PMID: 2506487Aug 1, 1989Paper

Effects of a new analogue of thyrotropin-releasing hormone on pentobarbital-induced sleeping time in rodents

Neuropharmacology
M Yamamoto, M Shimizu

Abstract

The effects of a new analogue of TRH, YM-14673 (N-[[(S)-4-oxo-2-azetidinyl]carbonyl]-L-histidyl-L-prolinamide dihydrate) on pentobarbital-sleeping time were observed in comparison with those of TRH in rodents. The YM-14673 was administered intravenously, orally and intramuscularly. In all cases it reduced pentobarbital-sleeping time in rats and/or mice in a dose-dependent manner. The analeptic activity of YM-14673 was about 10 times greater than that of TRH. Analeptic action was also observed with successive intravenous injections of YM-14673, once daily for 5 and 14 days in mice, suggesting that the drug induced no tolerance. In addition, there was evidence that the pituitary-thyroid axis was not necessary for the analeptic effects of YM-14673. In particular, it was noted that hypophysectomy did not reduce the antagonism by YM-14673 of pentobarbital-induced sleep and intracerebrally administered YM-14673 produced analeptic actions in mice. Pretreatment with atropine and baclofen antagonized the ability of YM-14673 to reduce sleep, induced by pentobarbital in mice. However, the analeptic action of YM-14673 was not reduced by the administration of haloperidol and phentolamine. These results suggest that YM-14673 produced facilit...Continue Reading

References

Nov 1, 1987·Naunyn-Schmiedeberg's Archives of Pharmacology·M Yamamoto, M Shimizu
Feb 1, 1974·Life Sciences·A J PrangeN P Plotnikoff
Dec 1, 1971·The Journal of Clinical Endocrinology and Metabolism·L S JacobsW H Daughaday
Oct 1, 1982·Pharmacology, Biochemistry, and Behavior·M MiyamotoY Nagawa

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