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Items: 1 to 50 of 106

1.

Indazole derivatives as novel bradykinin B1 receptor antagonists.

Bodmer-Narkevitch V, Anthony NJ, Cofre V, Jolly SM, Murphy KL, Ransom RW, Reiss DR, Tang C, Prueksaritanont T, Pettibone DJ, Bock MG, Kuduk SD.

Bioorg Med Chem Lett. 2010 Dec 1;20(23):7011-4. doi: 10.1016/j.bmcl.2010.09.121. Epub 2010 Sep 29.

PMID:
20971001
2.

Discovery of GlyT1 inhibitors with improved pharmacokinetic properties.

Wolkenberg SE, Zhao Z, Wisnoski DD, Leister WH, O'Brien J, Lemaire W, Williams DL Jr, Jacobson MA, Sur C, Kinney GG, Pettibone DJ, Tiller PR, Smith S, Gibson C, Ma BK, Polsky-Fisher SL, Lindsley CW, Hartman GD.

Bioorg Med Chem Lett. 2009 Mar 1;19(5):1492-5. doi: 10.1016/j.bmcl.2009.01.015. Epub 2009 Jan 10.

PMID:
19181525
3.

Discovery of N-{[1-(propylsulfonyl)-4-pyridin-2-ylpiperidin-4-yl]methyl}benzamides as novel, selective and potent GlyT1 inhibitors.

Zhao Z, Leister WH, O'Brien JA, Lemaire W, Williams DL Jr, Jacobson MA, Sur C, Kinney GG, Pettibone DJ, Tiller PR, Smith S, Hartman GD, Lindsley CW, Wolkenberg SE.

Bioorg Med Chem Lett. 2009 Mar 1;19(5):1488-91. doi: 10.1016/j.bmcl.2008.12.115. Epub 2009 Jan 9.

PMID:
19179073
4.

Bradykinin B1 receptor antagonists: an alpha-hydroxy amide with an improved metabolism profile.

Kuduk SD, Chang RK, Dipardo RM, Di Marco CN, Murphy KL, Ransom RW, Reiss DR, Tang C, Prueksaritanont T, Pettibone DJ, Bock MG.

Bioorg Med Chem Lett. 2008 Sep 15;18(18):5107-10. doi: 10.1016/j.bmcl.2008.07.126. Epub 2008 Aug 5.

PMID:
18722115
5.

2-Aminobenzophenones as a novel class of bradykinin B1 receptor antagonists.

Su DS, Lim JL, Tinney E, Wan BL, Murphy KL, Reiss DR, Harrell CM, O'Malley SS, Ransom RW, Chang RS, Pettibone DJ, Yu J, Tang C, Prueksaritanont T, Freidinger RM, Bock MG, Anthony NJ.

J Med Chem. 2008 Jul 10;51(13):3946-52. doi: 10.1021/jm800199h. Epub 2008 Jun 14.

PMID:
18553956
6.

A new class of bradykinin B1 receptor antagonists with high oral bioavailability and minimal PXR activity.

Feng DM, DiPardo RM, Wai JM, Chang RK, Di Marco CN, Murphy KL, Ransom RW, Reiss DR, Tang C, Prueksaritanont T, Pettibone DJ, Bock MG, Kuduk SD.

Bioorg Med Chem Lett. 2008 Jan 15;18(2):682-7.

PMID:
18240388
7.

Proline bis-amides as potent dual orexin receptor antagonists.

Bergman JM, Roecker AJ, Mercer SP, Bednar RA, Reiss DR, Ransom RW, Meacham Harrell C, Pettibone DJ, Lemaire W, Murphy KL, Li C, Prueksaritanont T, Winrow CJ, Renger JJ, Koblan KS, Hartman GD, Coleman PJ.

Bioorg Med Chem Lett. 2008 Feb 15;18(4):1425-30. doi: 10.1016/j.bmcl.2008.01.001. Epub 2008 Jan 8.

