Charles R. Thompson

Studies on Estrogen Tri-p-anisylchloroethylene:

Summary The pharmacology of Tace (tri-p-anisylchloroethylene), a new compound with estrogenic activity, differs in important respects from that of hexestrol which is typical of the natural and better known synthetic estrogens: (1) Tace does not cause and hexestrol does cause pituitary enlargement in rats; (2) Tace has a lesser but similar effect to hexestrol on organs in which the action of the two compounds is mediated through the pituitary; (3) fat storage resulting in long activity occurs following oral administration of large doses of Tace, while there is no fat storage and action is short following hexestrol administration; (4) estrogenic material equivalent in biologic potency to more than the administered dose of Tace is eliminated with the feces, while only small amounts of estrogenic material are eliminated following hexestrol administration.

Effect of drugs on the cardiac conditioned response of dogs

Abstract Dogs were conditioned to an anxiety response characterized by an increase in heart rate upon presentation of a musical tone. Meprobamate, chlordiazepoxide and diazepam effectively prevented the cardiac conditioned response. Phenobarbital and chlorpromazine were less effective. Amphetamine, 1.5 mg kg orally, also blocked the cardiac conditioned response. Atropine, meperidine, caffeine, imipramine and α-methyl-dopa had no effect on the cardiac conditioned response. Morphine and methyl phenidate were clearly active only in doses producing marked side effects. Ethanol in relatively small doses was mildly effective.

Fat Stsorage of an Estrogen in Women Following Orally Administered tri-p-anisylchloroethylene

Summary The repeated oral administration of TACE to human subjects results in storage of considerable amounts of estrogenic material in the body fat. This material remains in the fat for prolonged periods following cessation of TACE therapy. Results of studies in a limited number of cases suggest that both duration of therapy and the size of the doses are contributing factors governing the level of estrogenic material in the fat.

Etoxadrol (CL-1848C) a new dissociative anesthetic: studies in primates and other species.

L-l848C, the dextrorotatory isomer of c 2-ethyl-2-phenyl-4(2-piperidyl) (1,3dioxolane hydrochloride) from the dace mate, is a new agent which in primates has anesthetic properties similar to those of ketamine. The overt effects of CG1848C and ketamine in other animal species are also similar. Ketamine has been reported to induce in man a profound analgesia and somnolence,’ for which Domino and associates2 first proposed the term “dissociative anesthetic.”

Determination of Antialdosterone Activity in Adrenalectomized Dogs

Summary A method is described for detecting an aldosterone antagonist in unanesthetized adrenalectomized dogs maintained on long-acting replacement therapy. Using this method, spironolactone blocked mineralocorticoid effects on both Na and K excretion. The characteristics of the aldosterone antagonist were readily differentiated from those of a diuretic, chlorothiazide, by demonstration of qualitatively different effects on K excretion.

Anti-inflammatory activity of amidines of substituted triphenylethylenes☆

Abstract The anti-inflammatory activity of a new series of amidines and the expanded pharmacology of the prototype of this series, 1-1-bis-( p -anisyl)-2-( p -guanylphenyl)-ethylene (MER-13), is reported. The anti-inflammatory activity of MER-13 resembles that of cortisone acetate and differs from that of the gold salts and the salicylates. The only difference observed between the anti-inflammatory activity of MER-13 and cortisone acetate was a dose-response relationship for cortisone acetate in inhibiting granuloma formation and the lack of a dose-response relationship for MER-13 and the low order of oral potency possessed by MER-13. MER-13 is devoid of the other endocrine activities of the glucocorticoids. Acute and subacute toxicity studies are reported for MER-13.