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Items: 1 to 50 of 104

1.

Chemical genomics: massively parallel technologies for rapid lead identification and target validation.

Hacksell U, Nash N, Burstein ES, Piu F, Croston G, Brann MR.

Cytotechnology. 2002 Jan;38(1-3):3-10. doi: 10.1023/A:1021169023731.

2.

Identification of novel selective V2 receptor non-peptide agonists.

Del Tredici AL, Vanover KE, Knapp AE, Bertozzi SM, Nash NR, Burstein ES, Lameh J, Currier EA, Davis RE, Brann MR, Mohell N, Olsson R, Piu F.

Biochem Pharmacol. 2008 Oct 30;76(9):1134-41. doi: 10.1016/j.bcp.2008.08.004. Epub 2008 Aug 12.

PMID:
18761325
3.

Differential modulation of inflammatory pain by a selective estrogen receptor beta agonist.

Gardell LR, Hyldtoft L, Del Tredici AL, Andersen CB, Fairbairn LC, Lund BW, Gustafsson M, Brann MR, Olsson R, Piu F.

Eur J Pharmacol. 2008 Sep 11;592(1-3):158-9. doi: 10.1016/j.ejphar.2008.06.107. Epub 2008 Jul 4.

PMID:
18644363
4.

Broad modulation of neuropathic pain states by a selective estrogen receptor beta agonist.

Piu F, Cheevers C, Hyldtoft L, Gardell LR, Del Tredici AL, Andersen CB, Fairbairn LC, Lund BW, Gustafsson M, Schiffer HH, Donello JE, Olsson R, Gil DW, Brann MR.

Eur J Pharmacol. 2008 Aug 20;590(1-3):423-9. doi: 10.1016/j.ejphar.2008.05.015. Epub 2008 May 23.

PMID:
18559275
5.

Constitutively active mutants of the histamine H1 receptor suggest a conserved hydrophobic asparagine-cage that constrains the activation of class A G protein-coupled receptors.

Bakker RA, Jongejan A, Sansuk K, Hacksell U, Timmerman H, Brann MR, Weiner DM, Pardo L, Leurs R.

Mol Pharmacol. 2008 Jan;73(1):94-103. Epub 2007 Oct 24.

6.

Monitoring interactions between receptor tyrosine kinases and their downstream effector proteins in living cells using bioluminescence resonance energy transfer.

Tan PK, Wang J, Littler PL, Wong KK, Sweetnam TA, Keefe W, Nash NR, Reding EC, Piu F, Brann MR, Schiffer HH.

Mol Pharmacol. 2007 Dec;72(6):1440-6. Epub 2007 Aug 22.

7.

PET analysis of the 5-HT2A receptor inverse agonist ACP-103 in human brain.

Nordstrom AL, Mansson M, Jovanovic H, Karlsson P, Halldin C, Farde L, Vanover KE, Hacksell U, Brann MR, Davis RE, Weiner DM.

Int J Neuropsychopharmacol. 2008 Mar;11(2):163-71. Epub 2007 Aug 21.

PMID:
17708779
8.

ACP-103, a 5-hydroxytryptamine 2A receptor inverse agonist, improves the antipsychotic efficacy and side-effect profile of haloperidol and risperidone in experimental models.

Gardell LR, Vanover KE, Pounds L, Johnson RW, Barido R, Anderson GT, Veinbergs I, Dyssegaard A, Brunmark P, Tabatabaei A, Davis RE, Brann MR, Hacksell U, Bonhaus DW.

J Pharmacol Exp Ther. 2007 Aug;322(2):862-70. Epub 2007 May 22.

9.

Identification of the atypical L-type Ca2+ channel blocker diltiazem and its metabolites as ghrelin receptor agonists.

Ma JN, Schiffer HH, Knapp AE, Wang J, Wong KK, Currier EA, Owens M, Nash NR, Gardell LR, Brann MR, Olsson R, Burstein ES.

Mol Pharmacol. 2007 Aug;72(2):380-6. Epub 2007 May 2.

10.

In vitro pharmacology of clinically used central nervous system-active drugs as inverse H(1) receptor agonists.

Bakker RA, Nicholas MW, Smith TT, Burstein ES, Hacksell U, Timmerman H, Leurs R, Brann MR, Weiner DM.

J Pharmacol Exp Ther. 2007 Jul;322(1):172-9. Epub 2007 Apr 2.

11.

Pharmacology and signaling properties of epidermal growth factor receptor isoforms studied by bioluminescence resonance energy transfer.

