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Items: 33

1.

Design and synthesis of 4-heteroaryl 1,2,3,4-tetrahydroisoquinolines as triple reuptake inhibitors.

Liu S, Zha C, Nacro K, Hu M, Cui W, Yang YL, Bhatt U, Sambandam A, Isherwood M, Yet L, Herr MT, Ebeltoft S, Hassler C, Fleming L, Pechulis AD, Payen-Fornicola A, Holman N, Milanowski D, Cotterill I, Mozhaev V, Khmelnitsky Y, Guzzo PR, Sargent BJ, Molino BF, Olson R, King D, Lelas S, Li YW, Johnson K, Molski T, Orie A, Ng A, Haskell R, Clarke W, Bertekap R, O'Connell J, Lodge N, Sinz M, Adams S, Zaczek R, Macor JE.

ACS Med Chem Lett. 2014 May 13;5(7):760-5. doi: 10.1021/ml500053b. eCollection 2014 Jul 10.

2.

Monoamine reuptake site occupancy of sibutramine: Relationship to antidepressant-like and thermogenic effects in rats.

Li YW, Langdon S, Pieschl R, Strong T, Wright RN, Rohrbach K, Lelas S, Lodge NJ.

Eur J Pharmacol. 2014 Aug 15;737:47-56. doi: 10.1016/j.ejphar.2014.03.024. Epub 2014 May 10.

PMID:
24821570
3.

Discovery of a cyclopentylamine as an orally active dual NK1 receptor antagonist-serotonin reuptake transporter inhibitor.

Wu YJ, He H, Gao Q, Wu D, Bertekap R, Westphal RS, Lelas S, Newton A, Wallace T, Taber M, Davis C, Macor JE, Bronson J.

Bioorg Med Chem Lett. 2014 Mar 15;24(6):1611-4. doi: 10.1016/j.bmcl.2014.01.036. Epub 2014 Jan 27.

PMID:
24507922
4.

NK1 receptor antagonism lowers occupancy requirement for antidepressant-like effects of SSRIs in the gerbil forced swim test.

Lelas S, Li YW, Wallace-Boone TL, Taber MT, Newton AE, Pieschl RL, Davis CD, Molski TF, Newberry KS, Parker MF, Gillman KW, Bronson JJ, Macor JE, Lodge NJ.

Neuropharmacology. 2013 Oct;73:232-40. doi: 10.1016/j.neuropharm.2013.05.038. Epub 2013 Jun 12.

PMID:
23770339
5.

Discovery of disubstituted piperidines and homopiperidines as potent dual NK1 receptor antagonists-serotonin reuptake transporter inhibitors for the treatment of depression.

Wu YJ, He H, Bertekap R, Westphal R, Lelas S, Newton A, Wallace T, Taber M, Davis C, Macor JE, Bronson J.

Bioorg Med Chem. 2013 Apr 15;21(8):2217-2228. doi: 10.1016/j.bmc.2013.02.010. Epub 2013 Feb 19.

PMID:
23477943
6.

Design, optimization, and in vivo evaluation of a series of pyridine derivatives with dual NK1 antagonism and SERT inhibition for the treatment of depression.

Gillman KW, Parker MF, Silva M, Degnan AP, Tora GO, Lodge NJ, Li YW, Lelas S, Taber M, Krause RG, Bertekap RL, Newton AE, Pieschl RL, Lengyel KD, Johnson KA, Taylor SJ, Bronson JJ, Macor JE.

Bioorg Med Chem Lett. 2013 Jan 15;23(2):407-11. doi: 10.1016/j.bmcl.2012.11.094. Epub 2012 Nov 30.

PMID:
23253443
7.

Pharmacological and behavioral characterization of the novel CRF1 antagonist BMS-763534.

Lodge NJ, Lelas S, Li YW, Molski T, Grace J, Sivarao DV, Post-Munson D, Healy F, Bronson JJ, Hartz R, Macor JE, Zaczek R.

Neuropharmacology. 2013 Apr;67:284-93. doi: 10.1016/j.neuropharm.2012.10.025. Epub 2012 Nov 19.

PMID:
23174340
8.

A strategy to minimize reactive metabolite formation: discovery of (S)-4-(1-cyclopropyl-2-methoxyethyl)-6-[6-(difluoromethoxy)-2,5-dimethylpyridin-3-ylamino]-5-oxo-4,5-dihydropyrazine-2-carbonitrile as a potent, orally bioavailable corticotropin-releasing factor-1 receptor antagonist.

