NE-100, a novel potent sigma ligand, preferentially binds to sigma 1 binding sites in guinea pig brain.
The selectivity of N,N-dipropyl-2-[4-methoxy-3-(2-phenylethoxy)phenyl]-ethylamine monohydrochloride (NE-100) for sigma 1 and sigma 2 binding sites was studied by means of binding of [3H](+)-pentazocine and [3H]1,3-di-o-tolylguanidine ([3H]DTG) in guinea pig brain. NE-100 inhibited [3H](+)-pentazocine binding to sigma 1 binding sites potently with an IC50 value of 1.54 +/- 0.26 nM while it had a weak effect on [3H]DTG binding to sigma 2 binding sites. The inhibitory effect of NE-100 on [3H](+)-pentazocine was 55 times more potent than that on [3H]DTG binding. These results suggest that NE-100 is a potent and selective ligand for sigma 1 binding sites.
Chaki
S
S
Department of Pharmacology, Taisho Pharmaceutical Co. Ltd., Saitama, Japan.
Tanaka
M
M
Muramatsu
M
M
Otomo
S
S
D000818:Animals; D000840:Anisoles / Q000494:pharmacology*; D001667:Binding, Competitive / Q000187:drug effects; D001921:Brain / Q000187:drug effects / Q000378:metabolism*; D006146:Guanidines / Q000493:pharmacokinetics; D006168:Guinea Pigs; D066298:In Vitro Techniques; D008024:Ligands; D010423:Pentazocine / Q000493:pharmacokinetics; D011437:Propylamines / Q000494:pharmacology*; D017480:Receptors, sigma / Q000187:drug effects*
D000840:Anisoles; D006146:Guanidines; D008024:Ligands; D011437:Propylamines; D017480:Receptors, sigma; C083832:N,N-dipropyl-2-(4-methoxy-3-(2-phenylethoxy)phenyl)ethylamine monohydrochloride; C050232:1,3-ditolylguanidine; D010423:Pentazocine