Schiffer HH, Reding EC, Fuhs SR, Lu Q, Piu F, Wong S, Littler PL, Weiner DM, Keefe W, Tan PK, Nash NR, Knapp AE, Olsson R, Brann MR.

Mol Pharmacol. 2007 Feb;71(2):508-18. Epub 2006 Sep 12.

12.

Structural requirements of transmembrane domain 3 for activation by the M1 muscarinic receptor agonists AC-42, AC-260584, clozapine, and N-desmethylclozapine: evidence for three distinct modes of receptor activation.

Spalding TA, Ma JN, Ott TR, Friberg M, Bajpai A, Bradley SR, Davis RE, Brann MR, Burstein ES.

Mol Pharmacol. 2006 Dec;70(6):1974-83. Epub 2006 Sep 7.

13.

Integrative functional assays, chemical genomics and high throughput screening: harnessing signal transduction pathways to a common HTS readout.

Burstein ES, Piu F, Ma JN, Weissman JT, Currier EA, Nash NR, Weiner DM, Spalding TA, Schiffer HH, Del Tredici AL, Brann MR.

Curr Pharm Des. 2006;12(14):1717-29.

PMID:
16712484
14.

Pharmacological and behavioral profile of N-(4-fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl) carbamide (2R,3R)-dihydroxybutanedioate (2:1) (ACP-103), a novel 5-hydroxytryptamine(2A) receptor inverse agonist.

Vanover KE, Weiner DM, Makhay M, Veinbergs I, Gardell LR, Lameh J, Del Tredici AL, Piu F, Schiffer HH, Ott TR, Burstein ES, Uldam AK, Thygesen MB, Schlienger N, Andersson CM, Son TY, Harvey SC, Powell SB, Geyer MA, Tolf BR, Brann MR, Davis RE.

J Pharmacol Exp Ther. 2006 May;317(2):910-8. Epub 2006 Feb 9.

15.

Identification of novel subtype selective RAR agonists.

Piu F, Gauthier NK, Olsson R, Currier EA, Lund BW, Croston GE, Hacksell U, Brann MR.

Biochem Pharmacol. 2005 Dec 19;71(1-2):156-62. Epub 2005 Nov 21.

PMID:
16303118
16.

Discovery of a potent, orally available, and isoform-selective retinoic acid beta2 receptor agonist.

Lund BW, Piu F, Gauthier NK, Eeg A, Currier E, Sherbukhin V, Brann MR, Hacksell U, Olsson R.

J Med Chem. 2005 Dec 1;48(24):7517-9.

PMID:
16302793
17.

Characterization of the Mas-related gene family: structural and functional conservation of human and rhesus MrgX receptors.

Burstein ES, Ott TR, Feddock M, Ma JN, Fuhs S, Wong S, Schiffer HH, Brann MR, Nash NR.

Br J Pharmacol. 2006 Jan;147(1):73-82.

18.

Intrinsic efficacy of antipsychotics at human D2, D3, and D4 dopamine receptors: identification of the clozapine metabolite N-desmethylclozapine as a D2/D3 partial agonist.

Burstein ES, Ma J, Wong S, Gao Y, Pham E, Knapp AE, Nash NR, Olsson R, Davis RE, Hacksell U, Weiner DM, Brann MR.

J Pharmacol Exp Ther. 2005 Dec;315(3):1278-87. Epub 2005 Aug 31.

19.

The role of M1 muscarinic receptor agonism of N-desmethylclozapine in the unique clinical effects of clozapine.

Weiner DM, Meltzer HY, Veinbergs I, Donohue EM, Spalding TA, Smith TT, Mohell N, Harvey SC, Lameh J, Nash N, Vanover KE, Olsson R, Jayathilake K, Lee M, Levey AI, Hacksell U, Burstein ES, Davis RE, Brann MR.

Psychopharmacology (Berl). 2004 Dec;177(1-2):207-16. Epub 2004 Jul 16.

PMID:
15258717
20.

Pharmacological characterization of AC-90179 [2-(4-methoxyphenyl)-N-(4-methyl-benzyl)-N-(1-methyl-piperidin-4-yl)-acetamide hydrochloride]: a selective serotonin 2A receptor inverse agonist.

Vanover KE, Harvey SC, Son T, Bradley SR, Kold H, Makhay M, Veinbergs I, Spalding TA, Weiner DM, Andersson CM, Tolf BR, Brann MR, Hacksell U, Davis RE.

J Pharmacol Exp Ther. 2004 Sep;310(3):943-51. Epub 2004 Apr 21.

21.

Functional screening of drug target genes: m1 muscarinic acetylcholine receptor phenotypes in degenerative dementias.