PMID:
18207395
8.

Alpha-hydroxy amides as a novel class of bradykinin B1 selective antagonists.

Wood MR, Schirripa KM, Kim JJ, Kuduk SD, Chang RK, Di Marco CN, DiPardo RM, Wan BL, Murphy KL, Ransom RW, Chang RS, Holahan MA, Cook JJ, Lemaire W, Mosser SD, Bednar RA, Tang C, Prueksaritanont T, Wallace AA, Mei Q, Yu J, Bohn DL, Clayton FC, Adarayn ED, Sitko GR, Leonard YM, Freidinger RM, Pettibone DJ, Bock MG.

Bioorg Med Chem Lett. 2008 Jan 15;18(2):716-20. Epub 2007 Nov 19.

PMID:
18061443
9.

Bradykinin B1 antagonists: biphenyl SAR studies in the cyclopropanecarboxamide series.

Kuduk SD, DiPardo RM, Chang RK, Di Marco CN, Murphy KL, Ransom RW, Reiss DR, Tang C, Prueksaritanont T, Pettibone DJ, Bock MG.

Bioorg Med Chem Lett. 2007 Jul 1;17(13):3608-12. Epub 2007 Apr 24.

PMID:
17482459
10.

Potent bradykinin B1 receptor antagonists: 4-substituted phenyl cyclohexanes.

Su DS, Lim JL, Markowitz MK, Wan BL, Murphy KL, Reiss DR, Harrell CM, O'Malley SS, Ransom RW, Chang RS, Pettibone DJ, Tang C, Prueksaritanont T, Freidinger RM, Bock MG.

Bioorg Med Chem Lett. 2007 Jun 1;17(11):3006-9. Epub 2007 Mar 21.

PMID:
17428657
11.

Development of orally bioavailable and CNS penetrant biphenylaminocyclopropane carboxamide bradykinin B1 receptor antagonists.

Kuduk SD, Di Marco CN, Chang RK, Wood MR, Schirripa KM, Kim JJ, Wai JM, DiPardo RM, Murphy KL, Ransom RW, Harrell CM, Reiss DR, Holahan MA, Cook J, Hess JF, Sain N, Urban MO, Tang C, Prueksaritanont T, Pettibone DJ, Bock MG.

J Med Chem. 2007 Jan 25;50(2):272-82.

PMID:
17228869
12.

Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA.

Zhao Z, Wisnoski DD, O'Brien JA, Lemaire W, Williams DL Jr, Jacobson MA, Wittman M, Ha SN, Schaffhauser H, Sur C, Pettibone DJ, Duggan ME, Conn PJ, Hartman GD, Lindsley CW.

Bioorg Med Chem Lett. 2007 Mar 1;17(5):1386-91. Epub 2006 Dec 3.

PMID:
17210250
13.

Synthesis and SAR of GlyT1 inhibitors derived from a series of N-((4-(morpholine-4-carbonyl)-1-(propylsulfonyl)piperidin-4-yl)methyl)benzamides.

Zhao Z, O'Brien JA, Lemaire W, Williams DL Jr, Jacobson MA, Sur C, Pettibone DJ, Tiller PR, Smith S, Hartman GD, Wolkenberg SE, Lindsley CW.

Bioorg Med Chem Lett. 2006 Dec 1;16(23):5968-72. Epub 2006 Sep 20.

PMID:
16987662
14.

Design, synthesis, and in vivo efficacy of glycine transporter-1 (GlyT1) inhibitors derived from a series of [4-phenyl-1-(propylsulfonyl)piperidin-4-yl]methyl benzamides.

Lindsley CW, Zhao Z, Leister WH, O'Brien J, Lemaire W, Williams DL Jr, Chen TB, Chang RS, Burno M, Jacobson MA, Sur C, Kinney GG, Pettibone DJ, Tiller PR, Smith S, Tsou NN, Duggan ME, Conn PJ, Hartman GD.

ChemMedChem. 2006 Aug;1(8):807-11. No abstract available.

