1-(2-methoxyphenyl)piperazine is an effective blocker of striatal dopaminergic receptors in rat brain and is apparently the simplest chemical structure known to exert dopaminergic blocking activity. It is exhibited pronounced antihypertensive and weak sympatholytic activities in experimental animals. Blood pressure was also lowered in hypertensive patients and this effect was sometimes accompanied by a strong sedation, and after large repeated doses, by disorientation and stupor. In a filter paper bioassay 1-(2-methoxyphenyl)piperazine demonstrated acaricidal activity. 1-(2-methoxyphenyl)piperazine is a building block of many serotonergic and dopaminergic agents. Some of them have antidepressant activity.

A-967079 is a potent, selective, and orally bioavailable inhibitor of the TRPA1 channel, developed by developed by Abbott Laboratories for treatment pain disorder. A-967079 potently blocks human and rat TRPA1 channels. A-967079 is 1000-fold selective over other TRP channels and is 150-fold selective over 75 other ion channels, enzymes, and G-protein-coupled receptors. Oral dosing of A-967079 produces robust drug exposure in rodents and exhibits analgesic efficacy in allyl isothiocyanate-induced nocifensive response and osteoarthritic pain in rats. A-967079 attenuates cold allodynia produced by nerve injury but does not alter noxious cold sensation in naive animals, suggesting distinct roles of TRPA1 in physiological and pathological states. Unlike TRPV1 antagonists, A-967079 does not alter body temperature. It also does not produce locomotor or cardiovascular side effects.

IVABRADINE, (-)- is an (R)-enantiomers of Ivabradine. IVABRADINE, (-)- produced a concentration-dependent block of hKv1.5 channels. S 16260 (R configuration) and S 16257 (S configuration) of Ivabradine were equipotent in reducing the spontaneous firing of rabbit sinus node preparations, but S 16260 induced significant prolongations of action potential duration of ventricular preparation (guinea pig papillary muscle and rabbit purkinje fibers), contrary to S 16257. These in vitro data have been confirmed by in vivo studies in anesthetized pigs showing the equipotence of the two isomers in reducing the heart rate, the absence of effect of S 16257 on the QT interval corrected for heart rate (QTc) in contrast with S 16260 which induced a dose-dependent increase in the QTc, indicating a direct effect on ventricular repolarization.

A-803467 is a selective NaV1.8 channel blocker with IC50 of 8 nM, blocks tetrodotoxin-resistant currents, exhibits >100-fold selectivity against human NaV1.2, NaV1.3, NaV1.5, and NaV1.7. A-803467 reduces behavioral measures of chronic pain. Systemic administration of A-803467 demonstrated acute antinociceptive activity as measured as a reduction in mechanical allodynia in several models of inflammatory and neuropathic pain in rats. Additionally, systemic and intraspinal delivery of A-803467 attenuates both evoked and spontaneous firing of wide dynamic range neurons in rats with spinal nerve ligations.

PAP-1 (5-(4-phenoxybutoxy)psoralen) is the selective inhibitor of Kv1.3, voltage-gated K+ channel, that is highly expressed in cell membranes of activated effector memory T cells (TEM). The blockade of Kv1.3 results in membrane depolarization and inhibition of TEM proliferation and function. PAP-1 is 23-fold selective over Kv1.5, 33- to 125-fold selective over other Kv1-family channels, and 500- to 7500-fold selective over Kv2.1, Kv3.1, Kv3.2, Kv4.2, HERG, calcium-activated K+ channels, Na+, Ca2+, and Cl- channels. PAP-1 does not exhibit cytotoxic or phototoxic effects, is negative in the Ames test, and affects cytochrome P450-dependent enzymes only at micromolar concentrations. PAP-1 potently inhibits the proliferation of human TEM cells and suppresses delayed-type hypersensitivity, a CD4+ T cell-mediated reaction, in rats when administered intraperitoneally or orally. PAP-1 further effectively treats allergic contact dermatitis, a CD8+ T cell-mediated reaction.