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Neuropsychopharmacological study of 2,4-dihydro[1,2,4]triazolo[3,4-c][1,4]benzothiazine-1-one (IDPH-791).

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.
AuthorsA Y Junnarkar, P P Singh, G K Patnaik, D S Shrotri
JournalPharmacological research (Pharmacol Res) Vol. 26 Issue 2 Pg. 131-41 (Sep 1992) ISSN: 1043-6618 [Print] Netherlands
PMID1409254 (Publication Type: Comparative Study, Journal Article)
Chemical References
  • Muscle Relaxants, Central
  • Thiazines
  • Triazoles
  • Mephenesin
  • IDPH-791
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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