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Items: 31

1.

8-Piperazinyl-2,3-dihydropyrrolo[3,2-g]isoquinolines: potent, selective, orally bioavailable 5-HT1 receptor ligands.

Heightman TD, Gaster LM, Pardoe SL, Pilleux JP, Hadley MS, Middlemiss DN, Price GW, Roberts C, Scott CM, Watson JM, Gordon LJ, Holland VA, Powles J, Riley GJ, Stean TO, Trail BK, Upton N, Austin NE, Ayrton AD, Coleman T, Cutler L.

Bioorg Med Chem Lett. 2005 Oct 1;15(19):4370-4.

PMID:
16039851
2.

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
3.

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
4.

SB-431542 is a potent and specific inhibitor of transforming growth factor-beta superfamily type I activin receptor-like kinase (ALK) receptors ALK4, ALK5, and ALK7.

Inman GJ, Nicolás FJ, Callahan JF, Harling JD, Gaster LM, Reith AD, Laping NJ, Hill CS.

Mol Pharmacol. 2002 Jul;62(1):65-74.

PMID:
12065756
5.

Inhibition of transforming growth factor (TGF)-beta1-induced extracellular matrix with a novel inhibitor of the TGF-beta type I receptor kinase activity: SB-431542.

Laping NJ, Grygielko E, Mathur A, Butter S, Bomberger J, Tweed C, Martin W, Fornwald J, Lehr R, Harling J, Gaster L, Callahan JF, Olson BA.

Mol Pharmacol. 2002 Jul;62(1):58-64.

PMID:
12065755
6.

Identification of novel inhibitors of the transforming growth factor beta1 (TGF-beta1) type 1 receptor (ALK5).

Callahan JF, Burgess JL, Fornwald JA, Gaster LM, Harling JD, Harrington FP, Heer J, Kwon C, Lehr R, Mathur A, Olson BA, Weinstock J, Laping NJ.

J Med Chem. 2002 Feb 28;45(5):999-1001.

PMID:
11855979
7.

SB-272183, a selective 5-HT(1A), 5-HT(1B) and 5-HT(1D) receptor antagonist in native tissue.

Watson J, Roberts C, Scott C, Kendall I, Collin L, Day NC, Harries MH, Soffin E, Davies CH, Randall AD, Heightman T, Gaster L, Wyman P, Parker C, Price GW, Middlemiss DN.

Br J Pharmacol. 2001 Jul;133(6):797-806.

8.

The effect of SB-236057-A, a selective 5-HT1B receptor inverse agonist, on in vivo extracellular 5-HT levels in the freely-moving guinea-pig.

Roberts C, Hatcher P, Hagan JJ, Austin NE, Jeffrey P, Wyman P, Gaster LM, Routledge C, Middlemiss DN.

Naunyn Schmiedebergs Arch Pharmacol. 2000 Aug;362(2):177-83.

PMID:
10961381
9.

Biarylcarbamoylindolines are novel and selective 5-HT(2C) receptor inverse agonists: identification of 5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]- 5-pyridyl]carbamoyl]-6-trifluoromethylindoline (SB-243213) as a potential antidepressant/anxiolytic agent.

Bromidge SM, Dabbs S, Davies DT, Davies S, Duckworth DM, Forbes IT, Gaster LM, Ham P, Jones GE, King FD, Mulholland KR, Saunders DV, Wyman PA, Blaney FE, Clarke SE, Blackburn TP, Holland V, Kennett GA, Lightowler S, Middlemiss DN, Trail B, Riley GJ, Wood MD.

J Med Chem. 2000 Mar 23;43(6):1123-34.

PMID:
10737744
10.

SB-236057, a selective 5-HT1B receptor inverse agonist, blocks the 5-HT human terminal autoreceptor.

Middlemiss DN, Göthert M, Schlicker E, Scott CM, Selkirk JV, Watson J, Gaster LM, Wyman P, Riley G, Price GW.

