Alan A. Rubin

New Class of Antihypertensive Agents

Effective antihypertensive agents of the benzothiadiazine series, devoid of diuretic activity, are described. There follows a method of synthesis and a description of the pharmacological activity of one of these substances

Psychopharmacological Profile of Molindone

RECENT clinical reports1–3 have indicated that the combination of a neuroleptic and an antidepressant affords an added measure of therapeutic effectiveness in the treatment of certain mental disorders. In the course of our investigations on new psychoactive agents, we have found a compound (molindone hydrochloride, EN-1733A) with a profile in animals which predominantly resembles that of the neuroleptics and yet which contains some of the elements characteristic of antidepressants. Chemically, molindone (3 - ethyl - 6,7 - dihydro - 2 - methyl - 5-morpholino - methylindol - 4 - (5H) - one) is unlike any of the psycho therapeutic drugs at present available.

Effects of fenoprofen and aspirin on gastrointestinal microbleeding in man.

The 51Cr‐labeled erythrocyte assay was used to compare the effects of equipotent doses of fenoprofen and aspirin—600 mg.:1 Gm.; 400 mg.:650 mg. Based on the appearance of label in the feces of normal men, we conclude that (1) both fenoprofen and aspirin produced measurable gastrointestinal microbleeding in man and (2) the amount of microbleeding after fenoprofen was significantly less than that after the aspirin preparations used in this study.

Hemodynamic Aspects of Certain Antihypertensive Agents

Ideally, an antihypertensive agent should correct the fundamental defects which have led to the development of hypertensive disease. That such an agent is not available reflects the current state of our knowledge regarding the etiology of this disease. Little is known about the genetic organization of a susceptible individual, the intermediate processes responsible for the hemodynamic and pathologic changes or the factors that precipitate the overt signs of hypertension. Consequently, the traditional pharmacologic approach to the treatment of hypertension has been an empirical one, consisting essentially of a search for agents that lower blood pressure without causing unfavorable side effects. This report will be concerned with an evaluation of the major hemodynamic properties of some of these agents and the relevant implications for future pharmacologic emphasis in this area. It is generally recognized that the primary hemodynamic change in hypertension is the elevation of peripheral vascular resistance and that, furthermore, this change results from a diffuse arteriolar narrowing. The heart adjusts to the higher resistance by increasing its force of contraction, thereby maintaining an adequate flow of blood to the body tissues. Thus, although the load on the heart is increased, cardiac output, total blood volume and peripheral blood flow remain within normal limits.