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Items: 28

1.

Pharmacological Characterization of a Novel Beta 3 Adrenergic Agonist, Vibegron: Evaluation of Antimuscarinic Receptor Selectivity for Combination Therapy for Overactive Bladder.

Di Salvo J, Nagabukuro H, Wickham LA, Abbadie C, DeMartino JA, Fitzmaurice A, Gichuru L, Kulick A, Donnelly MJ, Jochnowitz N, Hurley AL, Pereira A, Sanfiz A, Veronin G, Villa K, Woods J, Zamlynny B, Zycband E, Salituro GM, Frenkl T, Weber AE, Edmondson SD, Struthers M.

J Pharmacol Exp Ther. 2017 Feb;360(2):346-355. doi: 10.1124/jpet.116.237313. Epub 2016 Dec 13.

PMID:
27965369
2.

Discovery of novel non-steroidal reverse indole mineralocorticoid receptor antagonists.

Ogawa AK, Bunte EV, Mal R, Lan P, Sun Z, Crespo A, Wiltsie J, Clemas J, Gibson J, Contino L, Lisnock J, Zhou G, Garcia-Calvo M, Jochnowitz N, Ma X, Pan Y, Brown P, Zamlynny B, Bateman T, Leung D, Xu L, Tong X, Liu K, Crook M, Sinclair P.

Bioorg Med Chem Lett. 2016 Jun 15;26(12):2866-2869. doi: 10.1016/j.bmcl.2016.04.052. Epub 2016 Apr 20.

PMID:
27161805
3.

Discovery of Vibegron: A Potent and Selective β3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder.

Edmondson SD, Zhu C, Kar NF, Di Salvo J, Nagabukuro H, Sacre-Salem B, Dingley K, Berger R, Goble SD, Morriello G, Harper B, Moyes CR, Shen DM, Wang L, Ball R, Fitzmaurice A, Frenkl T, Gichuru LN, Ha S, Hurley AL, Jochnowitz N, Levorse D, Mistry S, Miller RR, Ormes J, Salituro GM, Sanfiz A, Stevenson AS, Villa K, Zamlynny B, Green S, Struthers M, Weber AE.

J Med Chem. 2016 Jan 28;59(2):609-23. doi: 10.1021/acs.jmedchem.5b01372. Epub 2016 Jan 8.

PMID:
26709102
4.

Factor XII full and partial null in rat confers robust antithrombotic efficacy with no bleeding.

Cai TQ, Wu W, Shin MK, Xu Y, Jochnowitz N, Zhou Y, Hoos L, Bentley R, Strapps W, Thankappan A, Metzger JM, Ogletree ML, Tadin-Strapps M, Seiffert DA, Chen Z.

Blood Coagul Fibrinolysis. 2015 Dec;26(8):893-902. doi: 10.1097/MBC.0000000000000337.

PMID:
26192114
5.

Improved Stability of Proline-Derived Direct Thrombin Inhibitors through Hydroxyl to Heterocycle Replacement.

Chobanian HR, Pio B, Guo Y, Shen H, Huffman MA, Madeira M, Salituro G, Terebetski JL, Ormes J, Jochnowitz N, Hoos L, Zhou Y, Lewis D, Hawes B, Mitnaul L, O'Neill K, Ellsworth K, Wang L, Biftu T, Duffy JL.

ACS Med Chem Lett. 2015 Mar 13;6(5):553-7. doi: 10.1021/acsmedchemlett.5b00047. eCollection 2015 May 14.

6.

Titrating haemophilia B phenotypes using siRNA strategy: evidence that antithrombotic activity is separated from bleeding liability.

Metzger JM, Tadin-Strapps M, Thankappan A, Strapps WR, DiPietro M, Leander K, Zhang Z, Shin MK, Levorse J, Desai K, Xu Y, Lai K, Wu W, Chen Z, Cai TQ, Jochnowitz N, Bentley R, Hoos L, Zhou Y, Sepp-Lorenzino L, Seiffert D, Andre P.

Thromb Haemost. 2015 Jun;113(6):1300-11. doi: 10.1160/TH14-06-0505. Epub 2015 Mar 19.

PMID:
25790442
7.

Proof-of-concept Studies for siRNA-mediated Gene Silencing for Coagulation Factors in Rat and Rabbit.

