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Results: 1 to 20 of 91

Similar articles for PubMed (Select 22435740)

1.

(1aR,5aR)1a,3,5,5a-Tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalene-4-carboxylic acid (MK-1903): a potent GPR109a agonist that lowers free fatty acids in humans.

Boatman PD, Lauring B, Schrader TO, Kasem M, Johnson BR, Skinner P, Jung JK, Xu J, Cherrier MC, Webb PJ, Semple G, Sage CR, Knudsen J, Chen R, Luo WL, Caro L, Cote J, Lai E, Wagner J, Taggart AK, Carballo-Jane E, Hammond M, Colletti SL, Tata JR, Connolly DT, Waters MG, Richman JG.

J Med Chem. 2012 Apr 26;55(8):3644-66. doi: 10.1021/jm2010964. Epub 2012 Apr 9.

PMID:
22435740
2.

3-(1H-tetrazol-5-yl)-1,4,5,6-tetrahydro-cyclopentapyrazole (MK-0354): a partial agonist of the nicotinic acid receptor, G-protein coupled receptor 109a, with antilipolytic but no vasodilatory activity in mice.

Semple G, Skinner PJ, Gharbaoui T, Shin YJ, Jung JK, Cherrier MC, Webb PJ, Tamura SY, Boatman PD, Sage CR, Schrader TO, Chen R, Colletti SL, Tata JR, Waters MG, Cheng K, Taggart AK, Cai TQ, Carballo-Jane E, Behan DP, Connolly DT, Richman JG.

J Med Chem. 2008 Aug 28;51(16):5101-8. doi: 10.1021/jm800258p. Epub 2008 Jul 30.

PMID:
18665582
3.

Fluorinated pyrazole acids are agonists of the high affinity niacin receptor GPR109a.

Skinner PJ, Cherrier MC, Webb PJ, Shin YJ, Gharbaoui T, Lindstrom A, Hong V, Tamura SY, Dang HT, Pride CC, Chen R, Richman JG, Connolly DT, Semple G.

Bioorg Med Chem Lett. 2007 Oct 15;17(20):5620-3. Epub 2007 Aug 23.

PMID:
17804224
4.

Niacin lipid efficacy is independent of both the niacin receptor GPR109A and free fatty acid suppression.

Lauring B, Taggart AK, Tata JR, Dunbar R, Caro L, Cheng K, Chin J, Colletti SL, Cote J, Khalilieh S, Liu J, Luo WL, Maclean AA, Peterson LB, Polis AB, Sirah W, Wu TJ, Liu X, Jin L, Wu K, Boatman PD, Semple G, Behan DP, Connolly DT, Lai E, Wagner JA, Wright SD, Cuffie C, Mitchel YB, Rader DJ, Paolini JF, Waters MG, Plump A.

Sci Transl Med. 2012 Aug 22;4(148):148ra115. doi: 10.1126/scitranslmed.3003877.

5.

GPR109a agonists. Part 2: pyrazole-acids as agonists of the human orphan G-protein coupled receptor GPR109a.

Imbriglio JE, Chang S, Liang R, Raghavan S, Schmidt D, Smenton A, Tria S, Schrader TO, Jung JK, Esser C, Holt TG, Wolff MS, Taggart AK, Cheng K, Carballo-Jane E, Waters MG, Tata JR, Colletti SL.

Bioorg Med Chem Lett. 2010 Aug 1;20(15):4472-4. doi: 10.1016/j.bmcl.2010.06.041. Epub 2010 Jun 10.

PMID:
20615702
6.

Niacin stimulates adiponectin secretion through the GPR109A receptor.

Plaisance EP, Lukasova M, Offermanns S, Zhang Y, Cao G, Judd RL.

Am J Physiol Endocrinol Metab. 2009 Mar;296(3):E549-58. doi: 10.1152/ajpendo.91004.2008. Epub 2009 Jan 13.

7.

Potent tricyclic pyrazole tetrazole agonists of the nicotinic acid receptor (GPR109a).

Boatman PD, Schrader TO, Kasem M, Johnson BR, Skinner PJ, Jung JK, Xu J, Cherrier MC, Webb PJ, Semple G, Sage CR, Knudsen J, Chen R, Taggart AK, Carballo-Jane E, Richman JG.

Bioorg Med Chem Lett. 2010 May 1;20(9):2797-800. doi: 10.1016/j.bmcl.2010.03.062. Epub 2010 Mar 20.

PMID:
20363624
8.

beta-Arrestin1 mediates nicotinic acid-induced flushing, but not its antilipolytic effect, in mice.

Walters RW, Shukla AK, Kovacs JJ, Violin JD, DeWire SM, Lam CM, Chen JR, Muehlbauer MJ, Whalen EJ, Lefkowitz RJ.

J Clin Invest. 2009 May;119(5):1312-21. doi: 10.1172/JCI36806. Epub 2009 Apr 6.

9.

The psoriasis drug monomethylfumarate is a potent nicotinic acid receptor agonist.

