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Items: 47

1.

Pharmacological Characterization of a Novel 5-Hydroxybenzothiazolone-Derived β 2-Adrenoceptor Agonist with Functional Selectivity for Anabolic Effects on Skeletal Muscle Resulting in a Wider Cardiovascular Safety Window in Preclinical Studies.

Koziczak-Holbro M, Rigel DF, Dumotier B, Sykes DA, Tsao J, Nguyen NH, Bösch J, Jourdain M, Flotte L, Adachi Y, Kiffe M, Azria M, Fairhurst RA, Charlton SJ, Richardson BP, Lach-Trifilieff E, Glass DJ, Ullrich T, Hatakeyama S.

J Pharmacol Exp Ther. 2019 May;369(2):188-199. doi: 10.1124/jpet.118.255307. Epub 2019 Feb 28.

PMID:
30819762
2.

Sacubitril/valsartan (LCZ696) significantly reduces aldosterone and increases cGMP circulating levels in a canine model of RAAS activation.

Mochel JP, Teng CH, Peyrou M, Giraudel J, Danhof M, Rigel DF.

Eur J Pharm Sci. 2019 Feb 1;128:103-111. doi: 10.1016/j.ejps.2018.11.037. Epub 2018 Nov 30.

PMID:
30508581
3.

Discovery of a Novel Piperidine-Based Inhibitor of Cholesteryl Ester Transfer Protein (CETP) That Retains Activity in Hypertriglyceridemic Plasma.

Yamada K, Brousseau M, Honma W, Iimura A, Imase H, Iwaki Y, Kawanami T, LaSala D, Liang G, Mitani H, Nonomura K, Ohmori O, Pan M, Rigel DF, Umemura I, Yasoshima K, Zhu G, Mogi M.

J Med Chem. 2017 Oct 26;60(20):8466-8481. doi: 10.1021/acs.jmedchem.7b00900. Epub 2017 Oct 16.

PMID:
29035537
4.

Optimization of Allosteric With-No-Lysine (WNK) Kinase Inhibitors and Efficacy in Rodent Hypertension Models.

Yamada K, Levell J, Yoon T, Kohls D, Yowe D, Rigel DF, Imase H, Yuan J, Yasoshima K, DiPetrillo K, Monovich L, Xu L, Zhu M, Kato M, Jain M, Idamakanti N, Taslimi P, Kawanami T, Argikar UA, Kunjathoor V, Xie X, Yagi YI, Iwaki Y, Robinson Z, Park HM.

J Med Chem. 2017 Aug 24;60(16):7099-7107. doi: 10.1021/acs.jmedchem.7b00708. Epub 2017 Aug 3.

PMID:
28771350
5.

Characterization and Prediction of Cardiovascular Effects of Fingolimod and Siponimod Using a Systems Pharmacology Modeling Approach.

Snelder N, Ploeger BA, Luttringer O, Rigel DF, Webb RL, Feldman D, Fu F, Beil M, Jin L, Stanski DR, Danhof M.

J Pharmacol Exp Ther. 2017 Feb;360(2):356-367. doi: 10.1124/jpet.116.236208. Epub 2016 Dec 1.

PMID:
27934627
6.

Small-molecule WNK inhibition regulates cardiovascular and renal function.

Yamada K, Park HM, Rigel DF, DiPetrillo K, Whalen EJ, Anisowicz A, Beil M, Berstler J, Brocklehurst CE, Burdick DA, Caplan SL, Capparelli MP, Chen G, Chen W, Dale B, Deng L, Fu F, Hamamatsu N, Harasaki K, Herr T, Hoffmann P, Hu QY, Huang WJ, Idamakanti N, Imase H, Iwaki Y, Jain M, Jeyaseelan J, Kato M, Kaushik VK, Kohls D, Kunjathoor V, LaSala D, Lee J, Liu J, Luo Y, Ma F, Mo R, Mowbray S, Mogi M, Ossola F, Pandey P, Patel SJ, Raghavan S, Salem B, Shanado YH, Trakshel GM, Turner G, Wakai H, Wang C, Weldon S, Wielicki JB, Xie X, Xu L, Yagi YI, Yasoshima K, Yin J, Yowe D, Zhang JH, Zheng G, Monovich L.

Nat Chem Biol. 2016 Nov;12(11):896-898. doi: 10.1038/nchembio.2168. Epub 2016 Sep 5.

PMID:
27595330
7.