Chen Z, Luo B, Cai TQ, Thankappan A, Xu Y, Wu W, DiMuzio J, Lifsted T, DiPietro M, Disa J, Ng B, Leander K, Clark S, Hoos L, Zhou Y, Jochnowitz N, Jachec C, Szczerba P, Gindy ME, Strapps W, Sepp-Lorenzino L, Seiffert DA, Lubbers L, Tadin-Strapps M.

Mol Ther Nucleic Acids. 2015 Jan 27;4:e224. doi: 10.1038/mtna.2014.75.

8.

Discovery of MK-4409, a Novel Oxazole FAAH Inhibitor for the Treatment of Inflammatory and Neuropathic Pain.

Chobanian HR, Guo Y, Liu P, Chioda MD, Fung S, Lanza TJ, Chang L, Bakshi RK, Dellureficio JP, Hong Q, McLaughlin M, Belyk KM, Krska SW, Makarewicz AK, Martel EJ, Leone JF, Frey L, Karanam B, Madeira M, Alvaro R, Shuman J, Salituro G, Terebetski JL, Jochnowitz N, Mistry S, McGowan E, Hajdu R, Rosenbach M, Abbadie C, Alexander JP, Shiao LL, Sullivan KM, Nargund RP, Wyvratt MJ, Lin LS, DeVita RJ.

ACS Med Chem Lett. 2014 Apr 10;5(6):717-21. doi: 10.1021/ml5001239. eCollection 2014 Jun 12.

9.

Discovery of MK-3168: A PET Tracer for Imaging Brain Fatty Acid Amide Hydrolase.

Liu P, Hamill TG, Chioda M, Chobanian H, Fung S, Guo Y, Chang L, Bakshi R, Hong Q, Dellureficio J, Lin LS, Abbadie C, Alexander J, Jin H, Mandala S, Shiao LL, Li W, Sanabria S, Williams D, Zeng Z, Hajdu R, Jochnowitz N, Rosenbach M, Karanam B, Madeira M, Salituro G, Powell J, Xu L, Terebetski JL, Leone JF, Miller P, Cook J, Holahan M, Joshi A, O'Malley S, Purcell M, Posavec D, Chen TB, Riffel K, Williams M, Hargreaves R, Sullivan KA, Nargund RP, DeVita RJ.

ACS Med Chem Lett. 2013 Apr 20;4(6):509-13. doi: 10.1021/ml4000996. eCollection 2013 Jun 13.

10.

Improved Cav2.2 Channel Inhibitors through a gem-Dimethylsulfone Bioisostere Replacement of a Labile Sulfonamide.

Shao PP, Ye F, Chakravarty PK, Herrington JB, Dai G, Bugianesi RM, Haedo RJ, Swensen AM, Warren VA, Smith MM, Garcia ML, McManus OB, Lyons KA, Li X, Green M, Jochnowitz N, McGowan E, Mistry S, Sun SY, Abbadie C, Kaczorowski GJ, Duffy JL.

ACS Med Chem Lett. 2013 Sep 8;4(11):1064-8. doi: 10.1021/ml4002612. eCollection 2013 Nov 14.

11.

Design, synthesis, and evaluation of conformationally restricted acetanilides as potent and selective β3 adrenergic receptor agonists for the treatment of overactive bladder.

Moyes CR, Berger R, Goble SD, Harper B, Shen DM, Wang L, Bansal A, Brown PN, Chen AS, Dingley KH, Di Salvo J, Fitzmaurice A, Gichuru LN, Hurley AL, Jochnowitz N, Miller RR, Mistry S, Nagabukuro H, Salituro GM, Sanfiz A, Stevenson AS, Villa K, Zamlynny B, Struthers M, Weber AE, Edmondson SD.

J Med Chem. 2014 Feb 27;57(4):1437-53. doi: 10.1021/jm4017224. Epub 2014 Feb 5.

PMID:
24437735
12.

Factor XIIa inhibition by Infestin-4: in vitro mode of action and in vivo antithrombotic benefit.

Xu Y, Cai TQ, Castriota G, Zhou Y, Hoos L, Jochnowitz N, Loewrigkeit C, Cook JA, Wickham A, Metzger JM, Ogletree ML, Seiffert DA, Chen Z.

