Synthesis and comparative skeletal muscle relaxant activity of some 2,4-imidazolidinediones and their corresponding 5-hydroxy-2,4-imidazolidinediones
| Autor: | Thomas J. Schwan, K. O. Ellis, Ralph L. White, F. L. Wessels |
|---|---|
| Rok vydání: | 1978 |
| Předmět: |
Male
medicine.drug_class Metabolite Mice Inbred Strains Pharmacology In Vitro Techniques Dantrolene Sodium Dantrolene chemistry.chemical_compound Mice In vivo Drug Discovery medicine Animals Postural Balance Morphine Chemistry Muscle Relaxants Central Antagonist Imidazoles Skeletal muscle Muscle relaxant Rats Inbred Strains In vitro Rats medicine.anatomical_structure Molecular Medicine medicine.drug Muscle Contraction |
| Zdroj: | Journal of medicinal chemistry. 21(1) |
| ISSN: | 0022-2623 |
| Popis: | A series of 5-hydroxy substitution products of 2,4-imidazolidinediones, including the 5-hydroxy metabolite of the skeletal muscle contraction antagonist, dantrolene sodium, has been synthesized and evaluated for skeletal muscle relaxant activity. Most of these analogues are active in vivo with iv administration and in vitro. While two analogues are also active by oral and ip administration, only 1-[[[5-(3,4-dichlorophenyl)-2-furanyl]methylene]amino]-5-hydroxy-2,4-imidazolidinedione is sufficiently active in inhibiting the Straub tail in mice. However, none of these analogues has a muscle relaxant efficacy index greater than 1, comparable to dantrolene. |
| Databáze: | OpenAIRE |
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