Discovery of N-[5-(6-Chloro-3-cyano-1-methyl-1H-indol-2-yl)-pyridin-3-ylmethyl]-ethanesulfonamide, a Cortisol-Sparing CYP11B2 Inhibitor that Lowers Aldosterone in Human Subjects.

Papillon JP, Lou C, Singh AK, Adams CM, Ksander GM, Beil ME, Chen W, Leung-Chu J, Fu F, Gan L, Hu CW, Jeng AY, LaSala D, Liang G, Rigel DF, Russell KS, Vest JA, Watson C.

J Med Chem. 2015 Dec 10;58(23):9382-94. doi: 10.1021/acs.jmedchem.5b01545. Epub 2015 Nov 18.

PMID:
26540564
8.

Structure-Activity Relationships, Pharmacokinetics, and in Vivo Activity of CYP11B2 and CYP11B1 Inhibitors.

Papillon JP, Adams CM, Hu QY, Lou C, Singh AK, Zhang C, Carvalho J, Rajan S, Amaral A, Beil ME, Fu F, Gangl E, Hu CW, Jeng AY, LaSala D, Liang G, Logman M, Maniara WM, Rigel DF, Smith SA, Ksander GM.

J Med Chem. 2015 Jun 11;58(11):4749-70. doi: 10.1021/acs.jmedchem.5b00407. Epub 2015 May 21.

PMID:
25953419
9.

trans-3,4-Disubstituted pyrrolidines as inhibitors of the human aspartyl protease renin. Part II: prime site exploration using an oxygen linker.

Sellner H, Cottens S, Cumin F, Ehrhardt C, Kosaka T, Lorthiois E, Ostermann N, Webb RL, Rigel DF, Wagner T, Maibaum J.

Bioorg Med Chem Lett. 2015 Apr 15;25(8):1787-1791. doi: 10.1016/j.bmcl.2015.02.040. Epub 2015 Feb 23.

PMID:
25754490
10.

Aldosterone synthase inhibition: cardiorenal protection in animal disease models and translation of hormonal effects to human subjects.

Ménard J, Rigel DF, Watson C, Jeng AY, Fu F, Beil M, Liu J, Chen W, Hu CW, Leung-Chu J, LaSala D, Liang G, Rebello S, Zhang Y, Dole WP.

J Transl Med. 2014 Dec 10;12:340. doi: 10.1186/s12967-014-0340-9.

11.

Structure-based design of substituted piperidines as a new class of highly efficacious oral direct Renin inhibitors.

Ehara T, Irie O, Kosaka T, Kanazawa T, Breitenstein W, Grosche P, Ostermann N, Suzuki M, Kawakami S, Konishi K, Hitomi Y, Toyao A, Gunji H, Cumin F, Schiering N, Wagner T, Rigel DF, Webb RL, Maibaum J, Yokokawa F.

ACS Med Chem Lett. 2014 Apr 21;5(7):787-92. doi: 10.1021/ml500137b. eCollection 2014 Jul 10.

12.

Drug effects on the CVS in conscious rats: separating cardiac output into heart rate and stroke volume using PKPD modelling.

Snelder N, Ploeger BA, Luttringer O, Rigel DF, Fu F, Beil M, Stanski DR, Danhof M.

Br J Pharmacol. 2014 Nov;171(22):5076-92. doi: 10.1111/bph.12824. Epub 2014 Sep 5.

13.

Discovery and in Vivo Evaluation of Potent Dual CYP11B2 (Aldosterone Synthase) and CYP11B1 Inhibitors.

Meredith EL, Ksander G, Monovich LG, Papillon JP, Liu Q, Miranda K, Morris P, Rao C, Burgis R, Capparelli M, Hu QY, Singh A, Rigel DF, Jeng AY, Beil M, Fu F, Hu CW, LaSala D.

ACS Med Chem Lett. 2013 Oct 17;4(12):1203-7. doi: 10.1021/ml400324c. eCollection 2013 Dec 12.

14.

Chronic measurement of left ventricular pressure in freely moving rats.

Stehlin E, Malpas SC, Budgett DM, Barrett CJ, McCormick D, Whalley G, Fu F, Beil M, Rigel DF, Guild SJ.

J Appl Physiol (1985). 2013 Dec;115(11):1672-82. doi: 10.1152/japplphysiol.00683.2013. Epub 2013 Oct 10.

15.

