Diethylcarbamazine (DEC) produced an initial stimulation followed by depression of the movements of the intact worm and nerve-muscle preparation of Setaria cervi. The effective concentration of DEC was reduced to one hundredth in the nerve-muscle preparation as compared to the whole worm, suggesting that the cuticular barrier is highly effective in preventing the penetration of the drugs. The d...

The effects of NSAIDs (aspirin and indomethacin) on the isolated auricles of the rabbit heart were studied by observing the effects of these drugs on automaticity, excitability and contractility of the auricles. Aspirin (25,50,100 uM) produced concentration dependent depression in the automaticity of the SA node while indomethacin (10 uM, 25 uM) has stimulant effects and 50 uM produced depressa...

The central nervous system depressant activity of the crude methanol extract (REC) and fractions (RE1, RE2, and RE3) of Russelia equisetiformis were evaluated in mice using the following models: amphetamine-induced stereotypy, picrotoxin-induced convulsion and phenobarbitone sleeping time. At 200-400 mg/kg, REC significantly increased phenobarbitone-sleeping time [P < 0.05] in a dose- dependent...

The pharmacological effects on the central nervous system (CNS) of a range of available flavonoid glycosides were explored and compared to those of the glycosides 2S-hesperidin and linarin, recently isolated from valeriana. The glycosides 2S-neohesperidin, 2S-naringin, diosmin, gossipyn and rutin exerted a depressant action on the CNS of mice following i.p. injection, similar to that found with...

Metaphit, 1-(1-(3-isothiocyanatophenyl) cyclohexyl) piperidine, an analog of phencyclidine (PCP) has been shown previously to selectively block PCP receptors and to irreversibly antagonize the depressant effect of PCP in cerebellum. In this study, we examined the electrophysiological interactions of metaphit and naloxone with stereoisomers of cyclazocine, an agent known to have analgesic and ps...

N3-Substituted derivatives of 2',3'-O-isopropylideneuridine (1) were synthesized and their pharmacological effects on the central nervous system (CNS) examined using mice. Methyl (2), ethyl (3), propyl (4), butyl (5), allyl (6), benzyl (7), o-, m-, p-xylyls (8, 9, 10), and alpha-phenylethyl (11) derivatives of 1 were administered to mice by intracerebroventricular (i.c.v.) injection for evaluat...

Dexmedetomidine is an alpha(2)-adrenoreceptor agonist that, in spite of its potent sedative, amnesic, and analgesic properties, has minimal respiratory depressant effect. Even at doses adequate for general anaesthesia, it does not cause central apnoea. Thus, it has been claimed that "combining alpha(2)-agonists with opiate narcotics or non-steroidal anti-inflammatory drugs can enhance the analg...

Methyl (2), ethyl (3), propyl (4), butyl (5), allyl (6), benzyl (7), o-, m-, p-xylyl (8-10), and alpha-phenylethyl (11) derivatives of arabinofuranosyluracil (1) were synthesized and their pharmacological effects in mice were examined by using hypnotic activity and synergism with pentobarbital as indices for the CNS depressant effects. At a dose of 2.0 micromol/mouse by intracerebroventricular ...

In Australia, a study of 76 GHB users found they were stable, well-functioning, and highly educated. Some 29% typically drank more than five alcoholic drinks when using GHB and they had extensive experience with a range of other drugs which they used with GHB. But even though these users did not have a long or extensive experience with GHB, 99% reported at least one negative side effect. Of tho...

The central nervous system (CNS) depressant and anticonvulsant activities of iso-6-spectaline (SPEC) were investigated in animal models. The SPEC from Senna spectabilis var. excelsa (Schrad) (0.1, 0.5 and 1.0 mg/ kg) injected by oral route (p.o.) in mice caused a significant decrease in the motor activity up to 30 days after the administration and in the dose of 1.0 mg/kg significantly reduced ...