Add time:09/03/2019         Source:sciencedirect.com

A series of original 2(3H)-benzoxazolone and 2(3H)-benzothiazolone derivatives were evaluated for their affinity at σ1 and σ2 receptor subtypes in competition binding experiments, using [3H](+)-pentazocine or [3H]1,3-di-o-tolyl-guanidine (DTG) in the presence of 100 nM (+)-N-allylnormetazocine (NANM) in guinea pig brain membranes. Several of these derivatives showed preferential selectivity for σ1 binding sites. Compound 1 [3-(1-piperidinoethyl)-6-propylbenzothiazolin-2-one] emerged as a potent σ1 receptor ligand (Ki=0.6 nM) and displayed a moderate selectivity over the σ2 receptor subtype (Ki for σ2/Ki for σ1=29). Compounds 2 [3-(1-piperidinopropyl)-6-propanoylbenzothiazolin-2-one] and 3 [3-(1-piperidinopropyl)-6-propanoylbenzoxazolin-2-one] still showed rather high affinities for σ1 binding sites with Ki values of 2.3 and 8.5 nM, respectively. On the contrary, they had 87 and 58 fold less affinity at σ2 receptors, respectively. Unlike their potent affinity for σ binding sites, these compounds had negligible affinity for μ-, δ- and κ-opioid receptors, 5-HT2, dopamine D2, and muscarinic M2 receptors. σ Receptor ligands may affect neuronal transmission and display, in animal models, antipsychotic, cognitive, motor, neuroprotective and anticonvulsant activity. Therefore, on the basis of these findings, these novel σ receptor ligands were assayed, in mice, in three tests: maximal electroshock, subcutaneous pentylenetetrazol, and rotarod neurotoxicity. Compound 1, administered intraperitoneally, was the most effective against maximal electroshock-induced seizures and was devoid of significant neurotoxic effects.

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