LY-165163 is a partial agonist of serotonin receptors 5-HT1A and 5-HT1D. It exhibits marked activity at both pre- and postsynaptic dopaminergic D2 (D3 and D1) receptors. LY-165163 caused a significant and dose-dependent hypothermia in rats. As a 5-HT1D receptor agonist, LY-165163 was proposed for the ocular pain treatment.

B-HT 958 (2-amino-6-(p-chlorobenzyl)-4H-5,6,7,8-tetrahydrothiazolo[5,4-d]az epine), a compound chemically related to clonidine-like drugs of the azepine type, exerts a strong agonistic effect on brain dopamine autoreceptors. B-HT 958 is a partial agonist at peripheral alpha 2-adrenoceptors. In doses of about 1 mg/kg and with low frequency sympathetic stimulation (less than 6.4 Hz) it acts presynaptically as agonist; in this dose the drug acts postsynaptically mainly as antagonist.

Trifluoromethylphenylpiperazine (TFMPP) acts on serotonin receptors 5-HT1A, 5-HT1B, 5-HT1D, 5-HT2A and 5-HT2C and functions as a full agonist at all sites except the 5-HT2A receptor, where it acts as a weak partial agonist or antagonist. In addition, TFMPP binds to the sodium-dependent serotonin transporter, SERT and evokes the release of serotonin. Besides was shown, that the N-Benzylpiperazine/TFMPP combination produced effects, which crudely mimic those of MDMA, commonly known as ecstasy. The neurophysiological effects of TFMPP in humans was also studied and was shown that TFMPP may affect transmitter systems involved in speeding of interhemispheric communication in the male brain.

4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone or nicotine-derived nitrosamine ketone (NNK) is a tobacco-specific nitrosamine. NNK is considered to be a carcinogen. NNK induces deleterious mutations in oncogenes and tumor suppression genes by forming DNA adducts, which could be considered as tumor initiation. Meanwhile, the binding of NNK to the nicotinic acetylcholine receptor promotes tumor growth by enhancing and deregulating cell proliferation, survival, migration, and invasion, thereby creating a microenvironment for tumor growth.

CGS-20625 is a potent and selective ligand for the central benzodiazepine receptor. It acts as a partial agonist of GABAA channel in vitro and produces anxiolytic and anticonvulsant effects in vivo. The drug has low bioavailability so its clinical applications are limited, and it is mainly used as a tool compound.

Catharanthine is a terpene indole alkaloid produced by the medicinal plant Catharanthus roseus. Catharanthine is derived from strictosidine, but the exact mechanism by which this happens is currently unknown. Catharanthine is one of the two precursors that form vinblastine, the other being vindoline.

L-822179 is a triazolophthalazine that selectively attenuates the effects of GABA at GABA(A) receptors containing an alpha5 subunit. It is an orally active, functionally selective compound, which enhances cognition in animals without anxiogenic or convulsant effects. The dose-limiting adverse event of L-822179 is dizziness and/or light-headedness. L-822179 does not improve cognitive performance in the elderly; indeed the dose of 4 mg actually significantly impairs performance. In this regard, it could therefore be considered that this study is a failed trial in so far as the positive control, lorazepam, does not show the anticipated effect.