Results 101 to 110 of about 16,552 (150)

Pharmacophore development for antagonists at α1 adrenergic receptor subtypes

Journal of Computer-Aided Molecular Design, 1996
Many receptors, including alpha 1 adrenergic receptors, have a range of subtypes. This offers possibilities for the development of highly selective antagonists with potentially fewer detrimental effects. Antagonists developed for alpha 1A receptors, for example, would have potential in the treatment of benign prostatic hyperplasia.
John B. Bremner, Burak Coban, Renate Griffith   +2 more
openaire   +2 more sources

Receptor interactions of imidazolines. IX. Cirazoline is an alpha-1 adrenergic agonist and an alpha-2 adrenergic antagonist.

The Journal of Pharmacology and Experimental Therapeutics, 1982
The alpha-1 and alpha-2 adrenergic effects of cirazoline were evaluated in guinea-pig aorta and field-stimulated guinea-pig ileum, respectively. Cirazoline was found to be a full agonist at alpha-1 receptors having an ED50, dissociation constant (KA) and relative efficacy similar to that of (-)-norepinephrine.
R R, Ruffolo, J E, Waddell
openaire   +2 more sources

The impact of alpha-1-adrenergic receptor antagonists on the progression of Parkinson disease

Journal of the American Pharmacists Association
Alpha-1-adrenergic receptor antagonists (AARAs) are used in the treatment of benign prostatic hypertrophy. Some AARAs, such as terazosin, stimulate glycolysis and increase cellular adenosine triphosphate levels through activation of phosphoglycerate kinase 1 (PGK1), which has been suggested to be of therapeutic benefit in patients with Parkinson ...
Karla M. Opheim, Ergun Y. Uc, Matthew A. Cantrell, Brian C. Lund   +3 more
openaire   +2 more sources

Structure—Activity Relationships for alpha-1 Adrenergic Receptor Agonists and Antagonists

1987
Ahlquist (1948) proposed that adrenergic receptors could be classified into two separate subtypes, designated as alpha and beta and invoked this hypothesis to explain the varying effects of sympathomimetic amines. Subsequently, it became apparent that these classifications were inadequate because of the demonstration by Furchgott (1967) and Lands et al.
Robert M. DeMarinis, Margaret Wise, J. Paul Hieble, Robert R. Ruffolo   +3 more
openaire   +1 more source

Interaction Between Antidepressants and Alpha1-Adrenergic Receptor Antagonists on the Binding to Alpha1-Acid Glycoprotein

Journal of Pharmaceutical Sciences, 1986
alpha 1-Receptor antagonists and antidepressant agents are basic (cationic) drugs that are known to bind to alpha 1-acid glycoprotein (AAG). Since these drugs are frequently co-administered and since they bind to the same protein, this investigation was designed to evaluate the "in vitro" ability of antidepressants, alpha 1-receptor antagonists, and ...
D G, Ferry, N B, Caplan, L X, Cubeddu
openaire   +2 more sources

Reprint of: The impact of alpha-1-adrenergic receptor antagonists on the progression of Parkinson disease

Journal of the American Pharmacists Association
Alpha-1-adrenergic receptor antagonists (AARAs) are used in the treatment of benign prostatic hypertrophy. Some AARAs, such as terazosin, stimulate glycolysis and increase cellular adenosine triphosphate levels through activation of phosphoglycerate kinase 1 (PGK1), which has been suggested to be of therapeutic benefit in patients with Parkinson ...
Karla M. Opheim, Ergun Y. Uc, Matthew A. Cantrell, Brian C. Lund   +3 more
openaire   +2 more sources

Evidence for a central depressor action of postsynaptic α1-adrenergic receptor antagonists

Journal of the Autonomic Nervous System, 1981
The effects of alpha-adrenergic receptor antagonists on sympathetic nervous discharge (SND) recorded from the external carotid and splanchnic nerves were studied in baroreceptor intact and denervated cats. Prazosin (50 microgram/kg, i.v.) produced a rapid fall in mean arterial pressure (MAP) and no significant change in heart rate (HR) in baroreceptor ...
R B, McCall, S J, Humphrey
openaire   +2 more sources

Inhibition of α1-adrenergic responsiveness in intact cells by a new, irreversible receptor antagonist

Biochemical and Biophysical Research Communications, 1987
A novel alpha 1-adrenoreceptor antagonist, 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(2-bicyclo [2.2.2] octa-2,5-dienylcarbonyl) piperazine, was synthesized and shown to potently block alpha 1-adrenoceptor-induced Ca2+ mobilization in intact rat parotid acinar cells. Irreversible inhibition was complete in less than 5 min.
J, Helman, J W, Kusiak, J, Pitha, B J, Baum   +3 more
openaire   +2 more sources

Modeling the interactions between alpha(1)-adrenergic receptors and their antagonists.

Current computer-aided drug design, 2010
As crucial members of the G-protein coupled receptor (GPCR) superfamily, alpha (1)-adrenergic receptors (alpha(1)-ARs) are recognized to intervene the actions of endogenous catecholamines such as norepinephrine and epinephrine. So far three distinct alpha(1)-AR subtypes, alpha(1A), alpha(1B) and alpha(1D), have been characterized by functional analysis,
Lupei, Du, Minyong, Li
openaire   +1 more source

Suppression of experimental autoimmune uveoretinitis by prazosin, an α₁-adrenergic receptor antagonist

Current Eye Research, 1992
S-antigen (S-Ag)-induced experimental autoimmune uveoretinitis (EAU) was suppressed in Lewis and PVG rats by treatment beginning 4 days post immunization with prazosin, a specific alpha 1-adrenergic receptor antagonist. A significant suppression of EAU was observed at clinical and histological levels in both treated groups compared to a severe EAU ...
J M, Ruiz-Moreno, M, Misiuk-Hojlo, B, Thillaye, Y, de Kozak   +3 more
openaire   +2 more sources