T.D. Spies The use of nicotinic acid in the treatment of pellagra JAMA 110 1938 622 627
R. Altschul Influence of nicotinic acid on serum cholesterol in man Arch. Biochem. 54 1955 558 559
L.A. Carlson Studies on the effect of nicotinic acid on catecholamine stimulated lipolysis in adipose tissue in vitro Acta Med. Scand. 173 1963 719 722
L.A. Carlson Nicotinic acid: the broad-spectrum lipid drug. A 50th anniversary review J. Intern. Med. 258 2005 94 114 (Pubitemid 41025967)
P.L. Canner Fifteen year mortality in Coronary Drug Project patients: long-term benefit with niacin J. Am. Coll. Cardiol. 8 1986 1245 1255 (Pubitemid 17208898)
Anonymous Clofibrate and niacin in coronary heart disease JAMA 231 1975 360 381
A. Gille Nicotinic acid: pharmacological effects and mechanisms of action Annu. Rev. Pharmacol. Toxicol. 48 2008 79 106 (Pubitemid 351738150)
V.S. Kamanna The mechanism and mitigation of niacin-induced flushing Int. J. Clin. Pract. 63 2009 1369 1377
M.J. Chapman Niacin and fibrates in atherogenic dyslipidemia: pharmacotherapy to reduce cardiovascular risk Pharmacol. Ther. 126 2010 314 345
S. Offermanns International Union of Basic and Clinical Pharmacology. LXXXII: nomenclature and classification of hydroxy-carboxylic acid receptors (GPR81, GPR109A, and GPR109B) Pharmacol. Rev. 63 2011 269 290
V.S. Kamanna Niacin: an old drug rejuvenated Curr. Atheroscler. Rep. 11 2009 45 51
B.J. Wu Evidence that niacin inhibits acute vascular inflammation and improves endothelial dysfunction independent of changes in plasma lipids Arterioscler. Thromb. Vasc. Biol. 30 2010 968 975
M. Lukasova Nicotinic acid inhibits progression of atherosclerosis in mice through its receptor GPR109A expressed by immune cells J. Clin. Invest. 121 2011 1163 1173
H. Tang The psoriasis drug monomethylfumarate is a potent nicotinic acid receptor agonist Biochem. Biophys. Res. Commun. 375 2008 562 565
S. Tunaru PUMA-G and HM74 are receptors for nicotinic acid and mediate its anti-lipolytic effect Nat. Med. 9 2003 352 355 (Pubitemid 36362793)
W. Wang Effect of nicotinic acid administration on hepatic very low density lipoprotein-triglyceride production Am. J. Physiol. Endocrinol. Metab. 280 2001 E540 E547
S. Lamon-Fava Extended-release niacin alters the metabolism of plasma apolipoprotein (Apo) A-I and ApoB-containing lipoproteins Arterioscler. Thromb. Vasc. Biol. 28 2008 1672 1678
C. Hernandez Regulation of hepatic ApoC3 expression by PGC-1β mediates hypolipidemic effect of nicotinic acid Cell Metab. 12 2010 411 419
J. Shepherd Effects of nicotinic acid therapy on plasma high density lipoprotein subfraction distribution and composition and on apolipoprotein A metabolism J. Clin. Invest. 63 1979 858 867 (Pubitemid 9182535)
C.B. Blum High density lipoprotein metabolism in man J. Clin. Invest. 60 1977 795 807 (Pubitemid 8208471)
T.R. Joy, and R.A. Hegele Microsomal triglyceride transfer protein inhibition-friend or foe? Nat. Clin. Pract. Cardiovasc. Med. 5 2008 506 508
M. Hernandez Critical role of cholesterol ester transfer protein in nicotinic acid-mediated HDL elevation in mice Biochem. Biophys. Res. Commun. 355 2007 1075 1080 (Pubitemid 46389506)
J.W. van der Hoorn Niacin increases HDL by reducing hepatic expression and plasma levels of cholesteryl ester transfer protein in APOE*3Leiden. CETP mice Arterioscler. Thromb. Vasc. Biol. 28 2008 2016 2022
E. Lai Abstract 190: A niacin receptor partial agonist, MK-0354, robustly reduces plasma free fatty acids and produces little flushing but fails to alter LDL-C, HDL-C, and triglycerides in humans Circulation 116 2007 II-16
M. Briel Association between change in high density lipoprotein cholesterol and cardiovascular disease morbidity and mortality: systematic review and meta-regression analysis BMJ 338 2009 b92
A.G. Olsson Is high HDL cholesterol always good? Ann. Med. 41 2009 11 18
S.J. Nicholls HDL: still a target for new therapies? Curr. Opin. Investig. Drugs 9 2008 950 956