PMID:
16902933
15.

5-Piperazinyl pyridine carboxamide bradykinin B1 antagonists.

Kuduk SD, Di Marco CN, Chang RK, Wood MR, Kim JJ, Schirripa KM, Murphy KL, Ransom RW, Tang C, Torrent M, Ha S, Prueksaritanont T, Pettibone DJ, Bock MG.

Bioorg Med Chem Lett. 2006 May 15;16(10):2791-5. Epub 2006 Mar 10.

PMID:
16529929
16.

Generation and characterization of a humanized bradykinin B1 receptor mouse.

Hess JF, Chen RZ, Hey P, Breese R, Chang RS, Chen TB, Bock MG, Vogt T, Pettibone DJ.

Biol Chem. 2006 Feb;387(2):195-201.

PMID:
16497152
17.

Cyclopropylamino acid amide as a pharmacophoric replacement for 2,3-diaminopyridine. Application to the design of novel bradykinin B1 receptor antagonists.

Wood MR, Schirripa KM, Kim JJ, Wan BL, Murphy KL, Ransom RW, Chang RS, Tang C, Prueksaritanont T, Detwiler TJ, Hettrick LA, Landis ER, Leonard YM, Krueger JA, Lewis SD, Pettibone DJ, Freidinger RM, Bock MG.

J Med Chem. 2006 Feb 23;49(4):1231-4.

PMID:
16480259
18.

Inhibition of acute nociceptive responses in rat spinal cord by a bradykinin B1 receptor antagonist.

Conley RK, Wheeldon A, Webb JK, DiPardo RM, Homnick CF, Bock MG, Chen TB, Chang RS, Pettibone DJ, Boyce S.

Eur J Pharmacol. 2005 Dec 19;527(1-3):44-51. Epub 2005 Nov 28.

PMID:
16310181
19.

Bradykinin B1 antagonists: SAR studies in the 2,3-diaminopyridine series.

Kuduk SD, Chang RK, Ng C, Murphy KL, Ransom RW, Tang C, Prueksaritanont T, Freidinger RM, Pettibone DJ, Bock MG.

Bioorg Med Chem Lett. 2005 Sep 1;15(17):3925-9.

PMID:
15993596
20.

2,3-Diaminopyridine as a platform for designing structurally unique nonpeptide bradykinin B1 receptor antagonists.

Feng DM, Wai JM, Kuduk SD, Ng C, Murphy KL, Ransom RW, Reiss D, Chang RS, Harrell CM, MacNeil T, Tang C, Prueksaritanont T, Freidinger RM, Pettibone DJ, Bock MG.

Bioorg Med Chem Lett. 2005 May 2;15(9):2385-8.

PMID:
15837330
21.

International union of pharmacology. XLV. Classification of the kinin receptor family: from molecular mechanisms to pathophysiological consequences.

Leeb-Lundberg LM, Marceau F, Müller-Esterl W, Pettibone DJ, Zuraw BL.

Pharmacol Rev. 2005 Mar;57(1):27-77. Review.

PMID:
15734727
22.
23.

A novel selective positive allosteric modulator of metabotropic glutamate receptor subtype 5 has in vivo activity and antipsychotic-like effects in rat behavioral models.

Kinney GG, O'Brien JA, Lemaire W, Burno M, Bickel DJ, Clements MK, Chen TB, Wisnoski DD, Lindsley CW, Tiller PR, Smith S, Jacobson MA, Sur C, Duggan ME, Pettibone DJ, Conn PJ, Williams DL Jr.

J Pharmacol Exp Ther. 2005 Apr;313(1):199-206. Epub 2004 Dec 17.

PMID:
15608073
24.

2,3-diaminopyridine bradykinin B1 receptor antagonists.

Kuduk SD, Ng C, Feng DM, Wai JM, Chang RS, Harrell CM, Murphy KL, Ransom RW, Reiss D, Ivarsson M, Mason G, Boyce S, Tang C, Prueksaritanont T, Freidinger RM, Pettibone DJ, Bock MG.

