title: Selective MT(2) melatonin receptor antagonist blocks melatonin-induced antinociception in rats.
abstract: The present study was undertaken to assess the effects of intracerebroventricular (i.c.v.) luzindole (a selective MT(2) melatonin receptor antagonist) and prazosin (a selective MT(3) melatonin receptor antagonist) on melatonin-induced antinociception, so as to clarify which of melatonin receptor subtypes within the central nervous system (CNS) was mediating antinociception. The pain threshold of rats was measured by the hot water (50 degrees C) tail-flick test. It was found that intraperitoneal (i.p.) melatonin (30, 60, 120 mg/kg) resulted in a dose-dependent antinociception. Luzindole (50, 100 microgram) administered intracerebroventricularly antagonized significantly the antinociceptive effect induced by i.p. melatonin (120 mg/kg), whereas prazosin (50 microgram) did not. Neither luzindole (100 microgram, i.c.v.) nor prazosin (50 microgram, i.c.v.) affected the nociceptive threshold when given alone. The results suggest that melatonin-induced antinociception is mediated through the MT(2) melatonin receptor subtype within the CNS.
authors.affiliation: State Key Laboratory of Medical Neurobiology, Department of Neurobiology, Shanghai Medical University, Shanghai, China.
authors.forename: C X
authors.initials: CX
authors.lastname: Yu
authors.forename: C B
authors.initials: CB
authors.lastname: Zhu
authors.forename: S F
authors.initials: SF
authors.lastname: Xu
authors.forename: X D
authors.initials: XD
authors.lastname: Cao
authors.forename: G C
authors.initials: GC
authors.lastname: Wu
mesh_terms: D000700:Analgesics / Q000494:pharmacology*; D000818:Animals; D007276:Injections, Intraventricular; D008297:Male; D008550:Melatonin / Q000494:pharmacology*; D010147:Pain Measurement; D017288:Pain Threshold; D011224:Prazosin / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D011956:Receptors, Cell Surface / Q000037:antagonists & inhibitors*; D018160:Receptors, Cytoplasmic and Nuclear / Q000037:antagonists & inhibitors*; D044094:Receptors, Melatonin; D014363:Tryptamines / Q000494:pharmacology
chemical_list: D000700:Analgesics; D011956:Receptors, Cell Surface; D018160:Receptors, Cytoplasmic and Nuclear; D044094:Receptors, Melatonin; D014363:Tryptamines; C057154:luzindole; D008550:Melatonin; D011224:Prazosin