Eur J Pharmacol. 1999 Jun 30;375(1-3):359-65.

PMID:
10443589
11.

The selective 5-HT1B receptor inverse agonist SB-224289, potently blocks terminal 5-HT autoreceptor function both in vitro and in vivo.

Gaster LM, Ham P, Joiner GF, King FD, Mulholland KR, Wyman PA, Hagan JJ, Price GW, Roberts C, Routledge C, Selkirk J, Slade PD, Middlemiss DN.

Ann N Y Acad Sci. 1998 Dec 15;861:270-1. No abstract available.

PMID:
9928285
12.

SB-224289--a novel selective (human) 5-HT1B receptor antagonist with negative intrinsic activity.

Selkirk JV, Scott C, Ho M, Burton MJ, Watson J, Gaster LM, Collin L, Jones BJ, Middlemiss DN, Price GW.

Br J Pharmacol. 1998 Sep;125(1):202-8.

13.

The selective 5-HT1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2, 4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydro- spiro[furo[2,3-f]indole-3,4'-piperidine] (SB-224289) potently blocks terminal 5-HT autoreceptor function both in vitro and in vivo.

Gaster LM, Blaney FE, Davies S, Duckworth DM, Ham P, Jenkins S, Jennings AJ, Joiner GF, King FD, Mulholland KR, Wyman PA, Hagan JJ, Hatcher J, Jones BJ, Middlemiss DN, Price GW, Riley G, Roberts C, Routledge C, Selkirk J, Slade PD.

J Med Chem. 1998 Apr 9;41(8):1218-35.

PMID:
9548813
14.

Effects of selective h5-HT1B (SB-216641) and h5-HT1D (BRL-15572) receptor ligands on guinea-pig and human 5-HT auto- and heteroreceptors.

Schlicker E, Fink K, Molderings GJ, Price GW, Duckworth M, Gaster L, Middlemiss DN, Zentner J, Likungu J, Göthert M.

Naunyn Schmiedebergs Arch Pharmacol. 1997 Sep;356(3):321-7.

PMID:
9303568
15.

SB-216641 and BRL-15572--compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors.

Price GW, Burton MJ, Collin LJ, Duckworth M, Gaster L, Göthert M, Jones BJ, Roberts C, Watson JM, Middlemiss DN.

Naunyn Schmiedebergs Arch Pharmacol. 1997 Sep;356(3):312-20.

PMID:
9303567
16.

Stimulation of 5-HT1B receptors causes hypothermia in the guinea pig.

Hagan JJ, Slade PD, Gaster L, Jeffrey P, Hatcher JP, Middlemiss DN.

Eur J Pharmacol. 1997 Jul 23;331(2-3):169-74.

PMID:
9274976
17.

Importance of h5-HT1B receptor selectivity for 5-HT terminal autoreceptor activity: an in vivo microdialysis study in the freely-moving guinea-pig.

Roberts C, Price GW, Gaster L, Jones BJ, Middlemiss DN, Routledge C.

Neuropharmacology. 1997 Apr-May;36(4-5):549-57.

PMID:
9225280
18.

Serotonin 5-HT3 and 5-HT4 receptor antagonists.

Gaster LM, King FD.

Med Res Rev. 1997 Mar;17(2):163-214. Review. No abstract available.

PMID:
9057164
19.

Increased defaecation caused by 5-HT4 receptor activation in the mouse.

Banner SE, Smith MI, Bywater D, Gaster LM, Sanger GJ.

Eur J Pharmacol. 1996 Jul 18;308(2):181-6.

PMID:
8840130
20.

Selective and functional 5-hydroxytryptamine4 receptor antagonism by SB 207266.

Wardle KA, Bingham S, Ellis ES, Gaster LM, Rushant B, Smith MI, Sanger GJ.

Br J Pharmacol. 1996 Jun;118(3):665-70.

21.

Azabicyclic indole esters as potent 5-HT4 receptor antagonists.

