Accumulation of caffeine in healthy volunteers treated with furafylline.

The pharmacokinetics and tolerance of repeated oral doses of furafylline were investigated in normal volunteers. In accord with predictions from single dose studies, steady state was achieved on the first day following the administration of 90 mg and maintained by subsequent daily doses of 30 mg. When corrected for body weight there were no significant differences in minimum and maximum plateau levels of furafylline between males (1.

Characterization of a new crystalline synthetic gastric antacid, almagate.

A new crystalline hydrated aluminium-magnesium hydroxycarbonate, almagate (Almax) is described. It has been shown to have an empirical formula Al2 Mg6(OH)14(CO3)2 X 4 H2O X. X-ray diffraction spectra indicate that it is different from other related antacids and that its crystal structure is made up of brucite layers, in which magnesium is replaced by aluminium in the ratio of 3 to 1, interposed with negatively charged layers containing carbonate ions and water.

Evaluation of a new antacid, almagate.

Almagate (Al2Mg6(OH)14(CO3)2 X 4 H2O, Almax), a crystalline hydrated aluminium-magnesium hydroxycarbonate, was compared with a number of other known antacids in a battery of tests designed to demonstrate the properties of an ideal antacid. In dynamic tests for measurement of velocity of neutralization, total acid consuming capacity and duration of activity, almagate like other crystalline aluminium magnesium hydroxide derivatives such as hydrotalcite and magaldrate was rapidly acting, neutralized a high proportion of its theoretical acid consumption and maintained gastric pH between 3 and 5 for a prolonged period of time. It was more active than these two substances in respect of rapidity of action and did not lose antacid activity as the pH was raised.

Dopaminergic activity in a series of N-substituted 2-aminopyrimidines.

A series of N-substituted 2-aminopyrimidines were prepared and tested for pharmacological activity associated with stimulation of central and peripheral dopamine receptors using piribedil as the reference standard. Most of the new compounds showed some degree of dopaminergic activity although in many cases central activity was not accompanied by peripheral activity and vice versa. Clear relationships between structure and activity were not apparent and none of the new compounds possessed dopamine receptor blocking properties.

Synthesis and pharmacological properties of a series of antidopaminergic piperidyl benzamides.

The synthesis and pharmacological screening for anti-apomorphine, stomach emptying and local anaesthetic activities of some new piperidylbenzamides is described. One of these, N-(1'-benzyl-4'-piperidyl)-2-methoxy-4-amino-5-chlorobenzamide (clebopride) is more potent than metoclopramide in tests related to blockade of cerebral dopamine receptors.