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Biomedical subjects

J Pearl

Publications and source records attributed to J Pearl.

10 recordsLinked to original sources
PubMed1978

(exo, exo)-2-Aryltropane-3-carboxylic esters, hypoglycemic agents with accompanying analgesic activity.

(exo, exo)-2-Aryltropane-3-carboxylic esters of types 6, 7, and 10 lower circulating blood glucose levels by 60--80%. This activity is accompanied by an analgesic activity roughly equal to that of codeine. Both of these activities reside in the 1R enantiomer and extensive structure-activity studies failed to separate them. The specific opioid antagonist nalorphine blocks the analgesic activity but does not diminish the hypoglycemic action. Conformational integrity afforded by the ethylene bridge is neccessary for the observed activities.

Administration, Oral↗
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↗
PubMed1977

Parasympatholytic (anticholinergic) esters of the isomeric 2-tropanols. 1. Glycolates.

The 38 esters in Table I were prepared from the four isomeric 2-tropanols and a variety of racemic glycolic acids and their optical isomers. Anticholinergic activity in mice was measured in the peripheral nervous system (mydriasis) and in the central nervous system (anti-tremorine) and compared with that of atropine, scopolamine, and racemic 2-quinuclidinyl benzilate. The results (Table III) showed that several esters (such as 8, 12, 14, and 21) had significantly greater activity in both the peripheral and central nervous systems than did the reference compounds. Esters of (+)-2alpha-tropanol were more potent than those of either its epimer (-)-2beta-tropanol or its optical isomer(-)-2alpha-tropanol. Esters derived from (-)-glycolic acids were uniformly more potent than those from the (+)-glycolic acids. Esters of (+)-2alpha-notropanol and five of its N-substituted derivatives had markedly decreased activity. Peripheral/central activity ratios and time-activity profiles for five active compounds are discussed and compared with those of the reference compounds.

Animals↗
PubMed1976

Anticholinergic activity of antipsychotic drugs in relation to their extrapyramidal effects.

Antipsychotic drugs were evaluated with two indices of anticholinergic activity, mydriasis in mice in vivo and antagonism of carbamylcholine-induced contractions of guinea-pig tracheal strips in vitro. The drugs from most to least potent as oral mydriatic agents were mepazine, clozapine, thioridazine, promazine and chlorpromazine. Trifluoperazine, pimozide and haloperidol were inactive. These results were consistent with the hypothesis that anticholinergic activity of antipsychotic drugs is inversely related to their propensity to produce extrapyramidal effects in man. In vitro results appeared to predict the incidence of extraphyramidal effects less accurately than in vivo results.

Animals↗
PubMed1976

Boredom and arousal: comparison of tasks differing in visual complexity.

This experiment was designed to examine the relationship of boredom to arousal. 32 male subjects participated, with 16 subjects performing a low-visual-complexity task and the remainder performing a task high in visual complexity. Both physiological and subjective measures were obtained. Responses to subjective questionnaires showed significant increases in boredom for both groups. Physiological measures indicated a mixed pattern of change. These results suggest a complex response pattern for the construct of boredom which cannot be described as clearly showing either increasing or decreasing arousal.

Adolescent↗