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Items: 28

1.

Correction to Discovery of Indole- and Indazole-acylsulfonamides as Potent and Selective NaV1.7 Inhibitors for the Treatment of Pain.

Luo G, Chen L, Easton A, Newton A, Bourin C, Shields E, Mosure K, Soars MG, Knox RJ, Matchett M, Pieschl RL, Post-Munson DJ, Wang S, Herrington J, Graef J, Newberry K, Sivarao DV, Senapati A, Bristow LJ, Meanwell NA, Thompson LA, Dzierba C.

J Med Chem. 2019 Feb 28;62(4):2213. doi: 10.1021/acs.jmedchem.9b00202. Epub 2019 Feb 8. No abstract available.

PMID:
30734560
2.

Discovery of Indole- and Indazole-acylsulfonamides as Potent and Selective NaV1.7 Inhibitors for the Treatment of Pain.

Luo G, Chen L, Easton A, Newton A, Bourin C, Shields E, Mosure K, Soars MG, Knox RJ, Matchett M, Pieschl RL, Post-Munson DJ, Wang S, Herrington J, Graef J, Newberry K, Sivarao DV, Senapati A, Bristow LJ, Meanwell NA, Thompson LA, Dzierba C.

J Med Chem. 2019 Jan 24;62(2):831-856. doi: 10.1021/acs.jmedchem.8b01550. Epub 2019 Jan 8. Erratum in: J Med Chem. 2019 Feb 28;62(4):2213.

PMID:
30576602
3.

Preclinical Characterization of (R)-3-((3S,4S)-3-fluoro-4-(4-hydroxyphenyl)piperidin-1-yl)-1-(4-methylbenzyl)pyrrolidin-2-one (BMS-986169), a Novel, Intravenous, Glutamate N-Methyl-d-Aspartate 2B Receptor Negative Allosteric Modulator with Potential in Major Depressive Disorder.

Bristow LJ, Gulia J, Weed MR, Srikumar BN, Li YW, Graef JD, Naidu PS, Sanmathi C, Aher J, Bastia T, Paschapur M, Kalidindi N, Kumar KV, Molski T, Pieschl R, Fernandes A, Brown JM, Sivarao DV, Newberry K, Bookbinder M, Polino J, Keavy D, Newton A, Shields E, Simmermacher J, Kempson J, Li J, Zhang H, Mathur A, Kallem RR, Sinha M, Ramarao M, Vikramadithyan RK, Thangathirupathy S, Warrier J, Islam I, Bronson JJ, Olson RE, Macor JE, Albright CF, King D, Thompson LA, Marcin LR, Sinz M.

J Pharmacol Exp Ther. 2017 Dec;363(3):377-393. doi: 10.1124/jpet.117.242784. Epub 2017 Sep 27.

PMID:
28954811
4.

Discovery of non-zwitterionic aryl sulfonamides as Nav1.7 inhibitors with efficacy in preclinical behavioral models and translational measures of nociceptive neuron activation.

Wu YJ, Guernon J, McClure A, Luo G, Rajamani R, Ng A, Easton A, Newton A, Bourin C, Parker D, Mosure K, Barnaby O, Soars MG, Knox RJ, Matchett M, Pieschl R, Herrington J, Chen P, Sivarao DV, Bristow LJ, Meanwell NA, Bronson J, Olson R, Thompson LA, Dzierba C.

Bioorg Med Chem. 2017 Oct 15;25(20):5490-5505. doi: 10.1016/j.bmc.2017.08.012. Epub 2017 Aug 9.

PMID:
28818462
5.

Difluorocyclobutylacetylenes as positive allosteric modulators of mGluR5 with reduced bioactivation potential.

Degnan AP, Maxwell D, Balakrishnan A, Brown JM, Easton A, Gulianello M, Hanumegowda U, Hill-Drzewi M, Miller R, Santone KS, Senapati A, Shields EE, Sivarao DV, Westphal R, Whiterock VJ, Zhuo X, Bronson JJ, Macor JE.

Bioorg Med Chem Lett. 2016 Dec 15;26(24):5871-5876. doi: 10.1016/j.bmcl.2016.11.014. Epub 2016 Nov 9.

PMID:
27856084
6.

Oxazolidinone-based allosteric modulators of mGluR5: Defining molecular switches to create a pharmacological tool box.

