Under controlled conditions the effects of various “sympatholytic” agents on the cardiovascular responses to epinephrine and norepinephrine were compared in man. The dosages of the sympatholytic drugs administered approximated those usually employed clinically. Such basic data are given for the following agents: Dibenamine, the imidazoline derivatives [Priscoline and Regitine (C-73i)], the dihy...

Six novel imidazoline derivatives were synthesized and tested in antifungal assays. One of the compounds, N-cyclohexyl-2-imino-3-(4-nitrophenyl)imidazolidine-1-carboxamide showed moderate activity against several clinical strains of Candida albicans. Its structure was solved by X-ray crystallography and its mode of action was deduced using molecular modelling. It was found to be similar to that...

Under controlled conditions the effects of various "sympatholytic" agents on the cardiovascular responses to epinephrine and norepinephrine were compared in man. The dosages of the sympatholytic drugs administered approximated those usually employed clinically. Such basic data are given for the following agents: Dibenamine, the imidazoline derivatives [Priscoline and Regitine (C-7337)], the dih...

Tetryzoline(TH) is an adrenergic agent (vasoconstrictors) and derived from imidazoline. This compound is closely related to naphazoline hydrochloride in its pharmacological action. Nanotechnology has been used to provide advanced biomedical research tools in drug delivery. The fullerene family especially C60 derivatives have appealing photo-, electro-chemical and physical properties for biomedi...

The discovery of imidazoline ligands has opened up a new field of study. The investigation of imidazoline actions independent of adrenoceptors started in the mid 1980s. Imidazoline receptors are classified in several subtypes, I1, I2 and I3 binding sites. Although imidazoline sites have been the subjects of research for several years, but there is still controversy about their actions especiall...

The agonists of imidazoline I-1 receptors (I-1R) are widely used to lower blood pressure. It has been indicated that guanidinium derivatives show an ability to activate imidazoline receptors. Also, allantoin has a chemical stricture similar to guanidinium derivatives. Thus, it is of special interest to characterize the effect of allantoin on I-1R. In conscious male spontaneous hypertensive rats...

The geometries of various tautomers and isomers of 2-methylamino-2-imidazoline, 2-methylamino-2oxazoline, 2-methylamino-2-thiazoline, 2-phenylamino-2-imidazoline, 2-phenylamino-2-oxazoline, and 2-phenylamino-2-thiazoline have been studied using the Becke3LYP/6–31+G(d,p) DFT, ONIOM(Becke3LYP/6–31+G(d,p):HF/3–21G∗) and ONIOM(Becke3LYP/6–31+G(d,p):AM1) methods. The optimized geometries indicate th...

The selectivity of tizanidine to the imidazoline-receptor and alpha 2-adrenoceptor recognized by 3H-p-aminoclonidine was examined in rat kidney membranes and was compared with those of other imidazoline compounds. Tizanidine bound to the imidazoline-receptors with approximately 20 times higher affinity than the alpha 2-adrenoceptors. The order of relative selectivity to imidazoline receptor was...