Central Depressant Activity of Some Thiaxanthene Derivatives

2009 ◽  
Vol 19 (1) ◽  
pp. 87-100 ◽  
Author(s):  
I. Møller Nielsen ◽  
W. Hougs ◽  
N. Lassen ◽  
T. Holm ◽  
P. V. Petersen
Keyword(s):  
Central Depressant

Fluorinated tricyclic neuroleptics with prolonged action: 8-Methoxy, 8-ethoxy, 8-ethylthio and 8-hydroxy derivatives of 3-fluoro-10-(4-methylpiperazino)-10,11-dihydrodibenzo[b,f]thiepin

1982 ◽  
Vol 47 (5) ◽  
pp. 1382-1391 ◽  
Author(s):  
Jiří Jílek ◽  
Josef Pomykáček ◽  
Jiřina Metyšová ◽  
Miroslav Protiva
Keyword(s):  
Acetic Acid ◽  
Polyphosphoric Acid ◽  
Prolonged Action ◽  
Substitution Reactions ◽  
Methoxy Derivative ◽  
Chloro Derivatives ◽  
Boron Tribromide ◽  
Derivatives Of ◽  
Central Depressant ◽  
Boiling Toluene

Acids IIa-c were prepared by reactions of (4-fluoro-2-iodophenyl)acetic acid with 4-methoxythiophenol, 4-ethoxythiophenol and 4-(ethylthio)thiophenol and cyclized with polyphosphoric acid in boiling toluene to dibenzo[b,f]thiepin-10(11H)-ones IIIa-c. Reduction with sodium borohydride afforded the alcohols IVa-c which were treated with hydrogen chloride and gave the chloro derivatives Va-c. Substitution reactions with 1-methylpiperazine resulted in the title compounds Ia-c out of which the methoxy derivative Ia was transformed by demethylation with boron tribromide to the phenol Id. Compounds Ia-d are very potent neuroleptics exhibiting a clear prolongation of the central depressant and some prolongation of the cataleptic activity.

scholarly journals Pharmacological Studies on the Chinese Crude Drug"Shoma". III. Central Depressant and Antispasmodic Actions of Cimicifuga Rhizoma, Cimicifuga simplex WORMSK

1980 ◽  
Vol 100 (11) ◽  
pp. 1143-1150 ◽  
Author(s):  
MADOKA SHIBATA ◽  
MIO IKOMA ◽  
MAKOTO ONODA ◽  
FUYUE SATO ◽  
NOBUKO SAKURAI
Keyword(s):  
Crude Drug ◽  
Pharmacological Studies ◽  
Central Depressant

scholarly journals Toxicity and Neuropharmacological Effects of Elenine

2011 ◽  
Vol 2011 ◽  
pp. 1-10 ◽  
Author(s):  
Eduardo Navarro ◽  
S. J. Alonso ◽  
R. Navarro
Keyword(s):  
Open Field ◽  
Field Test ◽  
Chemical Structure ◽  
Open Field Test ◽  
Control Group ◽  
General Behaviour ◽  
Similar Chemical ◽  
Sedative Effects ◽  
Traction Test ◽  
Central Depressant

Elenine is the aglycone of elenoside, a cytotoxic arylnaphthalene lignan (NSC 644013-W/1) derived fromJusticia hyssopifolia. (Family: Acanthaceae). Elenoside is a β-D-glucoside, with a similar chemical structure to etoposide, exhibiting central depressant activity. In the present study, elenine was given to mice and rats at doses of 10, 20, and 40 mg/kg. Acute toxicity (24 h) and general behaviour in mice was studied as well as its effects on muscular relaxant activity, locomotor activity (Varimex test), and the open-field test and were compared with 10 mg/kg of chlorpromazine. Elenine produced a reduction in the permanence time in muscular relaxant activity (traction test). Spontaneous activity was lower in the Varimex test. The ambulation and rearing were lower compared with the control group, and an increase in boluses was observed in the open-field test. Thus, it can be concluded that elenine has central sedative effects at lower doses than those used with elenoside and has a possible application in conditions of anxiety.

Tricyclic psychotropic agents containing two chalcogen atoms in the central ring: 8-Substituted 6-(4-piperidyl)-6H-dibenz[b,e]-1,4-oxathiepins

1982 ◽  
Vol 47 (11) ◽  
pp. 3077-3093 ◽  
Author(s):  
Karel Šindelář ◽  
Jiřina Metyšová ◽  
Jiří Holubek ◽  
Emil Svátek ◽  
Jiří Protiva ◽  
...  
Keyword(s):  
Secondary Amine ◽  
Amino Alcohol ◽  
Sodium Hydride ◽  
Amino Alcohols ◽  
Central Ring ◽  
Psychotropic Agents ◽  
High Degree ◽  
By Products ◽  
Antiapomorphine Effect ◽  
Central Depressant

2-(2-Fluorophenylthio)benzaldehydes IXa-c and 5-chloro-2-(2-fluorophenylthio)acetophenone were treated with 1-methyl-4-piperidylmagnesium chloride and 3-dimethylaminopropylmagnesium chloride, respectively, and the resulting amino alcohols VIa-c, XVII and XVIII were cyclized with sodium hydride in dimethylformamide. In addition to the title compounds Ia-c, XIX and XX, several types of by-products were obtained. Demethylation of compound Ib by the chloroformate method afforded the secondary amine IIb which was transformed to the amino alcohols IIIb and Vb. Compounds Ia-c are very potent neuroleptics with a high degree of central depressant and cataleptic activity. The amino alcohol Vb exhibits a very strong antiapomorphine effect in rats.

Integrin

1967 ◽  
Vol 5 (13) ◽  
pp. 51-52
Keyword(s):  
Body Temperature ◽  
Social Contacts ◽  
Chronic Schizophrenics ◽  
Amphetamine Toxicity ◽  
Central Depressant

Pharmacology - Oxypertine (Integrin-Bayer) has structural affinities with some major phenothiazines, such as trifluoperazine, and also with tryptophan, which has been claimed to elevate mood and increase social contacts in chronic schizophrenics.1 In animals oxypertine is a potent central depressant;2 3 it lowers body temperature, and protects mice grouped together against amphetamine toxicity, about as much as does chlorpromazine.3

scholarly journals Central depressant and nootropic effects of daytime melatonin in mice

2014 ◽  
Vol 21 (3) ◽  
Author(s):  
Olakunle J Onaolapo ◽  
Adejoke Y Onaolapo ◽  
Akanni A Abiola ◽  
Eniafe A Lillian
Keyword(s):  
Central Depressant

scholarly journals Pharmacological studies on grayanoids. (I). Central depressant action of grayanotoxin (III)

1986 ◽  
Vol 40 ◽  
pp. 192
Author(s):  
Takao Ohgaki ◽  
Kazuo Yanada ◽  
Haruo Meguri ◽  
Yukio Yoneda ◽  
Masao Koida
Keyword(s):  
Depressant Action ◽  
Pharmacological Studies ◽  
Central Depressant
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