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NE-100, a Novel Sigma Ligand: Effects on [3H]TCP Binding to Intact Primary Cultured Neuronal Cells

NE-100, a Novel Sigma Ligand: Effects on [3H]TCP Binding to Intact Primary Cultured Neuronal Cells

H Yamamoto, T Yamamoto, N Sagi, S Okuyama, N Kawai, A Baba, T Moroji

Life Sci. 1995;56(2):PL39-43.

PMID: 7823755

Abstract:

N,N-dipropyl-2-[4-methoxy-3-(2-phenylethoxy)phenyl]-ethylamine monohydrochloride (NE-100), a potent and highly selective sigma ligand, haloperidol, (+)pentazocine, 1-(cyclopropyl-methyl)-4-(2'-(4"-fluorophenyl)-2'-oxoethyl) piperidine HBr (DuP 734) and 4-(2'-(4"-cyanophenyl)-2'-oxoethyl) 1-(cyclopropylmethyl)piperidine (XJ 448) inhibited carbachol-induced inositol 1,4,5-triphosphate (IP3) formation in a dose-dependent manner. The rank order of potency of the tested drugs for inhibition was: haloperidol > or = (+)pentazocine = NE-100 > DuP 734 = XJ 448. In addition, the effects of NE-100, DuP 734 and XJ 448 upon [3H]TCP binding were examined using primary cultured neuronal cells derived from the fetal rat telencephalon. These drugs inhibited [3H]TCP binding to intact cells. The ability of the test drugs to inhibit [3H]TCP binding to primary cultured neuronal cells was in the order: NE-100 > DuP 734 > XJ 448. These observations suggest that NE-100 indirectly modulates the N-methyl-D-aspartate (NMDA)/phencyclidine (PCP) receptor ion channel complex (NMDA receptor-ion channel), presumably through sigma-1 sites.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP149409574	NE-100		149409-57-4	Price

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