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At least 19 recordsLinked to original sources
PubMed1978

Synthesis of spiro[isobenzofuran-1(3H),4'-piperidines] as potential central nervous system agents. 4. Central nervous system depressants.

The synthesis of 1'-[3-(4-fluorobenzyoyl)propyl]-3-phenylspiro[isobenzofuran-1(3H),4'-piperidine] (2a) and eight halo and methoxy analogues is described. The compounds were generally more potent per os than chlorpromazine in the Sidman avoidance paradigm in rats and less potent than haloperido. 1'-[3-(4-Fluorobenzoyl)propyl]-3-(4-fluorophenyl)spiro[isobenzofuran-1(3H),4'-piperidine] (2e) approached the per os potency of haloperidol in this test and was shown to be active in inhibiting monkey avoidance also. Compound 2e was much less active than haloperidol in antagonizing apomorphine-induced emesis in dogs, apomorphine-induced stereotypy in rats, and amphetamine-induced circling in lesioned rats. This lack of nonselective, dopamine-receptor blocking effects makes 2e attrative as a potential neuroleptic.

Amphetamine↗
PubMed1978

2-Pyrrolidinylideneureas, a new class of central nervous system agents.

A series of N-aryl-N'-(1-methyl-2-pyrrolidinylidene)ureas was prepared and screened for pharmacological activity. Congeners possessing either phenyl or phenyl substituted with 4-nitro, 3-bromo, 3-chloro, 3-fluoro, and 3-methyl groups were found to demonstrate anxiolytic activity. 2,6-Disubstitution of the phenyl ring with methyl, chloro, and bromo imparted potent muscle-relaxant properties which appear to be centrally mediated. A significant separation of the anxiolytic and muscle-relaxant properties from other CNS activities, e.g., anticonvulsant, sedative, and hypnotic, was achieved.

Animals↗
PubMed1977

3-Aminotetrahydrocarbazoles as a new series of central nervous system agents.

3-Dimethylamino-1,2,3,4-tetrahydrocarbazole, a structurally modified tryptamine, prevented amphetamine-induced stereotyped behavior in rats and prevented reserpine-induced ptosis in mice. Further study of this compound and a number of substituted derivatives indicated that either imipramine-like or chlorpromazine-like profiles were obtainable by changing substituents and their positions.

Amphetamine↗
PubMed1979

Synthesis of spiro[isobenzofuran-1(3H),4'-piperidines] as potential central nervous system agents. 5. Conformationally mobile analogues derived by furan ring opening.

Synthesis and antitetrabenazine activity of 4-[2-(arylmethyl)phenyl]piperidines and 4-(benzyloxy)-4-phenylpiperidines, prepared as simplified and possibly more readily synthesized analogues of 3-phenylspiro[isobenzofuran-1 (3H),4'-piperidine], are reported. Several 4-[2-(arylmethyl)phenyl]piperidines display antitetrabenazine activity comparable to imipramine or amitriptyline but are two- to fourfold less active than analogous 3-arylspiro[isobenzofuran-1(3H),4'-piperidines]. Structure--activity relationships for 4-[2p(arylmethyl)phenyl]piperidines are generally similar to the profile established for 3-arylspiro[isobenzofuran-1(3H),4'-piperidines]. Significant antitetrabenazine activity is associated only with derivatives where the arylmethyl group is ortho to the piperidine ring. 4-(Benzyloxy)-4-phenylpiperidines and 4-[2-(arylmethyl)phenyl]-4-piperidinols and the corresponding methyl ethers and esters display weak to modest antitetrabenazine activity. 4-[2-(Arylmethyl)phenyl]-1,2,3,6-tetrahydropyridine derivatives, at best, exhibit modest antitetrabenazine activity, with the exception of 4-[2-(phenylmethyl)phenyl]-1,2,3,6-tetrahydropyridine which is approximately equipotent with amitriptyline. The results of these investigations allow certain speculations to be made with respect to the role of the furan ring in the 3-arylspiro[isobenzofuran-1(3H),4'-piperidines] and antitetrabenazine activity.

