TRK-380 (TAC-301) is an effective and selective β3-adrenergic receptor agonist. TRK-380 improves formalin-induced frequent urination in rats and carbachol-induced bladder contraction in dogs (a decrease of 37.6%).
Several different arachidonoyl amino acids, including N-arachidonoyl-L-alanine (NALA), have been isolated and characterized from bovine brain. The glycine congener (NAGly) was further characterized and found to suppress formalin-induced pain in rats. NALA may have activity at cannabinoid receptor and/or VR1, but has not been fully characterized to date.
Several different arachidonoyl amino acids, including N-arachidonoyl-3-hydroxy-γ-aminobutyric acid (NAG-3H-ABA), have been isolated and characterized from bovine brain. The glycine congener was further characterized and found to suppress formalin-induced pain in rats. NAG-3H-ABA was also found in rat brain by LC-MS techniques, but has not been fully characterized to date. Most arachidonoyl amino acids are poor ligands for the CB1 receptor.
CM398 is an orally active chemical compound that acts as a highly selective ligand for the sigma-2 receptor (K i =0.43 nM), demonstrating a significant ratio of selectivity between sigma-1 and sigma-2 receptors (1000-fold). Moreover, CM398 exhibits notable affinity towards dopamine (K i =32.90 nM) and serotonin transporters (K i =244.2 nM). In addition, CM398 has shown promising efficacy as an anti-inflammatory analgesic in a mouse model of inflammatory pain induced by formalin [1].
DDPM-2571 is a highly potent and in vivo active inhibitor of GABA transporter subtype 1 with anticonvulsant, anxiolytic, antidepressant and antinociceptive properties. DDPM-2571 was quickly distributed into the brain and was highly effective in the prevention of chemically-induced seizures (pentylenetetrazole and pilocarpine models) and 6-Hz convulsions. It demonstrated significant anxiolytic-like and antidepressant-like properties. DDPM-2571 had antinociceptive properties, both in the hot plate test and in the second phase of the formalin test.
N-Acylethanolamines (NAEs) are lipid-derived signaling compounds, with arachidonoyl ethanolamide functioning as an endogenous cannabinoid (CB) that activates CB1 and CB2 receptors. Among these, Palmitoleoyl Ethanolamide (POEA) is synthesized endogenously from palmitoleic acid. Notably, unlike arachidonoyl ethanolamide and palmitoyl ethanolamide, POEA lacks antinociceptive effects in the formalin-evoked pain model.
Potent and selective melanocortin MC4 receptor antagonist (IC50 values are 0.5 and 44.9 nM at MC4 and MC3 respectively) that antagonizes the effects of α-MSH. Suppresses thyrotropin-releasing hormone (TRH) release, attenuates food intake and reduces forma