A.V. Khera Cholesterol efflux capacity, high-density lipoprotein function, and atherosclerosis N. Engl. J. Med. 364 2011 127 135
L. Yvan-Charvet Cholesterol efflux potential and anti-inflammatory properties of high-density lipoprotein after treatment with niacin or anacetrapib Arterioscler. Thromb. Vasc. Biol. 30 2010 1430 1438
S.A. Sorrentino Endothelial-vasoprotective effects of high-density lipoprotein are impaired in patients with type 2 diabetes mellitus but are improved after extended-release niacin therapy Circulation 121 2010 110 122
E. Holzhauser Nicotinic acid has anti-atherogenic and anti-inflammatory properties on advanced atherosclerotic lesions independent of its lipid-modifying capabilities J. Cardiovasc. Pharmacol. 57 2011 447 454
S.H. Ganji Niacin inhibits vascular oxidative stress, redox-sensitive genes, and monocyte adhesion to human aortic endothelial cells Atherosclerosis 202 2009 68 75
S. Tavintharan Effects of niacin on cell adhesion and early atherogenesis: biochemical and functional findings in endothelial cells Basic Clin. Pharmacol. Toxicol. 104 2009 206 210
H.J. Knowles Niacin induces PPARγ expression and transcriptional activation in macrophages via HM74 and HM74a-mediated induction of prostaglandin synthesis pathways Biochem. Pharmacol. 71 2006 646 656 (Pubitemid 43121998)
T. Rubic Stimulation of CD36 and the key effector of reverse cholesterol transport ATP-binding cassette A1 in monocytoid cells by niacin Biochem. Pharmacol. 67 2004 411 419 (Pubitemid 38236129)
L. Yvan-Charvet Role of HDL, ABCA1, and ABCG1 transporters in cholesterol efflux and immune responses Arterioscler. Thromb. Vasc. Biol. 30 2010 139 143
B. Gustafson Adipose tissue, inflammation and atherosclerosis J. Atheroscler. Thromb. 17 2010 332 341
E.P. Plaisance Niacin stimulates adiponectin secretion through the GPR109A receptor Am. J. Physiol. Endocrinol. Metab. 296 2009 E549 E558
S. Westphal, and C. Luley Preferential increase in high-molecular weight adiponectin after niacin Atherosclerosis 198 2008 179 183 (Pubitemid 351406367)
J.E. Digby Anti-inflammatory effects of nicotinic acid in adipocytes demonstrated by suppression of fractalkine, RANTES, and MCP-1 and upregulation of adiponectin Atherosclerosis 209 2010 89 95
J.D. Morrow Identification of skin as a major site of prostaglandin D2 release following oral administration of niacin in humans J. Invest. Dermatol. 98 1992 812 815
Z. Benyo GPR109A (PUMA-G/HM74A) mediates nicotinic acid-induced flushing J. Clin. Invest. 115 2005 3634 3640 (Pubitemid 43121852)
Z. Benyó Nicotinic acid-induced flushing is mediated by activation of epidermal Langerhans cells Mol. Pharmacol. 70 2006 1844 1849 (Pubitemid 44771899)
D. Maciejewski-Lenoir Langerhans cells release prostaglandin D2 in response to nicotinic acid J. Invest. Dermatol. 126 2006 2637 2646
J. Hanson Nicotinic acid- and monomethyl fumarate-induced flushing involves GPR109A expressed by keratinocytes and COX-2-dependent prostanoid formation in mice J. Clin. Invest. 120 2010 2910 2919
K. Cheng Antagonism of the prostaglandin D2 receptor 1 suppresses nicotinic acid-induced vasodilation in mice and humans Proc. Natl. Acad. Sci. U.S.A. 103 2006 6682 6687
E.T. Bodor, and S. Offermanns Nicotinic acid: an old drug with a promising future Br. J. Pharmacol. 153 Suppl. 1 2008 S68 S75
R.B. Goldberg, and T.A. Jacobson Effects of niacin on glucose control in patients with dyslipidemia Mayo Clin. Proc. 83 2008 470 478 (Pubitemid 351536472)
T.A. Dalton, and R.S. Berry Hepatotoxicity associated with sustained-release niacin Am. J. Med. 93 1992 102 104
B.G. Brown Simvastatin and niacin, antioxidant vitamins, or the combination for the prevention of coronary disease N. Engl. J. Med. 345 2001 1583 1592 (Pubitemid 33126837)
A.J. Taylor Extended-release niacin or ezetimibe and carotid intima-media thickness N. Engl. J. Med. 361 2009 2113 2122
