Drugs that bind to imidazoline binding proteins have major physiological actions. To date, three subtypes of such proteins, I(1), I(2) and I(3), have been proposed, although characterisations of these binding proteins are lacking. I(2) binding sites are found throughout the brain, particularly dense in the arcuate nucleus of the hypothalamus. Selective I(2) ligands demonstrate antidepressant-li...

Moxonidine, an antihypertensive imidazoline compound, reduces blood pressure by selective activation of central imidazoline I(1)-receptors and inhibition of sympathetic nerve activity and by direct actions on the kidney, with both mechanisms resulting in diuresis and natriuresis. We hypothesized that the hypotensive and renal actions of moxonidine may be mediated by atrial natriuretic peptide (...

The I(2) subgroup of imidazoline-binding sites was identified as monoamine oxidases (MAOs), but it is unclear whether there are I(2)-binding sites located on proteins distinct from MAOs. To address this issue, we characterized I(2)-binding proteins in liver and brain of wild-type and MAO A- and MAO B-deficient mice. I(2)-binding sites were identified using [(3)H]idazoxan and the photoaffinity a...

BACKGROUND Numerous agents have been demonstrated to potentiate morphine analgesia, including clonidine (alpha(2)-adrenergic and I(1)-imidazoline receptor agonist) and BMS182874 (endothelin-A, ET(A,) receptor antagonist). ET has been shown to affect pharmacological actions of clonidine. The present study was conducted to determine whether alpha(2)-adrenergic and/or I(1)-imidazoline receptors ar...

Chronic stimulation of sympathetic nervous activity contributes to the development and maintenance of hypertension, leading to left ventricular hypertrophy (LVH), arrhythmias and cardiac death. Moxonidine, an imidazoline antihypertensive compound that preferentially activates imidazoline receptors in brainstem rostroventrolateral medulla, suppresses sympathetic activation and reverses LVH. We h...

Two types of chelating fibers containing an imidazoline or thioamide group were prepared through the functionalization of hydrazine-modified polyacrylonitrile fiber by ethylenediamine and through the amination and sulfurization reaction of the hydrazine-modified polyacrylonitrile fiber under appropriate conditions, respectively. It is shown that the reaction temperature, time, and agent concent...

BACKGROUND We have recently described the synthesis and circulatory properties of two novel centrally acting imidazoline agents: marsanidine (1-[(imidazolidin-2-yl)imino]indazole) and 7-Me-marsanidine (1-[(imidazolidin-2-yl)imino]-7-methylindazole). Marsanidine has proven to be a highly selective α2-adrenoceptor ligand with the α2/I1 selectivity ratio of 3879, while 7-Me-marsanidine has been sh...

A model for computing image ow in image sequences containing a very wide range of instantaneous ows is proposed. This model integrates the spatio-temporal image derivatives from multiple temporal scales to provide both reliable and accurate instantaneous ow estimates. The integration employs robust regression and automatic scale weighting in a generalized brightness constancy framework. In addi...

DABCO-catalyzed [3 + 2] annulation reaction of sulfamate-derived cyclic imines with isocyanoacetate proceeds under mild conditions, providing sulfamate-fused 2-imidazolines in moderate to excellent yields with moderate to excellent diastereoselectivities.