Huang H, Degnan AP, Balakrishnan A, Easton A, Gulianello M, Huang Y, Matchett M, Mattson G, Miller R, Santone KS, Senapati A, Shields EE, Sivarao DV, Snyder LB, Westphal R, Whiterock VJ, Yang F, Bronson JJ, Macor JE.

Bioorg Med Chem Lett. 2016 Sep 1;26(17):4165-9. doi: 10.1016/j.bmcl.2016.07.065. Epub 2016 Jul 28.

PMID:
27496211
7.

The Novel, Nicotinic Alpha7 Receptor Partial Agonist, BMS-933043, Improves Cognition and Sensory Processing in Preclinical Models of Schizophrenia.

Bristow LJ, Easton AE, Li YW, Sivarao DV, Lidge R, Jones KM, Post-Munson D, Daly C, Lodge NJ, Gallagher L, Molski T, Pieschl R, Chen P, Hendricson A, Westphal R, Cook J, Iwuagwu C, Morgan D, Benitex Y, King D, Macor JE, Zaczek R, Olson R.

PLoS One. 2016 Jul 28;11(7):e0159996. doi: 10.1371/journal.pone.0159996. eCollection 2016.

8.

The qEEG Signature of Selective NMDA NR2B Negative Allosteric Modulators; A Potential Translational Biomarker for Drug Development.

Keavy D, Bristow LJ, Sivarao DV, Batchelder M, King D, Thangathirupathy S, Macor JE, Weed MR.

PLoS One. 2016 Apr 1;11(4):e0152729. doi: 10.1371/journal.pone.0152729. eCollection 2016.

9.

Discovery and Preclinical Evaluation of BMS-955829, a Potent Positive Allosteric Modulator of mGluR5.

Yang F, Snyder LB, Balakrishnan A, Brown JM, Sivarao DV, Easton A, Fernandes A, Gulianello M, Hanumegowda UM, Huang H, Huang Y, Jones KM, Li YW, Matchett M, Mattson G, Miller R, Santone KS, Senapati A, Shields EE, Simutis FJ, Westphal R, Whiterock VJ, Bronson JJ, Macor JE, Degnan AP.

ACS Med Chem Lett. 2016 Jan 4;7(3):289-93. doi: 10.1021/acsmedchemlett.5b00450. eCollection 2016 Mar 10.

10.

40 Hz Auditory Steady-State Response Is a Pharmacodynamic Biomarker for Cortical NMDA Receptors.

Sivarao DV, Chen P, Senapati A, Yang Y, Fernandes A, Benitex Y, Whiterock V, Li YW, Ahlijanian MK.

Neuropsychopharmacology. 2016 Aug;41(9):2232-40. doi: 10.1038/npp.2016.17. Epub 2016 Feb 3.

11.

The 40-Hz auditory steady-state response: a selective biomarker for cortical NMDA function.

Sivarao DV.

Ann N Y Acad Sci. 2015 May;1344:27-36. doi: 10.1111/nyas.12739. Epub 2015 Mar 21. Review.

PMID:
25809615
12.

Translational psychiatry--light at the end of the tunnel.

Jones KA, Menniti FS, Sivarao DV.

Ann N Y Acad Sci. 2015 May;1344:1-11. doi: 10.1111/nyas.12725. Epub 2015 Mar 9. Review.

PMID:
25752480
13.

NR2B Antagonist CP-101,606 Abolishes Pitch-Mediated Deviance Detection in Awake Rats.

Sivarao DV, Chen P, Yang Y, Li YW, Pieschl R, Ahlijanian MK.

Front Psychiatry. 2014 Aug 5;5:96. doi: 10.3389/fpsyt.2014.00096. eCollection 2014.

14.

MK-801 disrupts and nicotine augments 40 Hz auditory steady state responses in the auditory cortex of the urethane-anesthetized rat.

Sivarao DV, Frenkel M, Chen P, Healy FL, Lodge NJ, Zaczek R.

Neuropharmacology. 2013 Oct;73:1-9. doi: 10.1016/j.neuropharm.2013.05.006. Epub 2013 May 18.

PMID:
23688921
15.

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
16.

Pyloric sphincter dysfunction in nNOS-/- and W/Wv mutant mice: animal models of gastroparesis and duodenogastric reflux.

Sivarao DV, Mashimo H, Goyal RK.