PKPD modelling of the interrelationship between mean arterial BP, cardiac output and total peripheral resistance in conscious rats.

Snelder N, Ploeger BA, Luttringer O, Rigel DF, Webb RL, Feldman D, Fu F, Beil M, Jin L, Stanski DR, Danhof M.

Br J Pharmacol. 2013 Aug;169(7):1510-24. doi: 10.1111/bph.12190.

16.

The discovery of novel potent trans-3,4-disubstituted pyrrolidine inhibitors of the human aspartic protease renin from in silico three-dimensional (3D) pharmacophore searches.

Lorthiois E, Breitenstein W, Cumin F, Ehrhardt C, Francotte E, Jacoby E, Ostermann N, Sellner H, Kosaka T, Webb RL, Rigel DF, Hassiepen U, Richert P, Wagner T, Maibaum J.

J Med Chem. 2013 Mar 28;56(6):2207-17. doi: 10.1021/jm3017078. Epub 2013 Mar 15.

PMID:
23425156
17.

A novel class of oral direct renin inhibitors: highly potent 3,5-disubstituted piperidines bearing a tricyclic p3-p1 pharmacophore.

Ostermann N, Ruedisser S, Ehrhardt C, Breitenstein W, Marzinzik A, Jacoby E, Vangrevelinghe E, Ottl J, Klumpp M, Hartwieg JC, Cumin F, Hassiepen U, Trappe J, Sedrani R, Geisse S, Gerhartz B, Richert P, Francotte E, Wagner T, Krömer M, Kosaka T, Webb RL, Rigel DF, Maibaum J, Baeschlin DK.

J Med Chem. 2013 Mar 28;56(6):2196-206. doi: 10.1021/jm301706j. Epub 2013 Mar 15.

PMID:
23360239
18.

The discovery of potent inhibitors of aldosterone synthase that exhibit selectivity over 11-beta-hydroxylase.

Adams CM, Hu CW, Jeng AY, Karki R, Ksander G, Lasala D, Leung-Chu J, Liang G, Liu Q, Meredith E, Rao C, Rigel DF, Shi J, Smith S, Springer C, Zhang C.

Bioorg Med Chem Lett. 2010 Aug 1;20(15):4324-7. doi: 10.1016/j.bmcl.2010.06.086. Epub 2010 Jun 19.

PMID:
20615692
19.

Pharmacodynamic and pharmacokinetic characterization of the aldosterone synthase inhibitor FAD286 in two rodent models of hyperaldosteronism: comparison with the 11beta-hydroxylase inhibitor metyrapone.

Rigel DF, Fu F, Beil M, Hu CW, Liang G, Jeng AY.

J Pharmacol Exp Ther. 2010 Jul;334(1):232-43. doi: 10.1124/jpet.110.167148. Epub 2010 Mar 30.

PMID:
20354176
20.

Pharmacokinetics and pharmacodynamics of LCZ696, a novel dual-acting angiotensin receptor-neprilysin inhibitor (ARNi).

Gu J, Noe A, Chandra P, Al-Fayoumi S, Ligueros-Saylan M, Sarangapani R, Maahs S, Ksander G, Rigel DF, Jeng AY, Lin TH, Zheng W, Dole WP.

J Clin Pharmacol. 2010 Apr;50(4):401-14. doi: 10.1177/0091270009343932. Epub 2009 Nov 23.

PMID:
19934029
21.

Echocardiographic examination in rats and mice.

Liu J, Rigel DF.

Methods Mol Biol. 2009;573:139-55. doi: 10.1007/978-1-60761-247-6_8. Review.

PMID:
19763926
22.

Recombinant human complement C5a receptor antagonist reduces infarct size after surgical revascularization.

Riley RD, Sato H, Zhao ZQ, Thourani VH, Jordan JE, Fernandez AX, Ma XL, Hite DR, Rigel DF, Pellas TC, Peppard J, Bill KA, Lappe RW, Vinten-Johansen J.

J Thorac Cardiovasc Surg. 2000 Aug;120(2):350-8.

23.

Tissue-specific pattern of stress kinase activation in ischemic/reperfused heart and kidney.

Yin T, Sandhu G, Wolfgang CD, Burrier A, Webb RL, Rigel DF, Hai T, Whelan J.

J Biol Chem. 1997 Aug 8;272(32):19943-50.

24.
25.

In vitro and in vivo evaluation of an endothelin inhibitor reveals novel K+ channel opening activity.

