PPARδ (delta) is the main target of a research chemical named GW501516. It has been shown that agonism of PPARδ changes the ... PPAR-alpha and PPAR-gamma are the molecular targets of a number of marketed drugs. The main classes of PPAR agonists are: An ... A fourth class of dual PPAR agonists, so-called glitazars, which bind to both the α and γ PPAR isoforms, are currently under ... A relatively recent avenue of drug research in treating depression and drug addiction is through PPARα and PPARγ activation. ...

PPAR-delta favours tumour angiogenesis. PPAR-delta is highly expressed in many tissues, including colon, small intestine, liver ... Peroxisome proliferator-activated receptor delta (PPAR-delta), or (PPAR-beta), also known as Nuclear hormone receptor 1 (NUC1) ... Both PPAR-delta and AMPK agonists are regarded as exercise mimetics. In adipose tissue PPAR-β/δ increases both oxidation as ... It and other PPAR-delta agonists are banned in sports. Peroxisome proliferator-activated receptor delta has been shown to ...

Barish GD, Narkar VA, Evans RM (March 2006). "PPAR delta: a dagger in the heart of the metabolic syndrome". The Journal of ... 1,000 fold selectivity over PPARα and PPARγ. In rats, binding of GW501516 to PPARδ recruits the coactivator PGC-1α. The PPARδ/ ... Billin AN (October 2008). "PPAR-beta/delta agonists for Type 2 diabetes and dyslipidemia: an adopted orphan still looking for a ... a PPAR delta agonist (PDF). 48th Annual Meeting of the Society of Toxicology. Baltimore: Society of Toxicology. p. 105. ...

... a PPAR delta agonist (PDF). 48th Annual Meeting of the Society of Toxicology. Baltimore: Society of Toxicology. p. 105. ... a PPAR delta agonist (PDF). 48th Annual Meeting of the Society of Toxicology. Baltimore: Society of Toxicology. p. 105. ... The PPAR modulator GW501516 has shown a positive effect on HDL-C and an antiatherogenic where LDL is an issue. However, ... "Effects of peroxisome proliferator-activated receptor alpha/delta agonists on HDL-cholesterol in vervet monkeys". J Lipid Res. ...

"PPAR-delta senses and orchestrates clearance of apoptotic cells to promote tolerance". Nature Medicine. 15 (11): 1266-72. doi: ...

November 2009). "PPAR-delta senses and orchestrates clearance of apoptotic cells to promote tolerance". Nature Medicine. 15 (11 ...

Metabolic modulators including peroxisome proliferator-activated receptor delta (PPARδ) agonists (e.g., GW 1516), PPARδ-AMP- ...

Seladelpar, a PPAR-delta receptor agonist, is being studied for treatment of PBC. Pruritus is a common symptom in people with ... Fibric acid derivatives, or fibrates, are agonists of the peroxisome proliferator activator receptor (PPAR), a nuclear receptor ... Among the fibrates, bezafibrate and fenofibrate, PPAR-alpha selective agonists, have been extensively studied as therapeutic ...

PPAR alpha and delta were found to upregulate PDK4 mRNA, but PPAR gamma activation downregulated expression. PDK4 is relevant ...

Billin AN (October 2008). "PPAR-beta/delta agonists for Type 2 diabetes and dyslipidemia: an adopted orphan still looking for a ... September 2011). "MBX-8025, a novel peroxisome proliferator receptor-delta agonist: lipid and other metabolic effects in ... is a PPARδ receptor agonist that is being investigated for drug use by Metabolex. According to a press release they are ... PPAR agonists, Trifluoromethyl compounds, Ethoxy compounds, Thioethers, All stub articles, Gastrointestinal system drug stubs) ...

Di Paola R, Esposito E, Mazzon E, Paterniti I, Galuppo M, Cuzzocrea S (August 2010). "GW0742, a selective PPAR-beta/delta ... It is mixed PPAR-B agonist antagonist depending on its dosage. It has weak activity on multiple nuclear receptors as well. It ... Niu HS, Ku PM, Niu CS, Cheng JT, Lee KS (2015). "Development of PPAR-agonist GW0742 as antidiabetic drug: study in animals". ... GW0742 (also known as GW610742) is a PPARδ/β agonist that has been investigated for drug use by GlaxoSmithKline. ...

