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Effect of SA4503, a novel sigma1 receptor agonist, against glutamate neurotoxicity in cultured rat retinal neurons.
Eur J Pharmacol. 1998 Jan 19; 342(1):105-11.EJ

Abstract

We examined the effects of sigma1 receptor agonists against glutamate-induced neurotoxicity in cultured retinal neurons. Primary cultures obtained from fetal rat retinas (16-19 d gestation) were used. The neurotoxic effect of glutamate was quantitatively assessed using the trypan blue exclusion method. A brief exposure of retinal cultures to glutamate (500 microM) led to delayed neuronal cell death. The glutamate-induced neurotoxicity was inhibited by (5R,10S)-(+)-5-methyl-10,11-dihydro-5H-dibenzo-[a,b]-cyclohepten-5 ,10-imine hydrogen maleate (MK-801). The sigma1 receptor agonists, 1-(3,4-dimethoxyphenethyl)-4-(3-phenylpropyl)-piperazine dihydrochloride (SA4503) and (+)-pentazocine at a concentration range of 0.1 approximately 100 microM reduced the glutamate-induced neurotoxicity in a dose-dependent manner. In addition, the neuroprotective effects of both SA4503 and (+)-pentazocine were antagonized by co-treatment with N,N-dipropyl-2-[4-methoxy-3-(2-phenylethoxy)phenyl]ethylamine monohydrochloride (NE-100), a putative sigma1 receptor antagonist. These findings suggest that sigma1 receptor agonists protect retinal cells against glutamate-induced neurotoxicity.

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Authors+Show Affiliations

Senda T
Discovery Research Division, Santen Pharmaceutical Co., Ltd., Osaka, Japan.
Mita S
No affiliation info available
Kaneda K
No affiliation info available
Kikuchi M
No affiliation info available
Akaike A
No affiliation info available

MeSH

Analgesics, OpioidAnimalsCell SurvivalCells, CulturedDizocilpine MaleateExcitatory Amino Acid AntagonistsGABA AntagonistsGlutamic AcidNeuronsPentazocinePiperazinesRatsReceptors, sigmaRetina

Pub Type(s)

Journal Article

Language

eng

PubMed ID

9544798

Citation

Senda, T, et al. "Effect of SA4503, a Novel Sigma1 Receptor Agonist, Against Glutamate Neurotoxicity in Cultured Rat Retinal Neurons." European Journal of Pharmacology, vol. 342, no. 1, 1998, pp. 105-11.
Senda T, Mita S, Kaneda K, et al. Effect of SA4503, a novel sigma1 receptor agonist, against glutamate neurotoxicity in cultured rat retinal neurons. Eur J Pharmacol. 1998;342(1):105-11.
Senda, T., Mita, S., Kaneda, K., Kikuchi, M., & Akaike, A. (1998). Effect of SA4503, a novel sigma1 receptor agonist, against glutamate neurotoxicity in cultured rat retinal neurons. European Journal of Pharmacology, 342(1), 105-11.
Senda T, et al. Effect of SA4503, a Novel Sigma1 Receptor Agonist, Against Glutamate Neurotoxicity in Cultured Rat Retinal Neurons. Eur J Pharmacol. 1998 Jan 19;342(1):105-11. PubMed PMID: 9544798.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Effect of SA4503, a novel sigma1 receptor agonist, against glutamate neurotoxicity in cultured rat retinal neurons. AU - Senda,T, AU - Mita,S, AU - Kaneda,K, AU - Kikuchi,M, AU - Akaike,A, PY - 1998/4/17/pubmed PY - 1998/4/17/medline PY - 1998/4/17/entrez SP - 105 EP - 11 JF - European journal of pharmacology JO - Eur J Pharmacol VL - 342 IS - 1 N2 - We examined the effects of sigma1 receptor agonists against glutamate-induced neurotoxicity in cultured retinal neurons. Primary cultures obtained from fetal rat retinas (16-19 d gestation) were used. The neurotoxic effect of glutamate was quantitatively assessed using the trypan blue exclusion method. A brief exposure of retinal cultures to glutamate (500 microM) led to delayed neuronal cell death. The glutamate-induced neurotoxicity was inhibited by (5R,10S)-(+)-5-methyl-10,11-dihydro-5H-dibenzo-[a,b]-cyclohepten-5 ,10-imine hydrogen maleate (MK-801). The sigma1 receptor agonists, 1-(3,4-dimethoxyphenethyl)-4-(3-phenylpropyl)-piperazine dihydrochloride (SA4503) and (+)-pentazocine at a concentration range of 0.1 approximately 100 microM reduced the glutamate-induced neurotoxicity in a dose-dependent manner. In addition, the neuroprotective effects of both SA4503 and (+)-pentazocine were antagonized by co-treatment with N,N-dipropyl-2-[4-methoxy-3-(2-phenylethoxy)phenyl]ethylamine monohydrochloride (NE-100), a putative sigma1 receptor antagonist. These findings suggest that sigma1 receptor agonists protect retinal cells against glutamate-induced neurotoxicity. SN - 0014-2999 UR - https://www.unboundmedicine.com/medline/citation/9544798/Effect_of_SA4503_a_novel_sigma1_receptor_agonist_against_glutamate_neurotoxicity_in_cultured_rat_retinal_neurons_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0014-2999(97)01450-7 DB - PRIME DP - Unbound Medicine ER -