Hartz RA, Ahuja VT, Zhuo X, Mattson RJ, Denhart DJ, Deskus JA, Vrudhula VM, Pan S, Ditta JL, Shu YZ, Grace JE, Lentz KA, Lelas S, Li YW, Molski TF, Krishnananthan S, Wong H, Qian-Cutrone J, Schartman R, Denton R, Lodge NJ, Zaczek R, Macor JE, Bronson JJ.

J Med Chem. 2009 Dec 10;52(23):7653-68. doi: 10.1021/jm900716v.

PMID:
19954247
9.

Synthesis, structure-activity relationships, and in vivo evaluation of N3-phenylpyrazinones as novel corticotropin-releasing factor-1 (CRF1) receptor antagonists.

Hartz RA, Ahuja VT, Arvanitis AG, Rafalski M, Yue EW, Denhart DJ, Schmitz WD, Ditta JL, Deskus JA, Brenner AB, Hobbs FW, Payne J, Lelas S, Li YW, Molski TF, Mattson GK, Peng Y, Wong H, Grace JE, Lentz KA, Qian-Cutrone J, Zhuo X, Shu YZ, Lodge NJ, Zaczek R, Combs AP, Olson RE, Bronson JJ, Mattson RJ, Macor JE.

J Med Chem. 2009 Jul 23;52(14):4173-91. doi: 10.1021/jm900301y.

PMID:
19552437
10.

In vitro intrinsic clearance-based optimization of N3-phenylpyrazinones as corticotropin-releasing factor-1 (CRF1) receptor antagonists.

Hartz RA, Ahuja VT, Rafalski M, Schmitz WD, Brenner AB, Denhart DJ, Ditta JL, Deskus JA, Yue EW, Arvanitis AG, Lelas S, Li YW, Molski TF, Wong H, Grace JE, Lentz KA, Li J, Lodge NJ, Zaczek R, Combs AP, Olson RE, Mattson RJ, Bronson JJ, Macor JE.

J Med Chem. 2009 Jul 23;52(14):4161-72. doi: 10.1021/jm900302q. Erratum in: J Med Chem. 2009 Sep 24;52(18):5770.

PMID:
19552436
11.

8-(4-Methoxyphenyl)pyrazolo[1,5-a]-1,3,5-triazines: selective and centrally active corticotropin-releasing factor receptor-1 (CRF1) antagonists.

Gilligan PJ, He L, Clarke T, Tivitmahaisoon P, Lelas S, Li YW, Heman K, Fitzgerald L, Miller K, Zhang G, Marshall A, Krause C, McElroy J, Ward K, Shen H, Wong H, Grossman S, Nemeth G, Zaczek R, Arneric SP, Hartig P, Robertson DW, Trainor G.

J Med Chem. 2009 May 14;52(9):3073-83. doi: 10.1021/jm9000242.

PMID:
19361210
12.

Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.

Gilligan PJ, Clarke T, He L, Lelas S, Li YW, Heman K, Fitzgerald L, Miller K, Zhang G, Marshall A, Krause C, McElroy JF, Ward K, Zeller K, Wong H, Bai S, Saye J, Grossman S, Zaczek R, Arneric SP, Hartig P, Robertson D, Trainor G.

J Med Chem. 2009 May 14;52(9):3084-92. doi: 10.1021/jm900025h.

PMID:
19361209
13.
14.

Anti-conflict effects of benzodiazepines in rhesus monkeys: relationship with therapeutic doses in humans and role of GABAA receptors.

Rowlett JK, Lelas S, Tornatzky W, Licata SC.

Psychopharmacology (Berl). 2006 Jan;184(2):201-11. Epub 2005 Dec 24.

PMID:
16378217
15.

The pharmacology of DMP696 and DMP904, non-peptidergic CRF1 receptor antagonists.

Li YW, Fitzgerald L, Wong H, Lelas S, Zhang G, Lindner MD, Wallace T, McElroy J, Lodge NJ, Gilligan P, Zaczek R.

CNS Drug Rev. 2005 Spring;11(1):21-52. Review.

16.

Effects of CRF1 receptor antagonists and benzodiazepines in the Morris water maze and delayed non-matching to position tests.

Hogan JB, Hodges DB Jr, Lelas S, Gilligan PJ, McElroy JF, Lindner MD.

Psychopharmacology (Berl). 2005 Apr;178(4):410-9. Epub 2004 Oct 14.

PMID:
15765256
17.

Different GABAA receptor subtypes mediate the anxiolytic, abuse-related, and motor effects of benzodiazepine-like drugs in primates.

Rowlett JK, Platt DM, Lelas S, Atack JR, Dawson GR.

Proc Natl Acad Sci U S A. 2005 Jan 18;102(3):915-20. Epub 2005 Jan 11.

