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NE-100, a Novel Sigma Receptor Ligand: In Vivo Tests

NE-100, a Novel Sigma Receptor Ligand: In Vivo Tests

S Okuyama, Y Imagawa, S Ogawa, H Araki, A Ajima, M Tanaka, M Muramatsu, A Nakazato, K Yamaguchi, M Yoshida

Life Sci. 1993;53(18):PL285-90.

PMID: 7901723

Abstract:

It has been suggested that sigma receptor antagonists may be useful as antipsychotic drugs. N, N-dipropyl-2-[4-methoxy-3-(2-phenylethoxy)phenyl]-ethylamine monohydrochloride (NE-100) is a novel compound with high affinity for the sigma receptor (IC50 = 4.16 nM), but low affinity (IC50 > 10,000 nM) for D1, D2, 5-HT1A, 5-HT2 and phencyclidine (PCP) receptors. The head-weaving behavior induced by either (+)SKF10047 or PCP was dose-dependently antagonized by NE-100 with oral ED50 at 0.27 and 0.12 mg/kg, respectively. NE-100 did not affect dopamine agonists-induced stereotyped behavior and/or hyperactivity. NE-100 failed to induce catalepsy in rats. These findings indicate that NE-100 may have antipsychotic activity without the liability of motor side effects typical of neuroleptics.

Chemicals Related in the Paper:

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

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