Webb RL, Hu S, Sills MA, Bazil MK, Cioffi CL, Shetty SS, Lappe RW, Rigel DF.

Biochem Biophys Res Commun. 1996 Oct 3;227(1):176-81.

PMID:
8858121
26.
27.
28.

Central and peripheral effects of sculpin pancreatic polypeptide and anglerfish peptide Y in rats.

Balasubramaniam A, Rigel DF, Chance WT, Fischer JE.

Pept Res. 1992 Mar-Apr;5(2):106-9.

PMID:
1581637
29.
30.
32.

N-alpha-biotinylated-neuropeptide Y analogs: syntheses, cardiovascular properties, and application to cardiac NPY receptor visualization.

Balasubramaniam A, Sheriff S, Ferguson DG, Stein M, Rigel DF.

Peptides. 1990 Nov-Dec;11(6):1151-6.

PMID:
1965029
33.

Salmon pancreatic polypeptide exhibits neuropeptide Y-like activities in rats.

Balasubramaniam A, Rigel DF, Chance WT, Stein M, Fischer JE, King D, Plisetskaya EM.

Peptides. 1990 Jul-Aug;11(4):673-7.

PMID:
2235676
34.

Characterization of neuropeptide Y binding sites in rat cardiac ventricular membranes.

Balasubramaniam A, Sheriff S, Rigel DF, Fischer JE.

Peptides. 1990 May-Jun;11(3):545-50.

PMID:
2166278
35.

Reduced amino acid transport in skeletal muscle caused by a circulating factor during endotoxemia.

Warner BW, Hasselgren PO, James JH, Hummel RP 3rd, Rigel DF, Fischer JE.

Ann Surg. 1990 Mar;211(3):323-8.

36.

Interaction of 125I-neuropeptide Y with rat cardiac membranes.

Sheriff S, Rigel DF, Fischer JE, Balasubramaniam A.

Neuropeptides. 1990 Mar;15(3):157-60.

PMID:
2174520
37.

Contractile effects of cardiac neuropeptides in isolated canine atrial and ventricular muscles.

Rigel DF, Grupp IL, Balasubramaniam A, Grupp G.

Am J Physiol. 1989 Oct;257(4 Pt 2):H1082-7.

PMID:
2801971
38.

Synthesis and biological properties of 4-norleucine-neuropeptide Y; secondary structure of neuropeptide Y.

Balasubramaniam A, Renugopalakrishnan V, Rigel DF, Nussbaum MS, Rapaka RS, Dobbs JC, Carreira LA, Fischer JE.

Biochim Biophys Acta. 1989 Aug 31;997(3):176-81.

PMID:
2765554
40.

Glycine-extended anglerfish peptide YG (aPY) a neuropeptide Y (NPY) homologue may be a precursor of a biologically active peptide.

Balasubramaniam A, Andrews PC, Renugopalakrishnan V, Rigel DF.

Peptides. 1989 May-Jun;10(3):581-5.

PMID:
2780417
42.

Hemodynamic and metabolic alterations during experimental sepsis in young and adult rats.

Pedersen PV, Warner BW, Bjornson HS, Hiyama DT, Li S, Rigel DF, Hasselgren PO, Fischer JE.

Surg Gynecol Obstet. 1989 Feb;168(2):148-56.

PMID:
2911792
43.

Syntheses and receptor affinities of partial sequences of peptide YY (PYY).

Balasubramaniam A, Servin AL, Rigel DF, Rouyer-Fessard CR, Laburthe M.

Pept Res. 1988 Sep-Oct;1(1):32-5.

PMID:
2856553
44.
45.

Superoxide dismutase in rats with sepsis. Effect on survival rate and amino acid transport.

Warner BW, Hasselgren PO, James JH, Bialkowska H, Rigel DF, Ogle C, Fischer JE.

Arch Surg. 1987 Oct;122(10):1142-6.

PMID:
3662793
46.

Effects of antihistamines and local anesthetics on excess tachycardia in conscious dogs.

Rigel DF, Katona PG.

J Pharmacol Exp Ther. 1986 Jul;238(1):367-71.

PMID:
2873237
47.

Excess tachycardia: heart rate after antimuscarinic agents in conscious dogs.

Rigel DF, Lipson D, Katona PG.

Am J Physiol. 1984 Feb;246(2 Pt 2):H168-73.

PMID:
6696128

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