Thromb Haemost. 2014 Apr 1;111(4):694-704. doi: 10.1160/TH13-08-0668. Epub 2013 Dec 12.

PMID:
24336918
13.

A novel benzazepinone sodium channel blocker with oral efficacy in a rat model of neuropathic pain.

Hoyt SB, London C, Abbadie C, Felix JP, Garcia ML, Jochnowitz N, Karanam BV, Li X, Lyons KA, McGowan E, Priest BT, Smith MM, Warren VA, Thomas-Fowlkes BS, Kaczorowski GJ, Duffy JL.

Bioorg Med Chem Lett. 2013 Jun 15;23(12):3640-5. doi: 10.1016/j.bmcl.2013.03.121. Epub 2013 Apr 5.

PMID:
23652221
14.

Aminopiperidine sulfonamide Cav2.2 channel inhibitors for the treatment of chronic pain.

Shao PP, Ye F, Chakravarty PK, Varughese DJ, Herrington JB, Dai G, Bugianesi RM, Haedo RJ, Swensen AM, Warren VA, Smith MM, Garcia ML, McManus OB, Lyons KA, Li X, Green M, Jochnowitz N, McGowan E, Mistry S, Sun SY, Abbadie C, Kaczorowski GJ, Duffy JL.

J Med Chem. 2012 Nov 26;55(22):9847-55. doi: 10.1021/jm301056k. Epub 2012 Nov 12.

PMID:
23098566
15.

A potent and selective indole N-type calcium channel (Ca(v)2.2) blocker for the treatment of pain.

Tyagarajan S, Chakravarty PK, Park M, Zhou B, Herrington JB, Ratliff K, Bugianesi RM, Williams B, Haedo RJ, Swensen AM, Warren VA, Smith M, Garcia M, Kaczorowski GJ, McManus OB, Lyons KA, Li X, Madeira M, Karanam B, Green M, Forrest MJ, Abbadie C, McGowan E, Mistry S, Jochnowitz N, Duffy JL.

Bioorg Med Chem Lett. 2011 Jan 15;21(2):869-73. doi: 10.1016/j.bmcl.2010.11.067. Epub 2010 Nov 21.

PMID:
21195616
16.

Discovery of a novel class of biphenyl pyrazole sodium channel blockers for treatment of neuropathic pain.

Tyagarajan S, Chakravarty PK, Zhou B, Taylor B, Eid R, Fisher MH, Parsons WH, Wyvratt MJ, Lyons KA, Klatt T, Li X, Kumar S, Williams B, Felix J, Priest BT, Brochu RM, Warren V, Smith M, Garcia M, Kaczorowski GJ, Martin WJ, Abbadie C, McGowan E, Jochnowitz N, Weber A, Duffy JL.

Bioorg Med Chem Lett. 2010 Dec 15;20(24):7479-82. doi: 10.1016/j.bmcl.2010.10.017. Epub 2010 Oct 14.

PMID:
21106456
17.

Substituted biaryl oxazoles, imidazoles, and thiazoles as sodium channel blockers.

Tyagarajan S, Chakravarty PK, Zhou B, Fisher MH, Wyvratt MJ, Lyons K, Klatt T, Li X, Kumar S, Williams B, Felix J, Priest BT, Brochu RM, Warren V, Smith M, Garcia M, Kaczorowski GJ, Martin WJ, Abbadie C, McGowan E, Jochnowitz N, Parsons WH.

Bioorg Med Chem Lett. 2010 Sep 15;20(18):5536-40. doi: 10.1016/j.bmcl.2010.07.064. Epub 2010 Jul 21.

PMID:
20709552
18.

Substituted biaryl pyrazoles as sodium channel blockers.

Tyagarajan S, Chakravarty PK, Zhou B, Taylor B, Fisher MH, Wyvratt MJ, Lyons K, Klatt T, Li X, Kumar S, Williams B, Felix J, Priest BT, Brochu RM, Warren V, Smith M, Garcia M, Kaczorowski GJ, Martin WJ, Abbadie C, McGowan E, Jochnowitz N, Parsons WH.

Bioorg Med Chem Lett. 2010 Sep 15;20(18):5480-3. doi: 10.1016/j.bmcl.2010.07.080. Epub 2010 Jul 24.

PMID:
20709545
19.

