The isomer of fucosterol, isofucosterol, has been identified as a minor constituent of marine sponge, Gynostemma pentafillum, oat seeds and a few other plants. Isofucosterol of marine sponge is believed to be the biosynthetic precursors of the antiviral orthoesterols and weinbersterols found in the same sponge. Isofucosterol exhibits lipase inhibitory effect, suggesting that it has potential as anti-obesity agent.

Sazetidine-A (6-[5-(azetidin-2-ylmethoxy)pyridin-3-yl]hex-5-yn-1-ol or AMOP-H-OH) is a "silent desensitizer" of neuronal nicotinic acetylcholine receptors (nAChRs), meaning that it desensitizes the receptor without first activating it. Later it was shown that Sazetidine-A is an agonist of native and recombinant alpha4beta2 nAChRs but shows differential efficacy on alpha4beta2 nAChRs subtypes. In animal models it is able to regulate the gain in body weight, alcohol and nicotine dependence. Sazetidine-A exerts analgesic, antidepressant and anxiolytic properties.

Sazetidine-A (6-[5-(azetidin-2-ylmethoxy)pyridin-3-yl]hex-5-yn-1-ol or AMOP-H-OH) is a "silent desensitizer" of neuronal nicotinic acetylcholine receptors (nAChRs), meaning that it desensitizes the receptor without first activating it. Later it was shown that Sazetidine-A is an agonist of native and recombinant alpha4beta2 nAChRs but shows differential efficacy on alpha4beta2 nAChRs subtypes. In animal models it is able to regulate the gain in body weight, alcohol and nicotine dependence. Sazetidine-A exerts analgesic, antidepressant and anxiolytic properties.

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.

(+)-DDMS (R-Didesmethylsibutramine , (R)-DDMS) is one of sibutramine active metabolites. Sibutramine is widely used in the treatment of obesity. Sibutramine acts by inhibiting the reuptake of serotonin and noradrenaline in synapses, thereby enhancing both satiety and energy expenditure. In preclinical models (R)-enantiomer of Didesmethylsibutramine was clearly more potent than the (S)-enantiomers and (R)-didesmethylsibutramine shows some activity in all tests. (S)-didesmethylsibutramine affected locomotor behavior and the Porsolt test but appeared to be completely inactive on food intake. R-Didesmethylsibutramine is more potent than sibutramine in depressing food intake and decreasing body weight, suggest that these enantioselective metabolites might be safer and more effective than sibutramine as potential therapies for obesity.

Imetit (S-[2-(4-(imidazolyl)ethyl]isothiourea) is a highly specific and potent histamine H3 receptor agonist. It is widely used to study H3-mediated signaling.

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.

The isomer of fucosterol, isofucosterol, has been identified as a minor constituent of marine sponge, Gynostemma pentafillum, oat seeds and a few other plants. Isofucosterol of marine sponge is believed to be the biosynthetic precursors of the antiviral orthoesterols and weinbersterols found in the same sponge. Isofucosterol exhibits lipase inhibitory effect, suggesting that it has potential as anti-obesity agent.

2-methyl-4,6-dinitrophenol (4,6-Dinitro-ortho-cresol, DNOC) is a yellow crystalline solid. DNOC is used agriculturally as a larvicide, ovicide and insecticide (against locusts and other insects) as well as a potato haulm desiccant. It is also used as a polymerization inhibitor and as an intermediate in the chemical industry. For agricultural uses, DNOC is mainly formulated as emulsifiable concentrate, either aqueous or oily. 4,6-Dinitro-o-cresol is an uncoupler of the mitochondrial respiratory system. It causes an increase in basal metabolic rate with raised temperature and weight loss in man and animals. After metabolic activation, 4,6-dinitro-o-cresol has mutagenic potential in vitro. In vivo, evidence of clastogenic effects was obtained with a herbicide containing 4,6-dinitro-o-cresol but not with the pure substance. A long-term study with rats yielded no evidence of carcinogenic effects. During the 1930s, DNOC, along with dinitrophenol, was used therapeutically as a weight-loss agent after animal experiments had demonstrated that dinitrophenols increased the basal metabolic rate (BMR). The earliest mention of the use of these compounds for weight loss is a publication by Cutting and Tainter (1933) in which the authors reported clinical studies of dinitrophenol for this purpose. Dodds and Robertson (1933) reported that the related compound, DNOC, exhibited a greater effect on metabolism than dinitrophenol, leading to the marketing of DNOC for weight loss. Following the publication of these reports, dinitrophenol, and to a lesser extent, DNOC, began selling in drug stores and was prescribed by physicians for weight loss. DNOC acts mainly as an inhibitor of oxidative phosphorylation at the mitochondrial level, inducing a significant increase in basal metabolism and hyperthermy. The oxidation of carbohydrate forms the main source of energy of the body and the energy is “stored” in the form of compounds containing phosphate (high energy phosphate bonds of adenosine triphosphate or ATP). This compound is then a source of energy to the body. DNOC inhibits the formation of ATP. In the presence of DNOC the oxidative process continues and is even increased, but the energy cannot be converted to a useable form and it is therefore dissipated as heat. In muscle ATP cannot be re-synthesized and is progressively broken down to adenylic acid. The shortage of ATP may lead to muscular paralysis which for critical organs, such as heart and respiratory muscles, includes a blocking of their vital functions and in the case of death by DNOC poisoning, to early rigor mortis.