoquinolinyl biaryl carboxamides as antagonists of TRPV1
Westaway S, Chung Y, Davis J, Holland V, Jerman J, Medhurst S, et al.
Bioorg Med Chem Lett
. 2006 Jun;
16(17):4533-6.
PMID: 16806913
Starting from the high throughput screening hit (3), novel N-tetrahydroquinolinyl, N-quinolinyl and N-isoquinolinyl carboxamides have been identified as potent antagonists of the ion channel TRPV1. The N-quinolinylnicotinamide (46) showed excellent...
9.
Elmes S, Winyard L, Medhurst S, Clayton N, Wilson A, Kendall D, et al.
Pain
. 2005 Nov;
118(3):327-335.
PMID: 16289798
The aim of the present study was to investigate the effects of cannabinoid agonists on established inflammatory hyperalgesia. We have compared the effects of pre-administration versus post-administration of a potent...
10.
Wilson A, Medhurst S, Dixon C, Bontoft N, Winyard L, Brackenborough K, et al.
Eur J Pain
. 2005 Oct;
10(6):537-49.
PMID: 16199187
Clinically, inflammatory pain is far more persistent than that typically modelled pre-clinically, with the majority of animal models focussing on short-term effects of the inflammatory pain response. The large attrition...