MK-5046 is an orally active, potent, selective agonist of the orphan G protein-coupled receptor bombesin receptor subtype-3 (BRS-3). In pharmacological testing using diet-induced obese mice, MK-5046 caused mechanism-based, dose-dependent reductions in food intake and body weight.

25CN-NBOH (or NBOH-2C-CN) is a compound indirectly derived from the phenethylamine series of hallucinogens, which was discovered in 2011 by Martin Hansen at the University of Copenhagen. This compound is notable as one of the most selective agonist ligands for the 5-HT2A receptor yet discovered, with a pKi of 8.88 at the human 5-HT2A receptor and with 100x selectivity for 5-HT2A over 5-HT2C, and 46x selectivity for 5-HT2A over 5-HT2B

Japanese scientists discovered AdipoRon during screening of a compound library. This drug is a selective agonist of adiponectin receptors 1 and 2, which activates 5′-adenosine monophosphate–activated protein kinase (AMPK) in cultured mammalian cells, an enzyme that is involved in many metabolic processes including the release of insulin, inhibition of lipid synthesis, and stimulation of glucose uptake. It was found, that after oral administration in mice AdipoRon effectively attenuated post-ischemic cardiac injury, thus could be a promising novel therapeutic approach treating cardiovascular complications caused by obesity-related disorders such as type 2 diabetes. In addition, recently investigation showed that AdipoRon has antiproliferative effects of adiponectin and may suppress the colorectal cancer cell growth.

(-)-∆8-Tetrahydrocannabinol (∆8-THC) has a very similar pharmacologic profile as (-)-∆9-tetrahydrocannabinol (∆9-THC), the most active constituent of cannabis. Delta-8-tetrahydrocannabinol (THC) has activity in man similar to that of its double-bond isomer, delta-9-THC. The spatial orientation of the side chain seems to play a pivotal role in cannabinergic activity. Introduction of a triple bond in the benzylic position of the n-heptyl-D8-THC analogue led to the classical cannabinoid AMG-1 with high CB1 and moderate CB2 affinity. AMG-1 is an analgesic drug which is a cannabinoid agonist.

PF-04479745 (PF-4479745) is a selective serotonin 5HT2C agonist. PF-4479745 displayed robust pharmacology in a preclinical canine model of stress urinary incontinence (SUI) and no measurable functional agonism at the key selectivity targets 5-HT2A and 5-HT2B in relevant tissue-based assay systems.

WAY 267464 dihydrochloride is a potent and selective agonist at the oxytocin receptor (OTR). WAY 267464 has been shown to cross the blood-brain-barrier to a significantly greater extent than exogenously applied oxytocin. WAY 267464 dose-dependently reduced anxiety on the four-plate test and prevented the deficits in prepulse inhibition induced by MK-801 or amphetamine. The ability of WAY 267464 to function as a V1AR antagonist may limit its potential therapeutic use in humans, as it would conceivably prevent the improvements in social behavior and social cognition that may be assumed to arise from a primary OTR agonist action.