GRI977143, a prototypic nonlipid agonist specific to the lysophosphatidic acid-2 LPA(2) receptor subtype, displays antiapoptotic activity and activates the ERK1/2 prosurvival pathway.

SL651498 was identified as a drug development candidate from a research program designed to discover subtype-selective GABA(A) receptor agonists for the treatment of generalized anxiety disorder and muscle spasms. SL651498 displayed high affinity for GABA(A) receptors containing alpha(1) and alpha(2 subunits, and weaker affinity for alpha5-containing GABA(A) receptors, it behaved as a full agonist at recombinant t GABA(A) receptors containing alpha(2) and alpha(3) subunits, and as a partial agonist at recombinant GABA(A) receptors expressing alpha(1) and alpha(5) subunits. It was shown, that SL651498 represented a promising alternative to agents currently used for the treatment of anxiety disorders and muscle spasms without the major side effects seen with classical benzodiazepines).

AH-7921 (3,4-Dichloro-N-([1-(dimethylamino)cyclohexyl] methyl)benzamide) is an N-substituted cyclohexylmethylbenzamide classified as an opioid analgesic with high addictive liability. The compound acts as an agonist of μ-opioid receptors, although at high doses it can also stimulate κ-opioid receptors. In animal studies, AH-7921 produced typical morphine-like actions, i.e., antinociception, respiratory depression, sedation, miosis, inhibition of gut propulsion, and lowered body temperature, with a potency almost equipotent to that of morphine. There is limited information available on the routes of administration and the doses of AH-7921 used. The compound is taken orally, nasally, by smoking, and, less commonly, by intravenous injection. Minimal oral effective doses for complete pain suppression by AH 7921 are 1.25 and 13.8 mg/kg for canine and rhesus monkey, respectively.

D-propylhexedrine is an optical isomer of propylhexedrine, a vasoconstrictor stimulating α-adrenergic receptors of the sympathetic nervous system. D-propylhexedrine is proposed to be less potent isomer, it is is less pressor and less excitatory on the central nervous system than is the L-isomer.

Purmorphamine is agonist of the protein Smoothened, a key part of the hedgehog signaling pathway, which is involved in bone growth and brain development as well as having a number of other functions in the body. Purmorphamine induces osteogenesis in multipotent mesenchymal progenitor cells. It demonstated neuroprotective action in mouse model of brain ischemia and cytoprotective effect in cellular model of amyotrophic lateral sclerosis.

J 113863 is a potent and high selective CKR-1 (CCR1) and CKR-3 (CCR3) chemokine receptor antagonist, which is also behaved as a full agonist of CCR2 and as a very partial agonist of CCR5. This compound was investigated for the treatment of multiple sclerosis and rheumatoid arthritis, but the status of these studies are not known.

PHA-543613 was discovered by Pfizer and has been under development primarily as a potential treatment of schizophrenia. PHA-543613 acts as an agonist to the Neuronal acetylcholine receptor protein alpha-7 subunit. A single human trial was conducted in healthy human volunteers, but the compound has been studied extensively in rat models for schizophrenia as well as Parkinson's disease and Alzheimer's disease.

UR-144 N-pentanoic acid is a potent synthetic cannabinoid designed by Abbott Laboratories as a CB2 selective agonist for pain management. UR-144 N-pentanoic acid is a metabolite of another CB2-selective cannabinoid UR-144. Pre-clinical studies of nociceptive and neuropathic pain have shown that CB2-selective ligands are analgesics without causing the adverse side effects linked with CB1 receptor activation. However, nor UR-144 nor UR-144 N-pentanoic acid has no therapeutic application.