[Montirelin hydrate (NS-3), a TRH analog, improved the disturbance of consciousness caused by head concussion and pentobarbital in mice]
| Autor: | Takako Shimizu, Masaru Tamura, Yojiro Ukai, Rika Shibahara, Yoshiaki Yoshikuni, Yoshinori Itoh, Kiyoshi Kimura, Takeshi Mushiroi |
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| Rok vydání: | 1996 |
| Předmět: |
Male
Pentobarbital medicine.medical_specialty Mice Inbred Strains chemistry.chemical_compound Mice Receptors Catecholamine Receptors GABA Dopamine Internal medicine medicine Prazosin Animals Anesthesia Rats Wistar Thyrotropin-Releasing Hormone Brain Concussion Pharmacology Muscarine Chemistry Antagonist Receptors Muscarinic Rats Endocrinology Analeptic Receptors Opioid Consciousness Disorders Righting reflex Acetylcholine medicine.drug |
| Zdroj: | Nihon yakurigaku zasshi. Folia pharmacologica Japonica. 107(5) |
| ISSN: | 0015-5691 |
| Popis: | Effects of a novel TRH analog, montirelin hydrate (NS-3), on the coma caused by head concussion and narcosis induced by pentobarbital were compared with those of TRH in mice. Head concussion caused a behavioral comatose state with loss of the righting reflex and spontaneous motor activity. NS-3 shortened the latent periods to the recovery of the righting reflex (0.03-0.1 mg/kg, i.v.) and spontaneous motor activity (0.1 mg/kg, i.v.) following the head concussion. In the case of TRH, higher doses were needed to induce such effects. NS-3 (0.1-0.3 mg/kg, i.v.) reversed the pentobarbital-induced narcosis in a dose-dependent manner. A similar effect was elicited by 30- to 100-fold higher doses of TRH than NS-3. The analeptic effect of NS-3 in the pentobarbital-narcotized mice was antagonized by SCH23390, a dopamine D1 antagonist or by the combined treatment with prazosin and scopolamine, while neither prazosin nor scopolamine alone antagonized the analeptic effect of NS-3. Taken together with the finding that NS-3 did not bind to dopamine, adrenaline or muscarine receptors, it is suggested that NS-3 may restore the disturbance of consciousness by activating the brain dopamine, noradrenaline and acetylcholine neurons without stimulating these receptors directly. |
| Databáze: | OpenAIRE |
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