Sigma opioid receptor; SKF-10,047 update

N. Khazan; G. A. Young; E. E. El-Fakahany; O. Hong; D. Calligaro

doi:10.1016/0143-4179(85)90022-8

Sigma opioid receptor; SKF-10,047 update

N. Khazan, G. A. Young, E. E. El-Fakahany, O. Hong, D. Calligaro

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4 Scopus citations

Abstract

We found that (-)-SKF-10,047 blocks EEG and behavioral effects of morphine in the naive rat, precipitates withdrawal in morphine-dependent rats, produces physical dependence as evidenced by naloxone-induced withdrawal, and displaces [³H] dihydromorphine from brain homogenates. (+)-SKF- 10,047 did not produce dependence upon chronic treatment, and it did not displace [³H] dihydromorphine from brain homogenates. Such pharmacodynamic dissociation of SKF-10,047 effects suggests an association of sigma receptors with psychotogenic, but not opioid characteristics. The latter are most likely mediated by mu or kappa receptors.

Original language	English (US)
Pages (from-to)	339-340
Number of pages	2
Journal	Neuropeptides
Volume	5
Issue number	4-6
DOIs	https://doi.org/10.1016/0143-4179(85)90022-8
State	Published - Feb 1985
Externally published	Yes

ASJC Scopus subject areas

Endocrinology
Neurology
Endocrine and Autonomic Systems
Cellular and Molecular Neuroscience

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abstract = "We found that (-)-SKF-10,047 blocks EEG and behavioral effects of morphine in the naive rat, precipitates withdrawal in morphine-dependent rats, produces physical dependence as evidenced by naloxone-induced withdrawal, and displaces [3H] dihydromorphine from brain homogenates. (+)-SKF- 10,047 did not produce dependence upon chronic treatment, and it did not displace [3H] dihydromorphine from brain homogenates. Such pharmacodynamic dissociation of SKF-10,047 effects suggests an association of sigma receptors with psychotogenic, but not opioid characteristics. The latter are most likely mediated by mu or kappa receptors.",

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AU - Khazan, N.

AU - Young, G. A.

AU - El-Fakahany, E. E.

AU - Hong, O.

AU - Calligaro, D.

PY - 1985/2

Y1 - 1985/2

N2 - We found that (-)-SKF-10,047 blocks EEG and behavioral effects of morphine in the naive rat, precipitates withdrawal in morphine-dependent rats, produces physical dependence as evidenced by naloxone-induced withdrawal, and displaces [3H] dihydromorphine from brain homogenates. (+)-SKF- 10,047 did not produce dependence upon chronic treatment, and it did not displace [3H] dihydromorphine from brain homogenates. Such pharmacodynamic dissociation of SKF-10,047 effects suggests an association of sigma receptors with psychotogenic, but not opioid characteristics. The latter are most likely mediated by mu or kappa receptors.

AB - We found that (-)-SKF-10,047 blocks EEG and behavioral effects of morphine in the naive rat, precipitates withdrawal in morphine-dependent rats, produces physical dependence as evidenced by naloxone-induced withdrawal, and displaces [3H] dihydromorphine from brain homogenates. (+)-SKF- 10,047 did not produce dependence upon chronic treatment, and it did not displace [3H] dihydromorphine from brain homogenates. Such pharmacodynamic dissociation of SKF-10,047 effects suggests an association of sigma receptors with psychotogenic, but not opioid characteristics. The latter are most likely mediated by mu or kappa receptors.

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Sigma opioid receptor; SKF-10,047 update

Abstract

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