Gastroenterology. 2008 Oct;135(4):1258-66. doi: 10.1053/j.gastro.2008.06.039. Epub 2008 Jun 20.

17.

Colorectal distension-induced pseudoaffective changes as indices of nociception in the anesthetized female rat: morphine and strain effects on visceral sensitivity.

Sivarao DV, Langdon S, Bernard C, Lodge N.

J Pharmacol Toxicol Methods. 2007 Jul-Aug;56(1):43-50. Epub 2006 Dec 22.

PMID:
17257861
18.

Effect of 4-(5-chloro-2-hydroxyphenyl)-3-(2-hydroxyethyl)-6-(trifluoromethyl)-quinolin-2(1H)-one (BMS-223131), a novel opener of large conductance Ca2+-activated K+ (maxi-K) channels on normal and stress-aggravated colonic motility and visceral nociception.

Sivarao DV, Newberry K, Langdon S, Lee AV, Hewawasam P, Plym MJ, Signor L, Myers R, Lodge NJ.

J Pharmacol Exp Ther. 2005 May;313(2):840-7. Epub 2005 Feb 8. Erratum in: J Pharmacol Exp Ther. 2005 Oct;315(1):476.

PMID:
15701710
20.

Fluorine substitution can block CYP3A4 metabolism-dependent inhibition: identification of (S)-N-[1-(4-fluoro-3- morpholin-4-ylphenyl)ethyl]-3- (4-fluorophenyl)acrylamide as an orally bioavailable KCNQ2 opener devoid of CYP3A4 metabolism-dependent inhibition.

Wu YJ, Davis CD, Dworetzky S, Fitzpatrick WC, Harden D, He H, Knox RJ, Newton AE, Philip T, Polson C, Sivarao DV, Sun LQ, Tertyshnikova S, Weaver D, Yeola S, Zoeckler M, Sinz MW.

J Med Chem. 2003 Aug 28;46(18):3778-81.

PMID:
12930139
21.

(S)-N-[1-(3-morpholin-4-ylphenyl)ethyl]- 3-phenylacrylamide: an orally bioavailable KCNQ2 opener with significant activity in a cortical spreading depression model of migraine.

Wu YJ, Boissard CG, Greco C, Gribkoff VK, Harden DG, He H, L'Heureux A, Kang SH, Kinney GG, Knox RJ, Natale J, Newton AE, Lehtinen-Oboma S, Sinz MW, Sivarao DV, Starrett JE Jr, Sun LQ, Tertyshnikova S, Thompson MW, Weaver D, Wong HS, Zhang L, Dworetzky SI.

J Med Chem. 2003 Jul 17;46(15):3197-200.

PMID:
12852750
22.

Lower esophageal sphincter is achalasic in nNOS(-/-) and hypotensive in W/W(v) mutant mice.

Sivarao DV, Mashimo HL, Thatte HS, Goyal RK.

Gastroenterology. 2001 Jul;121(1):34-42.

PMID:
11438492
23.

Functional anatomy and physiology of the upper esophageal sphincter.

Sivarao DV, Goyal RK.

Am J Med. 2000 Mar 6;108 Suppl 4a:27S-37S. Review.

PMID:
10718448
24.

Excitation of dorsal motor vagal neurons evokes non-nicotinic receptor-mediated gastric relaxation.

Krowicki ZK, Sivarao DV, Abrahams TP, Hornby PJ.

J Auton Nerv Syst. 1999 Sep 24;77(2-3):83-9.

PMID:
10580290
25.

Vagally-regulated gastric motor activity: evidence for kainate and NMDA receptor mediation.

Sivarao DV, Krowicki ZK, Abrahams TP, Hornby PJ.

Eur J Pharmacol. 1999 Mar 5;368(2-3):173-82.

PMID:
10193653
26.

Role of GABAA receptors in rat hindbrain nuclei controlling gastric motor function.

Sivarao DV, Krowicki ZK, Hornby PJ.

Neurogastroenterol Motil. 1998 Aug;10(4):305-13.

PMID:
9697105
27.

Intracisternal antisense oligonucleotides to TRH receptor abolish TRH-evoked gastric motor excitation.

Sivarao DV, Krowicki ZK, Abrahams TP, Hornby PJ.

Am J Physiol. 1997 Jun;272(6 Pt 1):G1372-81.

PMID:
9227472
28.

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