Acute Effects of Nalmefene on LH, Prolactin, and Testosterone in Male Rhesus Monkeys

The effects of the long-acting opioid antagonist, nalmefene [17-N-cyclopropylmethyl-3,14-β-dihydroxy-4,5-α-epoxy-6-methylene morphinan hydrochloride] on LH, T, and prolactin release in rhesus monkeys are unknown. The acute effects of nalmefene (0.01 and 0.10 mg/kg, IV) or placebo on LH, PRL, and T w...

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Bibliographic Details
Published in:Pharmacology, biochemistry and behavior biochemistry and behavior, 2000-06, Vol.66 (2), p.275-283
Main Authors: Mello, Nancy K, Mendelson, Jack H, Kelly, Maureen
Format: Article
Language:English
Subjects:
Animals
Biological and medical sciences
Genital system. Reproduction
Hypothalamus - drug effects
Hypothalamus - metabolism
Kinetics
Luteinizing hormone
Luteinizing Hormone - blood
Luteinizing Hormone - metabolism
Macaca mulatta
Male
Medical sciences
Nalmefene
Naltrexone - administration & dosage
Naltrexone - analogs & derivatives
Naltrexone - pharmacology
Narcotic Antagonists - administration & dosage
Narcotic Antagonists - pharmacology
Opioidantagonist
Pharmacology. Drug treatments
Pituitary Gland - drug effects
Pituitary Gland - metabolism
Prolactin
Prolactin - blood
Prolactin - metabolism
Testosterone
Testosterone - blood
Testosterone - metabolism
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Summary:The effects of the long-acting opioid antagonist, nalmefene [17-N-cyclopropylmethyl-3,14-β-dihydroxy-4,5-α-epoxy-6-methylene morphinan hydrochloride] on LH, T, and prolactin release in rhesus monkeys are unknown. The acute effects of nalmefene (0.01 and 0.10 mg/kg, IV) or placebo on LH, PRL, and T were studied, and samples were collected at 10-min intervals for 360 min to permit cluster analysis of pulsatile release patterns. LH increased significantly within 30 min after nalmefene, and remained significantly above baseline levels for 50 to 60 min ( p < 0.05). Testosterone increased significantly within 70 to 80 min after nalmefene, and remained significantly above baseline for 60 min ( p < 0.05). Although nalmefene antagonizes opioid agonists for 6–8 h, inhibitory feedback by testosterone appeared to limit the duration of its antagonism of endogenous opioid inhibition of LHRH and stimulation of LH. Nalmefene did not change LH or PRL pulse frequency or amplitude significantly in comparison to placebo administration.
ISSN:0091-3057
1873-5177
DOI:10.1016/S0091-3057(00)00190-8