A.J. Taylor The effect of 24 months of combination statin and extended-release niacin on carotid intima-media thickness: ARBITER 3 Curr. Med. Res. Opin. 22 2006 2243 2250 (Pubitemid 44789989)
National Institutes of Health, (2011) NIH stops clinical trial on combination cholesterol treatment. NIH News May 16, 2011 (http://public.nhlbi. nih.gov/newsroom/home/GetPressRelease.aspx?id=2792)
Armitage, J. et al. (2007) Treatment of HDL to Reduce the Incidence of Vascular Events HPS2-THRIVE July 19, 2010 (http://clinicaltrials.gov/ct2/show/ NCT00461630?term=hps2-thrive&rank=1)
M.H. Davidson Niacin use and cutaneous flushing: mechanisms and strategies for prevention Am. J. Cardiol. 101 2008 14B 19B
H. Oberwittler, and M. Baccara-Dinet Clinical evidence for use of acetyl salicylic acid in control of flushing related to nicotinic acid treatment Int. J. Clin. Pract. 60 2006 707 715 (Pubitemid 43811652)
J.F. Paolini Effects of laropiprant on nicotinic acid-induced flushing in patients with dyslipidemia Am. J. Cardiol. 101 2008 625 630
R.W. Walters β-Arrestin1 mediates nicotinic acid-induced flushing, but not its antilipolytic effect, in mice J. Clin. Invest. 119 2009 1312 1321
G. Semple 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 J. Med. Chem. 51 2008 5101 5108
J. Zhang Niaspan treatment improves neurological functional recovery in experimental autoimmune encephalomyelitis mice Neurobiol. Dis. 32 2008 273 280
S. Schilling Fumaric acid esters are effective in chronic experimental autoimmune encephalomyelitis and suppress macrophage infiltration Clin. Exp. Immunol. 145 2006 101 107 (Pubitemid 43893938)
L. Kappos Efficacy and safety of oral fumarate in patients with relapsing-remitting multiple sclerosis: a multicentre, randomised, double-blind, placebo-controlled phase IIb study Lancet 372 2008 1463 1472
A. Papadopoulou Dimethyl fumarate for multiple sclerosis Expert Opin. Investig. Drugs 19 2010 1603 1612
Anonymous Trial watch: Phase III success for Biogen's oral multiple sclerosis therapy Nat. Rev. Drug Discov. 10 2011 404
A. Shehadah Niaspan treatment induces neuroprotection after stroke Neurobiol. Dis. 40 2010 277 283
W.Y. Kwon Niacin attenuates lung inflammation and improves survival during sepsis by downregulating the nuclear factor-κB pathway Crit. Care Med. 39 2011 328 334
K.H. Cho Niacin ameliorates oxidative stress, inflammation, proteinuria, and hypertension in rats with chronic renal failure Am. J. Physiol. Renal Physiol. 297 2009 F106 F113
V.A. Mitrofanov Inflammatory degeneration of joint tissue in adjuvant arthritis after intraarticular treatment with the mixture of silver drug and nicotinic acid Bull. Exp. Biol. Med. 140 2005 702 704 (Pubitemid 43362052)
M. Rostami Yazdi, and U. Mrowietz Fumaric acid esters Clin. Dermatol. 26 2008 522 526
T. Soga Molecular identification of nicotinic acid receptor Biochem. Biophys. Res. Commun. 303 2003 364 369 (Pubitemid 36338250)
A. Wise Molecular identification of high and low affinity receptors for nicotinic acid J. Biol. Chem. 278 2003 9869 9874 (Pubitemid 36800490)
S. Tunaru Characterization of determinants of ligand binding to the nicotinic acid receptor GPR109A (HM74A/PUMA-G) Mol. Pharmacol. 68 2005 1271 1280 (Pubitemid 41539983)
G. Kostylina Neutrophil apoptosis mediated by nicotinic acid receptors (GPR109A) Cell Death Differ. 15 2008 134 142 (Pubitemid 350286181)
A. Schaub PUMA-G, an IFN-γ-inducible gene in macrophages is a novel member of the seven transmembrane spanning receptor superfamily Eur. J. Immunol. 31 2001 3714 3725 (Pubitemid 34030985)
N. Singh Blockade of dendritic cell development by bacterial fermentation products butyrate and propionate through a transporter (Slc5a8)-dependent inhibition of histone deacetylases J. Biol. Chem. 285 2010 27601 27608
P.M. Martin Expression and localization of GPR109A (PUMA-G/HM74A) mRNA and protein in mammalian retinal pigment epithelium Mol. Vis. 15 2009 362 372
