Primary pharmaco-toxicological evaluation of 2-iodomelatonin, a potent melatonin agonist.
Life Sci
; 53(17): 1357-65, 1993.
Article
em En
| MEDLINE
| ID: mdl-8412502
ABSTRACT
Series of experiments aimed at a primary pharmaco-toxicological evaluation of 2-iodomelatonin, a high-affinity melatonin analogue, were performed. In the rat ovulation-inhibition model, 2-iodomelatonin was much more potent than either melatonin or 6-chloromelatonin. The acute toxicity was extremely low and close to, though slightly higher than that reported previously for melatonin. In the rat, 2-iodomelatonin was slowly metabolized in vivo; its apparent elimination half-life was about 60 minutes, much longer than that reported for melatonin. The in vitro mutagenesis tests demonstrated clearly that 2-iodomelatonin in concentrations, exceeding the dose range employed in the in vivo studies, was actually devoid of mutagenic effects. The obtained results suggest that 2-iodomelatonin deserves a detailed pharmaco-toxicological evaluation and could be eventually used in pharmacokinetic and pharmacodynamic studies in humans.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Melatonina
Limite:
Animals
Idioma:
En
Revista:
Life Sci
Ano de publicação:
1993
Tipo de documento:
Article
País de afiliação:
Itália