J Med Chem. 2004 Dec 16;47(26):6439-42.

PMID:
15588075
25.

Development of an efficient and selective radioligand for bradykinin B1 receptor occupancy studies.

Su DS, Markowitz MK, Murphy KL, Wan BL, Zrada MM, Harrell CM, O'Malley SS, Hess JF, Ransom RW, Chang RS, Wallace MA, Raab CE, Dean DC, Pettibone DJ, Freidinger RM, Bock MG.

Bioorg Med Chem Lett. 2004 Dec 20;14(24):6045-8.

PMID:
15546726
26.

Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo.

Lindsley CW, Wisnoski DD, Leister WH, O'brien JA, Lemaire W, Williams DL Jr, Burno M, Sur C, Kinney GG, Pettibone DJ, Tiller PR, Smith S, Duggan ME, Hartman GD, Conn PJ, Huff JR.

J Med Chem. 2004 Nov 18;47(24):5825-8.

PMID:
15537338
27.

Effects of typical and atypical antipsychotics on human glycine transporters.

Williams JB, Mallorga PJ, Conn PJ, Pettibone DJ, Sur C.

Schizophr Res. 2004 Nov 1;71(1):103-12.

PMID:
15374578
28.

Pharmacological characterization and radioligand binding properties of a high-affinity, nonpeptide, bradykinin B1 receptor antagonist.

Ransom RW, Harrell CM, Reiss DR, Murphy KL, Chang RS, Hess JF, Miller PJ, O'Malley SS, Hey PJ, Kunapuli P, Su DS, Markowitz MK, Wallace MA, Raab CE, Jones AN, Dean DC, Pettibone DJ, Freidinger RM, Bock MG.

Eur J Pharmacol. 2004 Sep 19;499(1-2):77-84.

PMID:
15363953
29.

Generation and characterization of a human bradykinin receptor B1 transgenic rat as a pharmacodynamic model.

Hess JF, Ransom RW, Zeng Z, Chang RS, Hey PJ, Warren L, Harrell CM, Murphy KL, Chen TB, Miller PJ, Lis E, Reiss D, Gibson RE, Markowitz MK, DiPardo RM, Su DS, Bock MG, Gould RJ, Pettibone DJ.

J Pharmacol Exp Ther. 2004 Aug;310(2):488-97. Epub 2004 Mar 29.

PMID:
15051800
30.

A novel selective allosteric modulator potentiates the activity of native metabotropic glutamate receptor subtype 5 in rat forebrain.

O'Brien JA, Lemaire W, Wittmann M, Jacobson MA, Ha SN, Wisnoski DD, Lindsley CW, Schaffhauser HJ, Rowe B, Sur C, Duggan ME, Pettibone DJ, Conn PJ, Williams DL Jr.

J Pharmacol Exp Ther. 2004 May;309(2):568-77. Epub 2004 Jan 27.

PMID:
14747613
31.

Difference in mGluR5 interaction between positive allosteric modulators from two structural classes.

Williams DL Jr, O'Brien JA, Lemaire W, Chen TB, Chang RS, Jacobson MA, Ha SN, Wisnoski DD, Lindsley CW, Sur C, Duggan ME, Pettibone DJ, Conn PJ.

Ann N Y Acad Sci. 2003 Nov;1003:481-4. No abstract available.

PMID:
14684495
32.

N-desmethylclozapine, an allosteric agonist at muscarinic 1 receptor, potentiates N-methyl-D-aspartate receptor activity.

Sur C, Mallorga PJ, Wittmann M, Jacobson MA, Pascarella D, Williams JB, Brandish PE, Pettibone DJ, Scolnick EM, Conn PJ.

Proc Natl Acad Sci U S A. 2003 Nov 11;100(23):13674-9. Epub 2003 Oct 31.

33.

