Abstract |
The neuropsychopharmacological profile of a new centrally acting skeletal muscle relaxant, 2,4-dihydro[1,2,4]triazolo[3,4-c][1,4]benzothiazine-1-one (IDPH-791), an analogue of triazolobenzothiazine, has been described and compared to mephenesin, a well known centrally-acting muscle relaxant. IDPH-791 was found to be safer and of longer duration of action than mephenesin in all the tests conducted in this study. Both IDPH-791 and mephenesin caused ataxia, decrease in spontaneous activity and inhibition of pinnal reflex. IDPH-791 was 1.5 to 2.0 times more potent in exhibiting motor inco-ordination and anticonvulsant activity than mephenesin in mice and rats. IDPH-791 was twice as active in inhibiting various spinal polysynaptic reflexes, crossed extensor, flexor, and linguomandibular reflexes; however, both did not affect the typical monosynaptic reflex, patellar reflex. IDPH-791 and mephenesin did not have sedative activity. Although mephenesin exhibited haemolytic activity, IDPH-791 was devoid of this activity. It is concluded that IDPH-791 is a safe and effective centrally-acting muscle relaxant having a longer duration of action than mephenesin. IDPH-791 is also devoid of sedative and haemolytic activity.
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Authors | A Y Junnarkar, P P Singh, G K Patnaik, D S Shrotri |
Journal | Pharmacological research
(Pharmacol Res)
Vol. 26
Issue 2
Pg. 131-41
(Sep 1992)
ISSN: 1043-6618 [Print] Netherlands |
PMID | 1409254
(Publication Type: Comparative Study, Journal Article)
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Chemical References |
- Muscle Relaxants, Central
- Thiazines
- Triazoles
- Mephenesin
- IDPH-791
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Topics |
- Administration, Oral
- Animals
- Brain
(drug effects)
- Hypnosis
- Injections, Intraperitoneal
- Lethal Dose 50
- Mephenesin
(administration & dosage, pharmacology, toxicity)
- Mice
- Motor Activity
(drug effects)
- Muscle Relaxants, Central
(administration & dosage, pharmacology, toxicity)
- Muscle Relaxation
(drug effects)
- Paralysis
(chemically induced)
- Rabbits
- Rats
- Rats, Wistar
- Seizures
(prevention & control)
- Thiazines
(pharmacology)
- Triazoles
(pharmacology)
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