Methyl cholate is a cholesterol biosynthesis inhibitor. It exhibited inhibitory effect on the later step of cholesterol biosynthesis, indicating that its action mode is different from that of statins that act on the HMG-CoA reductase.

IMB-10 stabilizes binding of alpha(M)beta(2) to its endogenous ligands proMMP-9 and fibrinogen. It inhibited alpha(M)beta(2)-dependent migration in vitro and inflammation-induced neutrophil emigration in vivo. IMB-10 therapy inhibited the growth of both leukemia and lymphoma xenografts and significantly prolonged the survival of the mice with lymphoma. IMB-10 has potential as a therapy for leukocytic malignancies, particularly for lymphomas.

DBO-83 is a 3,8-diazabicyclo[3.2.1]octane derivative with antinociceptive properties. DBO-83 exhibits high affinity for the α4β2 subtype and is a full agonist at α4β2 and ganglionic receptors but lacks appreciable activity at neuromuscular receptors. DBO-83 exhibits antinociceptive activity in both rat and mouse models of acute and persistent pain. In addition DBO-83 modulates memory functions in rodents.

SNC80 is a highly selective agonist of δ opioid receptor but also binds to μ-δ opioid receptor heteromers to produce antinociception in mice. SNC80 also acts as anti-depressant, elicits dopamine-related behaviors and enhances behavioral responses to psychostimulants. SNC80 is not used medically, because of producing convulsions at high doses, although it is a useful drug in scientific research.

N-Methylquipazine is a tertiary amine analog of quipazine. It binds at 5-HT3 sites with an affinity similar to that of quipazine. N-methylquipazine has a low affinity for 5-HT1A, 5-HT1B, 5-HT2, a1, a2 and muscarinic receptors. It produces a concentration-dependent increase in extracellular dopamine levels in the anterior medial prefrontal cortex. This action is dependent on the presence of Ca+2, is impulse-dependent, and depends on newly synthesized dopamine stores. The increase in the anterior medial prefrontal cortex dopamine levels by n-methylquipazine is probably, not mediated by its interaction with the 5-HT3 receptor. It might be an be an attractive candidate as a radioligand for the PET studies of 5-HT3 receptors in man.

(S)-AM-1241 is enantiomer of the CB2 modulator, that has most penetrated the literature, has proven an important research tool for investigating CB2-mediated antinociception. (R, S)-AM1241 produces antinociception following local and systemic administration in naive rats. Behavioral, neurochemical, and electrophysiological studies suggest that (R, S)-AM1241 suppresses persistent pain through a CB2-specific mechanism. In cAMP inhibition assays, (R, S)-AM1241 was found to be an agonist at human CB(2), but an inverse agonist in rat and mouse CB(2) receptors. (R)-AM1241 bound with more than 40-fold higher affinity than (S)-AM1241, to all three CB(2) receptors and displayed a functional profile similar to that of the racemate. In contrast, S-AM1241 was an agonist at all three CB(2) receptors. In pain models, S-AM1241 was more efficacious than either R-AM1241 or the racemate. In preclinical studies (R, S)-AM1241, (R)-AM1241, and (S)-AM1241 produced antinociception to thermal, but not mechanical, stimulation of the hind paw in naive rats. Antinociception produced by (R, S)-AM1241 and (S)-AM1241 exhibited an inverted U-shaped dose-response curve. (R)-AM1241 produced greater antinociception than either (S)-AM1241 or (R, S)-AM1241. (R, S)-AM1241, (R)-AM1241, and (S)-AM1241 each produced CB2-mediated antinociception that was blocked by SR144528 but not by rimonabant. Local and systemic naloxone blocked morphine-induced antinociception but did not block antinociceptive effects of (R, S)-AM1241, (R)-AM1241, or (S)-AM1241. The physiological and toxicological properties of (S)-AM-1241 have not been evaluated in humans.

16alpha-hydroxyestrone is a naturally occurring estrone metabolite. It exerts estrogenic properties through covalent estrogen receptor (ER) binding. 16alpha-hydroxyestrone is a potential tumor initiator. The ratio 2-hydroxyestrone to 16alpha-hydroxyestrone could serve as an innovative intermediate biomarker for breast cancer risk. This biomarker could be used to identify women at high risk, and provide the analytic framework for the development of new pharmaceutical and dietary intervention strategies.