A novel melatonin antagonist affects melatonin-mediated processes in vitro and in vivo

Nava Zisapel; Moshe Laudon

doi:10.1016/0014-2999(87)90722-9

A novel melatonin antagonist affects melatonin-mediated processes in vitro and in vivo

Nava Zisapel^*, Moshe Laudon

^*Corresponding author for this work

Department of Neurobiology

Tel Aviv University

Research output: Contribution to journal › Article › peer-review

27 Scopus citations

Original language	English
Pages (from-to)	259-260
Number of pages	2
Journal	European Journal of Pharmacology
Volume	136
Issue number	2
DOIs	https://doi.org/10.1016/0014-2999(87)90722-9
State	Published - 14 Apr 1987

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title = "A novel melatonin antagonist affects melatonin-mediated processes in vitro and in vivo",

author = "Nava Zisapel and Moshe Laudon",

note = "Funding Information: Melatonin has a role in conveying the environmental photoperiodic stimuli that impinge upon the mammalian reproductive axis (Tamarkin, 1985). Some of the difficulties encountered in melatonin research stem from the lack of efficient blockers of melatonin activity. Our previous observations (Zisapel and Laudon, 1982) that melatonin inhibits the stimulated release of dopamine from the rat hypothalamus enabled us to test in vitro the potencies of putative melatonin antagonists. We have synthesized (to be described elsewhere) N-(3,5-dinitrophenyl)-5-methoxytryptamine (ML-23) and now report that it is a potent antagonist of melatonin in vitro and is also able to prevent the melatonin-mediated retardation of prostatal development in immature male rats. In the in vitro experiments, adult female rats (CD strain) at the estrous stage (i.e. when maximal responsiveness to melatonin occurs; Zisapel et al., 1983) were decapitated between 08:00 and 10:00 h; their hypothalami were excised and incubated with 0.4 /~M \[3H\]dopamine (New England Nuclear, Boston). The hypothalami were then transferred to a superfusion chamber and subjected to two successive sets of electrical field stimulation as described by Zisapel and Laudon (1982). The tissue fragments were exposed to melatonin (1 /~M) in the absence or presence of ML-23 (1 #M) during the interval (25 n-fin) between the two sets of stimuli. The quantities of 1 This work was supported in part by the Israel Academy of Science and Humanities. * To whom correspondence should be addressed.",

year = "1987",

month = apr,

day = "14",

doi = "10.1016/0014-2999(87)90722-9",

language = "אנגלית",

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journal = "European Journal of Pharmacology",

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T1 - A novel melatonin antagonist affects melatonin-mediated processes in vitro and in vivo

AU - Zisapel, Nava

AU - Laudon, Moshe

N1 - Funding Information: Melatonin has a role in conveying the environmental photoperiodic stimuli that impinge upon the mammalian reproductive axis (Tamarkin, 1985). Some of the difficulties encountered in melatonin research stem from the lack of efficient blockers of melatonin activity. Our previous observations (Zisapel and Laudon, 1982) that melatonin inhibits the stimulated release of dopamine from the rat hypothalamus enabled us to test in vitro the potencies of putative melatonin antagonists. We have synthesized (to be described elsewhere) N-(3,5-dinitrophenyl)-5-methoxytryptamine (ML-23) and now report that it is a potent antagonist of melatonin in vitro and is also able to prevent the melatonin-mediated retardation of prostatal development in immature male rats. In the in vitro experiments, adult female rats (CD strain) at the estrous stage (i.e. when maximal responsiveness to melatonin occurs; Zisapel et al., 1983) were decapitated between 08:00 and 10:00 h; their hypothalami were excised and incubated with 0.4 /~M \[3H\]dopamine (New England Nuclear, Boston). The hypothalami were then transferred to a superfusion chamber and subjected to two successive sets of electrical field stimulation as described by Zisapel and Laudon (1982). The tissue fragments were exposed to melatonin (1 /~M) in the absence or presence of ML-23 (1 #M) during the interval (25 n-fin) between the two sets of stimuli. The quantities of 1 This work was supported in part by the Israel Academy of Science and Humanities. * To whom correspondence should be addressed.

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A novel melatonin antagonist affects melatonin-mediated processes in vitro and in vivo

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