NE-100, a novel sigma receptor ligand: in vivo tests.

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.

• Authors: S Okuyama, Y Imagawa, S Ogawa, H Araki, A Ajima, M Tanaka, M Muramatsu, A Nakazato, K Yamaguchi, M Yoshida
• Journal: Life sciences (Life Sci) Vol. 53 Issue 18 Pg. PL285-90 ( 1993) ISSN: 0024-3205 [Print] Netherlands
• PMID: 7901723 (Publication Type: Journal Article)

Chemical References

• Anisoles
• Antipsychotic Agents
• Dopamine Agents
• Propylamines
• Receptors, sigma
• N,N-dipropyl-2-(4-methoxy-3-(2-phenylethoxy)phenyl)ethylamine monohydrochloride
• SK&F 10047
• Phenazocine
• Phencyclidine

Topics

• Animals
• Anisoles (metabolism, pharmacology)
• Antipsychotic Agents (metabolism, pharmacology)
• Behavior, Animal (drug effects)
• Binding, Competitive
• Catalepsy (chemically induced)
• Dopamine Agents (pharmacology)
• Drug Interactions
• Locomotion (drug effects)
• Male
• Phenazocine (analogs & derivatives, pharmacology)
• Phencyclidine (pharmacology)
• Propylamines (metabolism, pharmacology)
• Radioligand Assay
• Rats
• Rats, Inbred Strains
• Rats, Wistar
• Receptors, sigma (antagonists & inhibitors)
• Stereotyped Behavior (drug effects)