Tang H, Lu JY, Zheng X, Yang Y, Reagan JD.

Biochem Biophys Res Commun. 2008 Oct 31;375(4):562-5. doi: 10.1016/j.bbrc.2008.08.041. Epub 2008 Aug 21.

PMID:
18722346
10.

Pyrazole acids as niacin receptor agonists for the treatment of dyslipidemia.

Schmidt D, Smenton A, Raghavan S, Carballo-Jane E, Lubell S, Ciecko T, Holt TG, Wolff M, Taggart A, Wilsie L, Krsmanovic M, Ren N, Blom D, Cheng K, McCann PE, Gerard Waters M, Tata J, Colletti S.

Bioorg Med Chem Lett. 2009 Aug 15;19(16):4768-72. doi: 10.1016/j.bmcl.2009.06.054. Epub 2009 Jun 17.

PMID:
19592242
11.

Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate.

Shen HC, Ding FX, Raghavan S, Deng Q, Luell S, Forrest MJ, Carballo-Jane E, Wilsie LC, Krsmanovic ML, Taggart AK, Wu KK, Wu TJ, Cheng K, Ren N, Cai TQ, Chen Q, Wang J, Wolff MS, Tong X, Holt TG, Waters MG, Hammond ML, Tata JR, Colletti SL.

J Med Chem. 2010 Mar 25;53(6):2666-70. doi: 10.1021/jm100022r.

PMID:
20184326
12.

Comparison of rat and dog models of vasodilatation and lipolysis for the calculation of a therapeutic index for GPR109A agonists.

Carballo-Jane E, Gerckens LS, Luell S, Parlapiano AS, Wolff M, Colletti SL, Tata JR, Taggart AK, Waters MG, Richman JG, McCann ME, Forrest MJ.

J Pharmacol Toxicol Methods. 2007 Nov-Dec;56(3):308-16. Epub 2007 Jun 23.

PMID:
17643322
13.

Agonist lead identification for the high affinity niacin receptor GPR109a.

Gharbaoui T, Skinner PJ, Shin YJ, Averbuj C, Jung JK, Johnson BR, Duong T, Decaire M, Uy J, Cherrier MC, Webb PJ, Tamura SY, Zou N, Rodriguez N, Boatman PD, Sage CR, Lindstrom A, Xu J, Schrader TO, Smith BM, Chen R, Richman JG, Connolly DT, Colletti SL, Tata JR, Semple G.

Bioorg Med Chem Lett. 2007 Sep 1;17(17):4914-9. Epub 2007 Jun 10.

PMID:
17588745
14.

Acyl hydroxypyrazoles as novel agonists for high-affinity nicotinic acid receptor GPR109A: WO2008051403.

Shen HC.

Expert Opin Ther Pat. 2009 Aug;19(8):1149-55. doi: 10.1517/13543770902798061. Review.

PMID:
19566484
15.

Discovery of novel tricyclic full agonists for the G-protein-coupled niacin receptor 109A with minimized flushing in rats.

Shen HC, Ding FX, Deng Q, Wilsie LC, Krsmanovic ML, Taggart AK, Carballo-Jane E, Ren N, Cai TQ, Wu TJ, Wu KK, Cheng K, Chen Q, Wolff MS, Tong X, Holt TG, Waters MG, Hammond ML, Tata JR, Colletti SL.

J Med Chem. 2009 Apr 23;52(8):2587-602. doi: 10.1021/jm900151e.

PMID:
19309152
16.

Future of GPR109A agonists in the treatment of dyslipidaemia.

Wanders D, Judd RL.

Diabetes Obes Metab. 2011 Aug;13(8):685-91. doi: 10.1111/j.1463-1326.2011.01400.x. Review.

PMID:
21418500
17.

GPR109A (PUMA-G/HM74A) mediates nicotinic acid-induced flushing.

Benyó Z, Gille A, Kero J, Csiky M, Suchánková MC, Nüsing RM, Moers A, Pfeffer K, Offermanns S.

J Clin Invest. 2005 Dec;115(12):3634-40.

18.

Pyrazole derivatives as partial agonists for the nicotinic acid receptor.

van Herk T, Brussee J, van den Nieuwendijk AM, van der Klein PA, IJzerman AP, Stannek C, Burmeister A, Lorenzen A.

J Med Chem. 2003 Aug 28;46(18):3945-51.

PMID:
12930155
19.

1-Alkyl-benzotriazole-5-carboxylic acids are highly selective agonists of the human orphan G-protein-coupled receptor GPR109b.

Semple G, Skinner PJ, Cherrier MC, Webb PJ, Sage CR, Tamura SY, Chen R, Richman JG, Connolly DT.

J Med Chem. 2006 Feb 23;49(4):1227-30.

PMID:
16480258
20.

Nicotinic acid (niacin) receptor agonists: will they be useful therapeutic agents?

Kamanna VS, Kashyap ML.

Am J Cardiol. 2007 Dec 3;100(11 A):S53-61. Review.

PMID:
18047854
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