1,3-Diacylaminopropan-2-ols and corresponding 2-acyl derivatives as drug carriers: unexpected pharmacological properties.

The design of lipid vectors (pseudotriglycerides, PTGs), achieved by the amide isosteric substitution of the ester moieties of 1,3-diacylglycerols, is based on the structural similarity with natural triglycerides facilitating the passage of pharmacological agents across biological membranes. 2-S-Acetylthiorphan (hemiacetorphan) pseudotriglycerides, Z-glycine pseudotriglycerides and 1,3-diacylaminopropan-2-ols vector molecules differing by the nature of the acid side-chain are examined in acute toxicity, radioligand binding and guinea-pig ileum experiments. These evaluations have led us to distinguish two types of compounds.

A comparison of the inotropic effects of dopamine and epinine in human isolated cardiac preparations.

The positive inotropic effects of epinine and dopamine have been studied in isolated preparations obtained from human heart in the absence and in the presence of the selective beta adrenoceptors antagonists practolol and ICI 118,551. ED50 values of the two agonists were similar (about 3 x 10(-5) M). The inotropic efficacy of epinine was significantly higher than that of dopamine in adult ventricular and papillary muscles, it was similar to that of dopamine in juvenile myocardial preparations and in adult atria and pectinate muscles.

Effect of parathyroidectomy on development of hypertension and atrial responsiveness in spontaneous hypertensive rats.

1. In order to further clarify the relationships between parathyroid function and development of hypertension, the effects of parathyroidectomy (PTX) on blood pressure and on responsiveness of atria isolated from spontaneous hypertensive rats (SHR) were examined. 2.

Role of Na-H exchange in the inotropic action of Bay K 8644 and of ouabain in guinea-pig isolated atria.

1. The inotropic effects of two concentrations of ouabain and of Bay K 8644 have been studied in isolated left atria of the guinea-pig in physiological solutions at pH lowered from 7.4 to 6.

Competitive and stereoselective histamine H1 antagonistic effect of cicletanide in guinea-pig isolated ileum.

The histamine H1 antagonistic effects of the racemic form and the enantiomers of cicletanide, a new antihypertensive furopyridine derivative, were investigated in guinea-pig isolated ileum. Both the racemic and the (-) enantiomer behaved as competitive histamine antagonists (pA2 values of 6.8 and 7.