Wyman PA, Gaster LM, King FD, Sutton JM, Ellis ES, Wardle KA, Young TJ.

Bioorg Med Chem. 1996 Feb;4(2):255-61.

PMID:
8814883
22.

N-[(1-butyl-4-piperidinyl)methyl]-3,4dihydro-2H-[1,3]oxazino[3,2- a]indole10-carboxamide hydrochloride: the first potent and selective 5-HT4 receptor antagonist amide with oral activity.

Gaster LM, Joiner GF, King FD, Wyman PA, Sutton JM, Bingham S, Ellis ES, Sanger GJ, Wardle KA.

J Med Chem. 1995 Nov 24;38(24):4760-3. No abstract available.

PMID:
7490724
23.

Antagonism by SB 204070 of 5-HT-evoked contractions in the dog stomach: an in-vivo model of 5-HT4 receptor function.

Bingham S, King BF, Rushant B, Smith MI, Gaster L, Sanger GJ.

J Pharm Pharmacol. 1995 Mar;47(3):219-22.

PMID:
7602484
24.

The effects of SB 204070, a highly potent and selective 5-HT4 receptor antagonist, on guinea-pig distal colon.

Wardle KA, Ellis ES, Baxter GS, Kennett GA, Gaster LM, Sanger GJ.

Br J Pharmacol. 1994 Jul;112(3):789-94.

25.

Blockade of human atrial 5-HT4 receptors by SB 207710, a selective and high affinity 5-HT4 receptor antagonist.

Kaumann AJ, Gaster LM, King FD, Brown AM.

Naunyn Schmiedebergs Arch Pharmacol. 1994 May;349(5):546-8.

PMID:
7915008
26.

(1-Butyl-4-piperidinyl)methyl 8-amino-7-chloro-1,4-benzodioxane-5-carboxylate hydrochloride: a highly potent and selective 5-HT4 receptor antagonist derived from metoclopramide.

Gaster LM, Jennings AJ, Joiner GF, King FD, Mulholland KR, Rahman SK, Starr S, Wyman PA, Wardle KA, Ellis ES, et al.

J Med Chem. 1993 Dec 10;36(25):4121-3. No abstract available.

PMID:
8258837
27.

Synthesis of novel modified dipeptide inhibitors of human collagenase: beta-mercapto carboxylic acid derivatives.

Beszant B, Bird J, Gaster LM, Harper GP, Hughes I, Karran EH, Markwell RE, Miles-Williams AJ, Smith SA.

J Med Chem. 1993 Dec 10;36(25):4030-9.

PMID:
8258825
28.

(+/-) 3-Amino-6-carboxamido-1,2,3,4-tetrahydrocarbazole: a conformationally restricted analogue of 5-carboxamidotryptamine with selectivity for the serotonin 5-HT1D receptor.

King FD, Brown AM, Gaster LM, Kaumann AJ, Medhurst AD, Parker SG, Parsons AA, Patch TL, Raval P.

J Med Chem. 1993 Jun 25;36(13):1918-9. No abstract available. Erratum in: J Med Chem 1993 Oct 15;36(21):3218.

PMID:
8515429
29.

The dream ... an accessible America. Challenge for the clinician.

Gaster LS.

ASHA. 1992 Jun-Jul;34(6-7):42-3. No abstract available.

PMID:
1456979
30.

Substituted 3-amino-1,1-diaryl-2-propanols as potential antidepressant agents.

Clark JA, Clark MS, Gardner DV, Gaster LM, Hadley MS, Miller D, Shah A.

J Med Chem. 1979 Nov;22(11):1373-9.

PMID:
533885
31.

4-(6-Methoxy-2-naphthyl)butan-2-one and related analogues, a novel structural class of antiinflammatory compounds.

Goudie AC, Gaster LM, Lake AW, Rose CJ, Freeman PC, Hughes BO, Miller D.

J Med Chem. 1978 Dec;21(12):1260-4.

PMID:
722734

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