A-922500 is a potent, selective, and orally bioavailable DGAT-1 inhibitor. A-922500 confers weight loss and a reduction in liver triglycerides when dosed chronically in DIO mice and depletes serum triglycerides following a lipid challenge in a dose-dependent manner, thus, reproducing major phenotypical characteristics of DGAT-1(-/-) mice. A-922500 (0.03, 0.3 and 3 mg/kg, p.o.) dose-dependently attenuates the maximal postprandial rise in serum triglyceride concentrations. DGAT-1 inhibition by A-922500 can be a novel therapeutic approach to the treatment of hypertriglyceridemia in humans.

CB1-IN-1 is a peripas a peripherally restricted CB1R antagonist. It cause weight-loss in diet-induced obese mice.

Tetrahydro-4-Methylene-2-octyl-5-oxo-3-furancarboxylic acid or C75 is an inhibitor of fatty acid synthase. Additionally, C75 increased fatty acid oxidation and ATP levels by increasing carnitine palmitoyltransferase I (CPT I) activity. Unlike the activation produced by C75, the CoA derivative is a potent competitive inhibitor that binds tightly but reversibly to CPT I. C75 exerts antitumor and anti-obese potential. C75 has two enantiomers: (-)-C75 inhibits FAS activity in vitro and has a cytotoxic effect on tumor cell lines, without affecting food consumption, (+)-C75 inhibits CPT1 and its administration produces anorexia, suggesting that central inhibition of CPT1 is essential for the anorectic effect of C75.

CL-316243 is a selective and highly specific β3-adrenoceptor agonist. CL 316243 possesses anti-obesity and anti-diabetic effects due to increasing brown adipose tissue thermogenesis and metabolic rate, and consequently may be useful for treating obesity as well as non-insulin-dependent diabetes mellitus in obese persons, without causing excessive side effects.

Celastrol is a pentacyclic triterpenoid isolated from the root extracts of Tripterygium wilfordii, a perrennial creeping plant indigenous to large area in Southern China. Celastrol possess antioxidant and anti-inflammatory and anticancer action. In the mouse model of rheumatoid arthritis it reduced inflammatory swelling, suppressed humoral and skin response and reduced pathological progression of joint. Celastrol demonstrated efficacy in transgenic mouse model of amyotrophic lateral sclerosis. Anticancer activity of celastrol was shown in xenograft models of prostate cancer. Celastrol suppresses food intake, blocks reduction of energy expenditure, and leads to up to 45% weight loss in hyperleptinemic diet-induced obese (DIO) mice by increasing leptin sensitivity. Celastrol acts by interfering with the activity of Hsp90, IKK-beta and proteasome S26 subunit.

BIBO-3304 is a subtype selective nonpeptide antagonist with subnanomolar affinity for the Y1 receptor subtype that significantly inhibits food intake induced by application of NPY or by fasting. BIBO-3304 is a NPY Y1 receptor antagonist (IC50 values are 0.38 and 0.72 nM at human and rat receptors respectively) that displays > 2600-fold selectivity over Y2, Y4 and Y5 receptors.

CGP-71683A is a non-peptidic neuropeptide Y (NPY) Y5 receptor antagonist that was under development by Novartis. CGP-71683A is an extremely selective, non-peptide NPY Y5 receptor antagonist, displaying > 1000-fold selectivity over Y1, Y2 and Y4 receptors; IC50 values are 1.4, 2765, 7187 and 5637 nM at cloned rat Y5, Y1, Y2 and Y4 receptors respectively. CGP-71683A potently inhibits NPY-induced food intake following i.p. administration in diabetic, free-feeding and fasted rats.

L-Norpseudoephedrine is a psychostimulant drug of amphetamine family, first isolated from an Ephedra species. It is one of the two enantiomers of norpseudoephedrine, less potent that D-Norpseudoephedrine. L-Norpseudoephedrine is a norepinephrine and dopamine releasing agent, and has thermogenic and anorectic effect.

PSN632408 is an optimized agonist of GPR119 receptors. Systemic administration of PSN632408 suppresses food intake, reduces weight gain and white adipose tissue deposition in rats. PSN632408 treatment improved the function and/or mass of β-cells, significantly increased both human α- and β-cell areas in islet grafts and stimulated α- and β-cell replication. PSN632408 may be useful as a therapeutic agent for the treatment of obesity, diabetes and related metabolic disorders.

Evodiamine, a naturally occurring indole alkaloid, is one of the main bioactive ingredients of Evodia Rutaecara, the dried unripe fruit of which is also known as Wu zhu yu (Wu Zhu Yu, interchangeably) or Evodia Fruit. Evodia Fruit used in Traditional Chinese Medicine for the purposes of warmth, intestinal comfort (specifically; to alleviate abdominal pain, acid regurgitation, nausea and diarrhea), dysmenorrheal, and fighting inflammation and infections. With respect to the pharmacological actions of evodiamine, more attention has been paid to beneficial effects in insults involving cancer, obesity, nociception, inflammation, cardiovascular diseases, Alzheimer's disease, infectious diseases and thermo-regulative effects. Evodiamine has evolved a superior ability to bind various proteins including TRPV1, the aryl hydrocarbon receptor (AhR), and topoisomerases I and II. There are currently no human studies on evodia rutaecarpa berries or evodiamine.