NEUROPSYCHOPHARMACOLOGICAL STUDY OF 2,4-DIHYDRO[1,2,4] TRIAZOLO[3,4-C][1,4]BENZOTHIAZINE-1-ONE (IDPH-791)

被引:7
|
作者
JUNNARKAR, AY
SINGH, PP
PATNAIK, GK
SHROTRI, DS
机构
[1] IDPL RES CTR, DEPT PHARMACOL, DIV BIOL, BALANAGAR TOWNSHIP, HYDERABAD 500037, INDIA
[2] BJ MED COLL, DEPT PHARMACOL, Pune 411001, INDIA
[3] CENT DRUG RES INST, DEPT PHARMACOL, LUCKNOW 226001, UTTAR PRADESH, INDIA
关键词
IDPH-791; TRIAZOLOBENZOTHIAZINE; CENTRALLY-ACTING MUSCLE RELAXANT; NEUROPSYCHOPHARMACOLOGICAL STUDY;
D O I
10.1016/S1043-6618(05)80126-4
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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. © 1992 The Italian Pharmacological Society.
引用
收藏
页码:131 / 141
页数:11
相关论文
共 50 条
  • [21] The synthesis of 8-tertbutyl-9-oxo-1,2,4-triazolo[4,5-b]-1,2,4-triazolo[3,4-c]-1,2,4-triazine
    Mironovich, LM
    Ivanov, MA
    Kovalchuk, EP
    KHIMIYA GETEROTSIKLICHESKIKH SOEDINENII, 2001, (09): : 1255 - 1257
  • [22] PYRIDAZINE DERIVATIVES AND RELATED-COMPOUNDS .6. SYNTHESIS OF TRIAZOLO [3',4'-5,1]PYRAZOLO[3,4-C]PYRIDAZINE, PYRIDO[2',1'-3,2]-[1,2,4]TRIAZOLO[5',1'-5,1]PYRAZOLO[3,4-C]PYRIDAZINE AND NAPHTHO[2,1-E]-PYRIDAZINO[3',4'-3,4]PYRAZOLO[5,1-C] [1,2,4]TRIAZINE DERIVATIVES
    DEEB, A
    BAYOUMY, B
    HATABA, A
    FIKRY, R
    HETEROCYCLES, 1991, 32 (05) : 901 - 905
  • [23] 8-[2-Chloro-5-(trifluoromethyl)phenyl]-4H-[1,2,4]oxadiazolo-[3,4-c][1,4]benzoxazin-1-one
    Berezin, Andrey A.
    Koutentis, Panayiotis A.
    MOLBANK, 2011, (02)
  • [24] Synthesis and Biological Evaluation of Some [1,2,4]Triazolo[3,4-b][1,3,4]Thiadiazoles and [1,2,4]Triazolo[3,4-b][1,3,4]Thiadiazines
    Naveena, Channamata Shankara
    Poojary, Boja
    Chandrashekhar, Chikkanna
    Kumari, Nalilu Suchetha
    LETTERS IN DRUG DESIGN & DISCOVERY, 2011, 8 (02) : 189 - 200
  • [25] PREPARATION OF [1,2,4]TRIAZOLO[5,1-C][1,2,4]TRIAZINE DERIVATIVES FROM 3,4-DIAMINO[1,2,4]TRIAZINE
    MOLINA, P
    ALAJARIN, M
    DEVEGA, JP
    LOPEZ, A
    HETEROCYCLES, 1989, 29 (08) : 1607 - 1613
  • [26] FLUORINATED [1,2,4]TRIAZOLO[1,5-a]PYRIMIDINES AND [1,2,4]TRIAZOLO[5,1-c][1,2,4]TRIAZINES
    Ulomskiy, E. N.
    Medvedeva, N. R.
    Shchepochkin, A. V.
    Eltsov, O. S.
    Rusinov, V. L.
    Chupakhin, O. N.
    Deeva, E. G.
    Kiselev, O. I.
    CHEMISTRY OF HETEROCYCLIC COMPOUNDS, 2011, 47 (09) : 1164 - 1169
  • [27] Fluorinated [1,2,4]triazolo[1,5-a]pyrimidines and [1,2,4]triazolo[5,1-c][1,2,4]triazines*
    E. N. Ulomskiy
    N. R. Medvedeva
    A. V. Shchepochkin
    O. S. Eltsov
    V. L. Rusinov
    O. N. Chupakhin
    E. G. Deeva
    O. I. Kiselev
    Chemistry of Heterocyclic Compounds, 2011, 47 : 1164 - 1169
  • [28] Synthesis and antimicrobial activities of some new [1,2,4] triazolo[3,4-b][1,3,4]thiadiazoles and [1,2,4]triazolo[3,4-b][1,3,4]thiadiazines
    Demirbas, N
    Demirbas, A
    Karaoglu, SA
    Çelik, E
    ARKIVOC, 2005, : 75 - 91
  • [29] NUCLEOSIDES 515: SYNTHESIS OF NOVEL 1,2,4-TRIAZOLO[3,4-c]-1,2,4-TRIAZOLE NUCLEOSIDES
    Mosselhi, M. A. N.
    Neidlein, R.
    NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS, 2009, 28 (11-12): : 1095 - 1103
  • [30] 2,5-diphenyl-2,5,6,8-tetrahydro-1,2,4-triazolo[3,4-c][1,4]oxazin-4-ium hexafluoridophosphate
    Wu, Jie
    Wei, Siping
    Liu, Bo
    Wang, Wenhai
    Lan, Jingbo
    ACTA CRYSTALLOGRAPHICA SECTION E-STRUCTURE REPORTS ONLINE, 2008, 64 : O1602 - U3228