"Roles of PPAR delta in lipid absorption and metabolism: a new target for the treatment of type 2 diabetes". Biochimica et ... April 2000). "The Pro12Ala polymorphism in PPAR gamma2 may confer resistance to type 2 diabetes". Biochemical and Biophysical ...

... has been reported to have various anti-inflammatory possibly via PPAR delta activation Nuciferine suppresses the ... "Nuciferine inhibits LPS-induced inflammatory response in BV2 cells by activating PPAR-γ". International Immunopharmacology. 63 ...

... possibly by dual PPAR-alpha/delta activation and increased mitochondrial fatty acid oxidation". Diabetes, Obesity & Metabolism ... TTA acts as a peroxisome proliferator-activated receptor alpha (PPARα) agonist and increases mitochondrial fatty acid oxidation ...

... 's activity at the peroxisome proliferator-activated receptor delta (PPAR-δ) receptor has prompted speculation ... Telmisartan activates PPAR-δ receptors in several tissues. Also, telmisartan has a PPAR-γ agonist activity.: 171 The substance ... PPAR-γ), a central regulator of insulin and glucose metabolism. It is believed that telmisartan's dual mode of action may ... "Angiotensin II receptor blocker telmisartan enhances running endurance of skeletal muscle through activation of the PPAR-δ/AMPK ...

Three subtypes of PPARs are known: PPAR-alpha, PPAR-delta, and PPAR-gamma. The protein encoded by this gene is PPAR-gamma and ... Two isoforms of PPARG are detected in the human and in the mouse: PPAR-γ1 (found in nearly all tissues except muscle) and PPAR- ... Ahmadian M, Suh JM, Hah N, Liddle C, Atkins AR, Downes M, Evans RM (May 2013). "PPARγ signaling and metabolism: the good, the ... miR3666 PPAR-gamma agonists have been used in the treatment of hyperlipidaemia and hyperglycemia. Many insulin sensitizing ...

... , in conjunction with PDK2 and PDK4, are primary targets of peroxisome proliferator-activated receptor delta/beta (PPAR ... beta/delta), with PDK3 having five elements that respond to these receptors. Model organisms have been used in the study of ... human pyruvate dehydrogenase kinase gene family are direct targets of the peroxisome proliferator-activated receptor beta/delta ... human pyruvate dehydrogenase kinase gene family are direct targets of the peroxisome proliferator-activated receptor beta/delta ...

PPARα, PPARδ). The function of PPARα is that it promotes bile acid excretion and lowers inflammation by acting on nuclear ... An important regulator in bile acid homeostasis is the alpha and delta isoforms of the peroxisome proliferator-activated ...

Together with peroxisome proliferator-activated receptor delta and peroxisome proliferator-activated receptor gamma, PPAR-alpha ... by PPAR-α. PPAR-α also inhibits glycolysis, while promoting liver gluconeogenesis and glycogen synthesis. In macrophages, PPAR- ... PPAR-α is a transcription factor regulated by free fatty acids, and is a major regulator of lipid metabolism in the liver. PPAR ... PPAR-α, agonists may carry therapeutic value for the treatment of non-alcoholic fatty liver disease. PPAR-alpha may also be a ...

This PG directly binds with and activates PPARγ thereby inducing the transcription of genes containing the PPARγ response ... Forman BM, Tontonoz P, Chen J, Brun RP, Spiegelman BM, Evans RM (1995). "15-Deoxy-delta 12, 14-prostaglandin J2 is a ligand for ... PGD2, PGJ2, Δ12-PGJ2, and 15-deoxy-Δ12,14-PGJ2 activate the transcription factor, PPARγ, with 15-deoxy-Δ12,14-PGJ2 being the ... Oliva JL, Pérez-Sala D, Castrillo A, Martínez N, Cañada FJ, Boscá L, Rojas JM (2003). "The cyclopentenone 15-deoxy-delta 12,14- ...

It lacks affinity for cannabinoid receptors, but acts as an agonist at both TRPV1 and PPARγ. Cannabichromene Cannabicitran ... Cannabicyclol Cannabielsoin Cannabigerol Cannabinodiol Cannabitriol Delta-6-CBD Taglialatela-Scafati O, Pagani A, Scala F, De ... as a Novel PPARγ Agonist via a Combined Computational and Functional Study". Molecules (Basel, Switzerland). 25 (5): 1119. doi: ...