Weiner DM, Goodman MW, Colpitts TM, Feddock MA, Duggento KL, Nash NR, Levey AI, Brann MR.

Am J Pharmacogenomics. 2004;4(2):119-28.

PMID:
15059034
22.

Pharmacology of polymorphic variants of the human 5-HT1A receptor.

Del Tredici AL, Schiffer HH, Burstein ES, Lameh J, Mohell N, Hacksell U, Brann MR, Weiner DM.

Biochem Pharmacol. 2004 Feb 1;67(3):479-90.

PMID:
15037200
23.

Discovery of novel peptide/receptor interactions: identification of PHM-27 as a potent agonist of the human calcitonin receptor.

Ma JN, Currier EA, Essex A, Feddock M, Spalding TA, Nash NR, Brann MR, Burstein ES.

Biochem Pharmacol. 2004 Apr 1;67(7):1279-84.

PMID:
15013843
24.

Loss-of-function polymorphic variants of the human angiotensin II type 1 receptor.

Hansen JL, Haunsø S, Brann MR, Sheikh SP, Weiner DM.

Mol Pharmacol. 2004 Mar;65(3):770-7.

25.

8R-lisuride is a potent stereospecific histamine H1-receptor partial agonist.

Bakker RA, Weiner DM, ter Laak T, Beuming T, Zuiderveld OP, Edelbroek M, Hacksell U, Timmerman H, Brann MR, Leurs R.

Mol Pharmacol. 2004 Mar;65(3):538-49. Erratum in: Mol Pharmacol. 2004 Apr;65(4):1048.

26.

Psychosis of Parkinson's disease: serotonin 2A receptor inverse agonists as potential therapeutics.

Weiner DM, Vanover KE, Brann MR, Meltzer HY, Davis RE.

Curr Opin Investig Drugs. 2003 Jul;4(7):815-9. Review.

PMID:
14619402
27.

Distribution analysis of nonsynonymous polymorphisms within the G-protein-coupled receptor gene family.

Lee A, Rana BK, Schiffer HH, Schork NJ, Brann MR, Insel PA, Weiner DM.

Genomics. 2003 Mar;81(3):245-8.

PMID:
12659808
28.

Discovery of the first nonpeptide agonist of the GPR14/urotensin-II receptor: 3-(4-chlorophenyl)-3-(2- (dimethylamino)ethyl)isochroman-1-one (AC-7954).

Croston GE, Olsson R, Currier EA, Burstein ES, Weiner D, Nash N, Severance D, Allenmark SG, Thunberg L, Ma JN, Mohell N, O'Dowd B, Brann MR, Hacksell U.

J Med Chem. 2002 Nov 7;45(23):4950-3.

PMID:
12408704
29.

Molecular cloning and pharmacology of functionally distinct isoforms of the human histamine H(3) receptor.

Wellendorph P, Goodman MW, Burstein ES, Nash NR, Brann MR, Weiner DM.

Neuropharmacology. 2002 Jun;42(7):929-40.

PMID:
12069903
30.

Discovery of an ectopic activation site on the M(1) muscarinic receptor.

Spalding TA, Trotter C, Skjaerbaek N, Messier TL, Currier EA, Burstein ES, Li D, Hacksell U, Brann MR.

Mol Pharmacol. 2002 Jun;61(6):1297-302.

31.

5-hydroxytryptamine2A receptor inverse agonists as antipsychotics.

Weiner DM, Burstein ES, Nash N, Croston GE, Currier EA, Vanover KE, Harvey SC, Donohue E, Hansen HC, Andersson CM, Spalding TA, Gibson DF, Krebs-Thomson K, Powell SB, Geyer MA, Hacksell U, Brann MR.

J Pharmacol Exp Ther. 2001 Oct;299(1):268-76.

32.

Functional importance of the Ala(116)-Pro(136) region in the calcium-sensing receptor. Constitutive activity and inverse agonism in a family C G-protein-coupled receptor.

Jensen AA, Spalding TA, Burstein ES, Sheppard PO, O'Hara PJ, Brann MR, Krogsgaard-Larsen P, Bräuner-Osborne H.

J Biol Chem. 2000 Sep 22;275(38):29547-55.

33.

The ras-related GTPase rac1 regulates a proliferative pathway selectively utilized by G-protein coupled receptors.

Burstein ES, Hesterberg DJ, Gutkind JS, Brann MR, Currier EA, Messier TL.

Oncogene. 1998 Sep 24;17(12):1617-23.

34.

The second intracellular loop of the m5 muscarinic receptor is the switch which enables G-protein coupling.