Attenuation of PGF2alpha release in ewes infused with the oxytocin antagonist L-368,899.

Mann GE, Lamming GE, Scholey D, Hunter M, Pettibone DJ.

Domest Anim Endocrinol. 2003 Oct;25(3):255-62.

PMID:
14550509
34.

Development of a scintillation proximity assay for analysis of Na+/Cl- -dependent neurotransmitter transporter activity.

Williams JB, Mallorga PJ, Lemaire W, Williams DL, Na S, Patel S, Conn PJ, Pettibone DJ, Austin C, Sur C.

Anal Biochem. 2003 Oct 1;321(1):31-7. Erratum in: Anal Biochem. 2012 Oct 1;429(1):18. Conn, Jeffrey P [corrected to Conn, P Jeffrey].

PMID:
12963052
35.

Pharmacology and expression analysis of glycine transporter GlyT1 with [3H]-(N-[3-(4'-fluorophenyl)-3-(4'phenylphenoxy)propyl])sarcosine.

Mallorga PJ, Williams JB, Jacobson M, Marques R, Chaudhary A, Conn PJ, Pettibone DJ, Sur C.

Neuropharmacology. 2003 Oct;45(5):585-93.

PMID:
12941372
36.

A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5.

O'Brien JA, Lemaire W, Chen TB, Chang RS, Jacobson MA, Ha SN, Lindsley CW, Schaffhauser HJ, Sur C, Pettibone DJ, Conn PJ, Williams DL Jr.

Mol Pharmacol. 2003 Sep;64(3):731-40.

PMID:
12920211
37.

Discovery of a potent, non-peptide bradykinin B1 receptor antagonist.

Su DS, Markowitz MK, DiPardo RM, Murphy KL, Harrell CM, O'Malley SS, Ransom RW, Chang RS, Ha S, Hess FJ, Pettibone DJ, Mason GS, Boyce S, Freidinger RM, Bock MG.

J Am Chem Soc. 2003 Jun 25;125(25):7516-7.

PMID:
12812482
38.

Benzodiazepines as potent and selective bradykinin B1 antagonists.

Wood MR, Kim JJ, Han W, Dorsey BD, Homnick CF, DiPardo RM, Kuduk SD, MacNeil T, Murphy KL, Lis EV, Ransom RW, Stump GL, Lynch JJ, O'Malley SS, Miller PJ, Chen TB, Harrell CM, Chang RS, Sandhu P, Ellis JD, Bondiskey PJ, Pettibone DJ, Freidinger RM, Bock MG.

J Med Chem. 2003 May 8;46(10):1803-6.

PMID:
12723943
39.

Molecular and pharmacological diversity of the kinin B1 receptor.

Hess JF, Hey PJ, Chen TB, Pettibone DJ, Chang RS.

Int Immunopharmacol. 2002 Dec;2(13-14):1747-54.

PMID:
12489788
40.

A nonpeptide oxytocin receptor antagonist radioligand highly selective for human receptors.

Lemaire W, O'Brien JA, Burno M, Chaudhary AG, Dean DC, Williams PD, Freidinger RM, Pettibone DJ, Williams DL Jr.

Eur J Pharmacol. 2002 Aug 16;450(1):19-28.

PMID:
12176104
41.

The effects of deleting the mouse neurotensin receptor NTR1 on central and peripheral responses to neurotensin.

Pettibone DJ, Hess JF, Hey PJ, Jacobson MA, Leviten M, Lis EV, Mallorga PJ, Pascarella DM, Snyder MA, Williams JB, Zeng Z.

J Pharmacol Exp Ther. 2002 Jan;300(1):305-13.

PMID:
11752130
42.

Molecular cloning and pharmacological characterization of the canine B1 and B2 bradykinin receptors.

Hess JF, Hey PJ, Chen TB, O'Brien J, Omalley SS, Pettibone DJ, Chang RS.

Biol Chem. 2001 Jan;382(1):123-9.

PMID:
11258662
43.