Analgesic effects of a substituted N-triazole oxindole (TROX-1), a state-dependent, voltage-gated calcium channel 2 blocker.

Abbadie C, McManus OB, Sun SY, Bugianesi RM, Dai G, Haedo RJ, Herrington JB, Kaczorowski GJ, Smith MM, Swensen AM, Warren VA, Williams B, Arneric SP, Eduljee C, Snutch TP, Tringham EW, Jochnowitz N, Liang A, Euan MacIntyre D, McGowan E, Mistry S, White VV, Hoyt SB, London C, Lyons KA, Bunting PB, Volksdorf S, Duffy JL.

J Pharmacol Exp Ther. 2010 Aug;334(2):545-55. doi: 10.1124/jpet.110.166363. Epub 2010 May 3.

PMID:
20439438
20.

Correlation between pharmacologically-induced changes in cystometric parameters and spinal c-Fos expression in rats.

Nagabukuro H, Degenhardt A, Villa KL, Mistry SL, Gichuru L, Jochnowitz N, Abbadie C.

Auton Neurosci. 2010 Aug 25;156(1-2):19-26. doi: 10.1016/j.autneu.2010.02.006. Epub 2010 Mar 24.

PMID:
20335078
21.

Fasting enhances the response of arcuate neuropeptide Y-glucose-inhibited neurons to decreased extracellular glucose.

Murphy BA, Fioramonti X, Jochnowitz N, Fakira K, Gagen K, Contie S, Lorsignol A, Penicaud L, Martin WJ, Routh VH.

Am J Physiol Cell Physiol. 2009 Apr;296(4):C746-56. doi: 10.1152/ajpcell.00641.2008. Epub 2009 Feb 11.

22.

The role of melanin-concentrating hormone-1 receptors in the voiding reflex in rats.

Hegde LG, Ping XL, Jochnowitz N, Craig DA.

J Pharmacol Exp Ther. 2009 Jan;328(1):165-73. doi: 10.1124/jpet.108.143495. Epub 2008 Oct 10.

PMID:
18849359
23.

Imidazopyridines: a novel class of hNav1.7 channel blockers.

London C, Hoyt SB, Parsons WH, Williams BS, Warren VA, Tschirret-Guth R, Smith MM, Priest BT, McGowan E, Martin WJ, Lyons KA, Li X, Karanam BV, Jochnowitz N, Garcia ML, Felix JP, Dean B, Abbadie C, Kaczorowski GJ, Duffy JL.

Bioorg Med Chem Lett. 2008 Mar 1;18(5):1696-701. doi: 10.1016/j.bmcl.2008.01.047. Epub 2008 Jan 18.

PMID:
18243692
24.

Benzazepinone Nav1.7 blockers: potential treatments for neuropathic pain.

Hoyt SB, London C, Ok H, Gonzalez E, Duffy JL, Abbadie C, Dean B, Felix JP, Garcia ML, Jochnowitz N, Karanam BV, Li X, Lyons KA, McGowan E, Macintyre DE, Martin WJ, Priest BT, Smith MM, Tschirret-Guth R, Warren VA, Williams BS, Kaczorowski GJ, Parsons WH.

Bioorg Med Chem Lett. 2007 Nov 15;17(22):6172-7. Epub 2007 Sep 11.

PMID:
17889534
25.

Reversal of neuropathic pain by alpha-hydroxyphenylamide: a novel sodium channel antagonist.

Ko SH, Jochnowitz N, Lenkowski PW, Batts TW, Davis GC, Martin WJ, Brown ML, Patel MK.

Neuropharmacology. 2006 Jun;50(7):865-73. Epub 2006 Feb 7.

PMID:
16464480
26.
27.

Association of lipid peroxidation with antenatal betamethasone and oxygen radial disorders in preterm infants.

Weinberger B, Anwar M, Henien S, Sosnovsky A, Hiatt M, Jochnowitz N, Witz G, Hegyi T.

Biol Neonate. 2004;85(2):121-7. Epub 2003 Nov 19.

PMID:
14631157
28.

Treatment of mice with methamphetamine produces cell loss in the substantia nigra.

Sonsalla PK, Jochnowitz ND, Zeevalk GD, Oostveen JA, Hall ED.

Brain Res. 1996 Oct 28;738(1):172-5.

PMID:
8949944

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