CP-809101 is a potent, functionally selective 5-HT(2C) agonist that displays approximately 100% efficacy in vitro. CP-809101 has a pharmacological profile similar to that of the atypical antipsychotics with low extrapyramidal symptom liability. CP-809101 was active in novel object recognition, an animal model of cognitive function. It had promising results in animal models of obesity and psychosis.

Epibatidine is a piperidine alkaloid that is secreted by the Ecuadoran frog Epipedobates anthonyi. Many laboratories began to synthesize epibatidine and after studying it, scientists realized it was too toxic to be used as a pain-relieving drug. Epibatine is the exo-isomer of the two possible geometric isomers and can exist as two enantiomers (+) – or R- Epibatidine and (-) or S- Epibatidine. The natural compound is the (+) isomer, although there is a little difference in pharmacological activity between (+) and (-) isomers. Epibatidine binds to nicotinic acetylcholine receptors (nAChR) rather than opiate receptors, which is common of most analgesics such as morphine. Epibatidine and both its isomers are extremely potent full agonists for neuronal acetylcholine receptors: alpha4/beta2 and alpha3/beta2. Epibatidine binds not only to nAChR in the brain but also at other neuro-muscular junctions throughout the body. This is not desired as it caused seizures and respiratory and digestive problems. Currently only rudimentary research into epibatidine's effects has been performed.

S-14506 was originally identified and developed in France by Scientists at the Institut de Recherches Servier. S-14506 showed potent binding and antagonistic activity against the 5HT1-A receptor. It was found to work synergistically with D2 receptor antagonists and was therefore studied in animal models for depression, psychosis, and anxiety. A tritium labeled version was also studied as a potential 5HT1-A receptor PET imaging agent.

WIN 55212-2 is the synthetic cannabimimetic compound. It is a potent aminoalkylindole cannabinoid receptor agonist. WIN 55,212-2 increases expression of anti-oxidant Cu/Zn SOD and is able to prevent inflammation induced by Aβ1-42 in cultured astrocytes. It exerts neuroprotective and anti-inflammatory actions against Aβ damage through both CB₁ and CB₂ receptors. WIN 55212-2 attenuates hyperalgesia and allodynia in a rat model of neuropathic pain. In the clinical trial, it was revealed that WIN 55212-2, applied topically, decreases the intraocular pressure of human glaucoma resistant to conventional therapies within the first 30 min.

SR 59230A is orally active, selective antagonist of the beta-3 adrenergic receptor, SR 59230A has high affinity for the β3 adrenoceptors occurring in human gut that affect the function of human colonic circular smooth muscle.

LY344864 is a selective 5-HT1F receptor agonist (EC50 = 3 nM). In a rat model of migraine, LY344864 inhibited neurogenic dural inflammation following i.v. and oral administration.