Burstein ES, Spalding TA, Brann MR.

J Biol Chem. 1998 Sep 18;273(38):24322-7.

35.

Identification of a ligand-dependent switch within a muscarinic receptor.

Spalding TA, Burstein ES, Henderson SC, Ducote KR, Brann MR.

J Biol Chem. 1998 Aug 21;273(34):21563-8.

36.

Design and synthesis of m1-selective muscarinic agonists: (R)-(-)-(Z)-1-Azabicyclo[2.2.1]heptan-3-one, O-(3-(3'-methoxyphenyl)-2-propynyl)oxime maleate (CI-1017), a functionally m1-selective muscarinic agonist.

Tecle H, Barrett SD, Lauffer DJ, Augelli-Szafran C, Brann MR, Callahan MJ, Caprathe BW, Davis RE, Doyle PD, Eubanks D, Lipiniski W, Mirzadegan T, Moos WH, Moreland DW, Nelson CB, Pavia MR, Raby C, Schwarz RD, Spencer CJ, Thomas AJ, Jaen JC.

J Med Chem. 1998 Jul 2;41(14):2524-36.

PMID:
9651157
37.
38.

Constitutive activation of the m5 muscarinic receptor by a series of mutations at the extracellular end of transmembrane 6.

Spalding TA, Burstein ES, Wells JW, Brann MR.

Biochemistry. 1997 Aug 19;36(33):10109-16.

PMID:
9254607
39.

Pharmacology of muscarinic receptor subtypes constitutively activated by G proteins.

Burstein ES, Spalding TA, Brann MR.

Mol Pharmacol. 1997 Feb;51(2):312-9.

40.

Interactions of muscarinic receptors with the heterotrimeric G proteins Gq and G12: transduction of proliferative signals.

Burstein ES, Bräuner-Osborne H, Spalding TA, Conklin BR, Brann MR.

J Neurochem. 1997 Feb;68(2):525-33.

41.

Use of random-saturation mutagenesis to study receptor-G protein coupling.

Burstein ES, Spalding TA, Brann MR.

Methods Mol Biol. 1997;83:143-57. Review. No abstract available.

PMID:
9210143
42.

Functional partial agonism at cloned human muscarinic acetylcholine receptors.

Bräuner-Osborne H, Ebert B, Brann MR, Falch E, Krogsgaard-Larsen P.

Eur J Pharmacol. 1996 Oct 10;313(1-2):145-50.

PMID:
8905341
43.

Dopamine D2 receptor dimers and receptor-blocking peptides.

Ng GY, O'Dowd BF, Lee SP, Chung HT, Brann MR, Seeman P, George SR.

Biochem Biophys Res Commun. 1996 Oct 3;227(1):200-4.

PMID:
8858125
44.

Constitutive activation of chimeric m2/m5 muscarinic receptors and delineation of G-protein coupling selectivity domains.

Burstein ES, Spalding TA, Brann MR.

Biochem Pharmacol. 1996 Feb 23;51(4):539-44.

PMID:
8619900
45.

Structure of a G-protein-coupling domain of a muscarinic receptor predicted by random saturation mutagenesis.

Hill-Eubanks D, Burstein ES, Spalding TA, Bräuner-Osborne H, Brann MR.

J Biol Chem. 1996 Feb 9;271(6):3058-65.

46.
47.

Pharmacology of muscarinic acetylcholine receptor subtypes (m1-m5): high throughput assays in mammalian cells.

Bräuner-Osborne H, Brann MR.

Eur J Pharmacol. 1996 Jan 4;295(1):93-102.

PMID:
8925880
48.

Pharmacology of a constitutively active muscarinic receptor generated by random mutagenesis.

Spalding TA, Burstein ES, Brauner-Osborne H, Hill-Eubanks D, Brann MR.

J Pharmacol Exp Ther. 1995 Dec;275(3):1274-9.

PMID:
8531092
49.

Annulated heterocyclic bioisosteres of norarecoline. Synthesis and molecular pharmacology at five recombinant human muscarinic acetylcholine receptors.

Bräuner-Osborne H, Ebert B, Brann MR, Falch E, Krogsgaard-Larsen P.

J Med Chem. 1995 Jun 9;38(12):2188-95.

PMID:
7783150
50.

High throughput assays of cloned adrenergic, muscarinic, neurokinin, and neurotrophin receptors in living mammalian cells.

Messier TL, Dorman CM, Braüner-Osborne H, Eubanks D, Brann MR.

Pharmacol Toxicol. 1995 May;76(5):308-11.

PMID:
7567780

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