The best-known PPAR ligands are the thiazolidinediones. After PPARδ (delta) was identified in humans in 1992, it turned out to ... PPARα and PPARγ are the molecular targets of a number of marketed drugs. For instance the hypolipidemic fibrates activate PPARα ... The three main forms of PPAR are transcribed from different genes: PPARα - chromosome 22q12-13.1 (OMIM 170998) PPARβ/δ - ... beta/delta, and gamma. In addition, PPARγ was reported to be involved in cancer pathogenesis and growth. PPARγ activation by ...

... is a phenyloxyacetate PPARδ receptor agonist. It is less potent and PPARδ selective than GW 501516. GW 501516 GFT505 ... March 2007). "Neuroprotective efficacy of the peroxisome proliferator-activated receptor delta-selective agonists in vitro and ... PPAR agonists, All stub articles, Pharmacology stubs). ...

2008). "PPAR and LXR activators regulate ABCA12 expression in human keratinocytes". J. Invest. Dermatol. 128 (1): 104-9. doi: ... 2009). "Ceramide stimulates ABCA12 expression via peroxisome proliferator-activated receptor {delta} in human keratinocytes". J ...

Additionally, Delta-9-Tetrahydrocannabinol (THC) is a partial agonist at both the CB1 and CB2 receptors, with the former being ... a non-adipogenic PPARγ agonist from nature". Biochimica et Biophysica Acta (BBA) - General Subjects. 1830 (10): 4813-9. doi: ... Delta 9-tetrahydrocannabivarin (THCV) is a partial agonist at CB2 receptors and this activity might be implicated in ∆9-THCV- ...

... is also an agonist of the PPARα and PPARγ nuclear receptors. WIN 55,212-2 reduces voluntary wheel running in ... Shmist YA, Goncharov I, Eichler M, Shneyvays V, Isaac A, Vogel Z, Shainberg A (February 2006). "Delta-9-tetrahydrocannabinol ... O'Sullivan SE (June 2016). "An update on PPAR activation by cannabinoids". British Journal of Pharmacology. 173 (12): 1899-1910 ... cannabimimetic activity of a class of compounds structurally distinct from delta 9-tetrahydrocannabinol". The Journal of ...

Rogawski MA, Bazil CW (July 2008). "New molecular targets for antiepileptic drugs: alpha(2)delta, SV2A, and K(v)7/KCNQ/M ... 2013). "Antiepileptic action of N-palmitoylethanolamine through CB1 and PPAR-α receptor activation in a genetic model of ... Lampen A, Carlberg C, Nau H (2001). "Peroxisome proliferator-activated receptor delta is a specific sensor for teratogenic ... 2013). Charpier S (ed.). "PPAR-alpha agonists as novel antiepileptic drugs: preclinical findings". PLOS ONE. 8 (5): e64541. ...

Alternatively, overexpressing miR-382 resulted in attenuated drinking and the inhibition of DRD1 and delta fosB upregulation in ... and 222 significantly inhibited adipogenesis and repressed induction of the master regulators PPARγ and CCAAT/enhancer-binding ... and its overexpression results in the upregulation of DRD1 and delta fosB, a transcription factor that activates a series of ...

The pharmacological effects of CBD may involve PPARγ agonism, inhibition of voltage-gated cation channels, and intracellular ... Nabiximols (brand name Sativex), an oromucosal spray made of a complex botanical mixture containing cannabidiol (CBD), delta-9- ... Cannabidiol, in an oral-mucosal spray formulation combined with delta-9-tetrahydrocannabinol, is a product available by ... with a delta-9 tetrahydrocannabinol concentration of not more than 0.3 percent on a dry weight basis," including CBD, from the ...

THCA binds to and activates PPARγ with higher potency than its decarboxylated products. THCA shows a similar metabolism to THC ... Rosenqvist E, Ottersen T (1975). "The crystal and molecular structure of delta-9-tetrahydrocannabinolic acid b". Acta Chemica ... December 2017). "Tetrahydrocannabinolic acid is a potent PPARγ agonist with neuroprotective activity". British Journal of ... "7 CFR § 990.25 - Standards of performance for detecting total delta-9 tetrahydrocannabinol (THC) concentration levels". LII / ...