18.

Synthesis, structure-activity relationships, and in vivo properties of 3,4-dihydro-1H-pyrido[2,3-b]pyrazin-2-ones as corticotropin-releasing factor-1 receptor antagonists.

Dzierba CD, Takvorian AG, Rafalski M, Kasireddy-Polam P, Wong H, Molski TF, Zhang G, Li YW, Lelas S, Peng Y, McElroy JF, Zaczek RC, Taub RA, Combs AP, Gilligan PJ, Trainor GL.

J Med Chem. 2004 Nov 4;47(23):5783-90.

PMID:
15509177
19.

Anxiolytic-like effects of the corticotropin-releasing factor1 (CRF1) antagonist DMP904 [4-(3-pentylamino)-2,7-dimethyl-8-(2-methyl-4-methoxyphenyl)-pyrazolo-[1,5-a]-pyrimidine] administered acutely or chronically at doses occupying central CRF1 receptors in rats.

Lelas S, Wong H, Li YW, Heman KL, Ward KA, Zeller KL, Sieracki KK, Polino JL, Godonis HE, Ren SX, Yan XX, Arneric SP, Robertson DW, Hartig PR, Grossman S, Trainor GL, Taub RA, Zaczek R, Gilligan PJ, McElroy JF.

J Pharmacol Exp Ther. 2004 Apr;309(1):293-302. Epub 2004 Jan 23.

PMID:
14742750
20.

The anxiolytic CRF(1) antagonist DMP696 fails to function as a discriminative stimulus and does not substitute for chlordiazepoxide in rats.

Lelas S, Zeller KL, Ward KA, McElroy JF.

Psychopharmacology (Berl). 2003 Apr;166(4):408-15. Epub 2003 Feb 18.

PMID:
12590355
21.

The CRF(1) receptor antagonist DMP696 produces anxiolytic effects and inhibits the stress-induced hypothalamic-pituitary-adrenal axis activation without sedation or ataxia in rats.

McElroy JF, Ward KA, Zeller KL, Jones KW, Gilligan PJ, He L, Lelas S.

Psychopharmacology (Berl). 2002 Dec;165(1):86-92. Epub 2002 Oct 12.

PMID:
12474122
22.

Discriminative stimulus effects of zolpidem in squirrel monkeys: role of GABA(A)/alpha1 receptors.

Rowlett JK, Spealman RD, Lelas S, Cook JM, Yin W.

Psychopharmacology (Berl). 2003 Jan;165(3):209-15. Epub 2002 Nov 6.

PMID:
12420154
23.

Role of GABAA/benzodiazepine receptors containing alpha 1 and alpha 5 subunits in the discriminative stimulus effects of triazolam in squirrel monkeys.

Lelas S, Rowlett JK, Spealman RD, Cook JM, Ma C, Li X, Yin W.

Psychopharmacology (Berl). 2002 May;161(2):180-8. Epub 2002 Mar 13.

PMID:
11981598
24.

Isobolographic analysis of chlordiazepoxide and triazolam combinations in squirrel monkeys discriminating triazolam.

Lelas S, Rowlett JK, Spealman RD.

Psychopharmacology (Berl). 2001 Nov;158(2):181-9.

PMID:
11702092
25.
26.

Transduction of the discriminative stimulus effects of zolpidem by GABA(A)/alpha1 receptors.

Rowlett JK, Lelas S, Spealman RD.

Eur J Pharmacol. 2000 Oct 6;406(1):R9-R10.

PMID:
11011051
27.

Using behavior to elucidate receptor mechanisms: a review of the discriminative stimulus effects of benzodiazepines.

Lelas S, Spealman RD, Rowlett JK.

Exp Clin Psychopharmacol. 2000 Aug;8(3):294-311. Review.

PMID:
10975618
28.
29.

Discriminative-stimulus effects of triazolam and midazolam in rhesus monkeys.

Lelas S, Gerak LR, France CP.

Behav Pharmacol. 1999 Feb;10(1):39-50.

PMID:
10780301
30.
31.
32.

Pharmacological profile of a deuterium-substituted mirfentanil derivative, OHM10579, in rhesus monkeys.

Lelas S, Gerak LR, Landers LK, Brandt MR, Bagley JR, Brockunier LL, France CP.

Pharmacol Biochem Behav. 1998 Jul;60(3):665-75.

PMID:
9678650
33.

Interaction of metabolism of aspartate and inosine and energy state of malignant cells.

Kovacević Z, Popović J, Brkljac O, Lelas S.

Biochem J. 1987 Oct 1;247(1):47-51.

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