In vitro studies on L-771,688 (SNAP 6383), a new potent and selective alpha1A-adrenoceptor antagonist.

Chang RS, Chen TB, O'Malley SS, Pettibone DJ, DiSalvo J, Francis B, Bock MG, Freidinger R, Nagarathnam D, Miao SW, Shen Q, Lagu B, Murali Dhar TG, Tyagarajan S, Marzabadi MR, Wong WC, Gluchowski C, Forray C.

Eur J Pharmacol. 2000 Dec 15;409(3):301-12.

PMID:
11108825
44.

De novo design of a novel oxazolidinone analogue as a potent and selective alpha1A adrenergic receptor antagonist with high oral bioavailability.

Lagu B, Tian D, Jeon Y, Li C, Wetzel JM, Nagarathnam D, Shen Q, Forray C, Chang RS, Broten TP, Ransom RW, Chan TB, O'Malley SS, Schorn TW, Rodrigues AD, Kassahun K, Pettibone DJ, Freidinger RO, Gluchowski C.

J Med Chem. 2000 Jul 27;43(15):2775-8. No abstract available.

PMID:
10956183
45.

Selective alpha1a adrenergic receptor antagonists based on 4-aryl-3,4-dihydropyridine-2-ones.

Nantermet PG, Barrow JC, Selnick HG, Homnick CF, Freidinger RM, Chang RS, O'Malley SS, Reiss DR, Broten TP, Ransom RW, Pettibone DJ, Olah T, Forray C.

Bioorg Med Chem Lett. 2000 Aug 7;10(15):1625-8.

PMID:
10937710
46.

Nonpeptide oxytocin antagonists: analogs of L-371,257 with improved potency.

Williams PD, Bock MG, Evans BE, Freidinger RM, Gallicchio SN, Guidotti MT, Jacobson MA, Kuo MS, Levy MR, Lis EV, Michelson SR, Pawluczyk JM, Perlow DS, Pettibone DJ, Quigley AG, Reiss DR, Salvatore C, Stauffer KJ, Woyden CJ.

Bioorg Med Chem Lett. 1999 May 3;9(9):1311-6.

PMID:
10340620
47.

Progress in the development of oxytocin antagonists for use in preterm labor.

Williams PD, Bock MG, Evans BE, Freidinger RM, Pettibone DJ.

Adv Exp Med Biol. 1998;449:473-9.

PMID:
10026841
48.

Nonpeptide oxytocin antagonists: potent, orally bioavailable analogs of L-371,257 containing a 1-R-(pyridyl)ethyl ether terminus.

Kuo MS, Bock MG, Freidinger RM, Guidotti MT, Lis EV, Pawluczyk JM, Perlow DS, Pettibone DJ, Quigley AG, Reiss DR, Williams PD, Woyden CJ.

Bioorg Med Chem Lett. 1998 Nov 3;8(21):3081-6.

PMID:
9873680
49.

Development of orally active oxytocin antagonists: studies on 1-(1-[4-[1-(2-methyl-1-oxidopyridin-3-ylmethyl)piperidin-4-yloxy]-2- methoxybenzoyl]piperidin-4-yl)-1,4-dihydrobenz[d][1,3]oxazin-2-one (L-372,662) and related pyridines.

Bell IM, Erb JM, Freidinger RM, Gallicchio SN, Guare JP, Guidotti MT, Halpin RA, Hobbs DW, Homnick CF, Kuo MS, Lis EV, Mathre DJ, Michelson SR, Pawluczyk JM, Pettibone DJ, Reiss DR, Vickers S, Williams PD, Woyden CJ.

J Med Chem. 1998 Jun 4;41(12):2146-63.

PMID:
9622556
50.

Cloning and expression of the rhesus monkey oxytocin receptor.

Salvatore CA, Woyden CJ, Guidotti MT, Pettibone DJ, Jacobson MA.

J Recept Signal Transduct Res. 1998 Jan;18(1):15-24.

PMID:
9493565

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