Animals↗
PubMed1977

Synthesis of spiro[isobenzofuran-1(3H),4'-piperidines] as potential central nervous system agents. 2. Compounds containing a heteroatom attached to nitrogen.

The synthesis and antitetrabenazine activity of a series of N-heteroatom derivatives of 3-phenylspiro[isobenzofuran-1,4'-piperidines] are reported. Optimal antitetrabenazine activity is associated with compounds containing a sterically unhindered, basic nitrogen. Hydroxylamines 6, 11, 12, and 13 possess the most significant activity with ED50's of 1.4, 3.5, 4.7, and 4.0, respectively.

Animals↗
PubMedDate not supplied

The human distribution of some barbiturate sedatives in combination with miscellaneous CNS-active drugs.

This paper presents 14 cases in which the distribution of barbiturates and the hydroxylated metabolites in combination with miscellaneous CNS-active drugs was studied. In 7 of these cases the other drug present was methadone, and in the remainder dihydrocodeine, morphine, propoxyphene, amitriptyline, meprobamate, cyclizine and dipipanone, diphenhydramine and methaqualine. Amitriptyline, methadone, cyclizine and dipipanone, methaqualone and diphenhydramine appeared to modify the distribution of amylorbarbitone and quinalbarbitone. Likewise, the barbituates seemed to alter the distribution of amitriptyline, propoxyphene and, in one instance, methadone.

Adult↗
PubMed1978

Effect of specimen storage and preservation on toxicological analyses of urine.

1. The stability of nineteen classes of drugs or their metabolites in urine specimens, for the purpose of toxicological screening has been studied for periods of up to thirty-six weeks. 2. The effect of specimen preservation by refrigation and by the addition of boric acid, chloroform, sodium fluoride, mercuric chloride, and buffers, has been assessed. 3. With the exception of flurazepam, glutethimide, and secobarbital, specimens may be retained at room temperature for periods in excess of six weeks without deterioration. 4. Preservation by the addition of sodium fluoride (5 g/l) followed by freezing, thawing, and filtration significantly prevents specimen deterioration, and may be used as the method of choice.

Central Nervous System Agents↗
PubMed1979

Adverse reactions to drugs in general practice.

Of 817 patients in a general-practice survey of adverse reactions to drugs, 41% were thought to have "certainly" or "probably" had a reaction to the drug prescribed. Adverse effects on the gastrointestinal and central nervous systems were the most frequently reported, and 90% of reactions had occurred by the fourth day of treatment. More patients given drugs acting on the central nervous system and antihistamines reported reactions than those in other categories. A higher incidence of adverse drug effects is shown in this general-practice survey than in other, mainly hospital-based, surveys. Further intensive surveillance for adverse effects of drugs is recommended to provide additional information on the burden of drug-induced disease in the community.

Adolescent↗
PubMed1978

Enzyme multiplied immunoassay technique: a review.

A brief review of the various immunoassays is presented before the basic mechanism of the enzyme multiplied immunoassay technique (EMIT) is described. This is followed by a presentation of the specific advantages and disadvantages of this method, as well as its correlation with other methods as applied to qualitative and quantitative determinations of each type of drug for which EMIT technology is available.

Central Nervous System Agents↗
PubMed1979

[Cesium].

Cesium is an alkaline metal close to Rubidium, which is studied in psychopharmacology in the prospect of a possible antidepressive effect. It has stimulating properties of the motor activity on the animal, antagonizes some sedative substances but does not modify either self-stimulation behaviour or induced agressivity. Given in large doses, Cesium presents hypertensive effects bound with a stimulation of the adrenal Epinephrine secretion. As for the synapses Cesium increases the neuro-transmitter release. However the Norepinephrine turn-over is not modified in the central nervous system while that of Serotonin is increased as well as the cerebral concentrations of Tryptophan, Serotonin and 5.HIAA. These very fragmentary data about the toxico-pharmacological properties of Cesium, as well as the very prolonged half-life of this ion (from 50 to 100 days), explain that contrary to Rubidium it has not still been used in man.

Animals↗