Dihydroalprenolol

Hydrogenated alprenolol derivative where the extra hydrogens are often tritiated. This radiolabeled form of ALPRENOLOL, a beta-adrenergic blocker, is used to label the beta-adrenergic receptor for isolation and study.

Also Known As:

Networked: 41 relevant articles (0 outcomes, 6 trials/studies)

Bio-Agent Context: Research Results

Experts

1.	Benedito, Marco Antonio Campana: 1 article (09/2004)
2.	Pedrazzoli, Mario: 1 article (09/2004)
3.	Biagi, A: 1 article (08/2000)
4.	Bortoletto, M: 1 article (08/2000)
5.	Calci, M: 1 article (08/2000)
6.	Candido, R: 1 article (08/2000)
7.	Caretta, R: 1 article (08/2000)
8.	Fabris, B: 1 article (08/2000)
9.	Fischetti, F: 1 article (08/2000)
10.	Zaccaria, M: 1 article (08/2000)

Related Diseases

1.	Sepsis (Septicemia) 01/01/1999 - "The [(3)H]dihydroalprenolol binding studies show that the density of beta(2)-AR was decreased by 12 and 35% during the early and late phases of sepsis, respectively. " 09/30/1998 - "Changes in the distribution of beta-adrenoceptors (beta ARs) in the plasma membrane and the light vesicle fractions of rat liver during different phases of sepsis were studied using [3H]dihydroalprenolol binding and photoaffinity labeling with [125I]iodocyanopindolol diazirine. " 01/01/1996 - "Changes in the distribution of beta-adrenergic receptors in two subcellular fractions, the sarcolemma and the light vesicle, of rat heart during sepsis were studied, using [3H]dihydroalprenolol ([3H]DHA) binding and photoaffinity labeling with [125I]iodocyanopindolol ([125I]ICYP). "
2.	Heart Failure 12/01/1985 - "Despite a 44% increase in receptor density as measured by antagonist binding studies with [3H]dihydroalprenolol, there was a twofold decrease in receptor affinity, i.e., an increase in the dissociation constant (Kd) (5.6 +/- 0.7 to 12 +/- 1.6 nM) in heart failure. " 06/01/1990 - "In 14 patients with stable, class II-III heart failure we studied circulating lymphocytes to determine the number of beta adrenergic receptors, the dissociation constant of 3H dihydroalprenolol (kd) and the intracellular content of cyclic AMP (AMPc). " 12/01/1985 - "Agonist displacement of [3H]dihydroalprenolol binding with isoproterenol in the presence and absence of 5'-guanylylimidodiphosphate [Gpp(NH)p] demonstrated a striking loss of high affinity binding sites in heart failure (51 +/- 16 to 11 +/- 5%). " 10/03/1980 - "Compared with sham-operated guinea pigs, chronic heart failure produced by aortic constriction resulted in a 79% increase in alpha 1-adrenoceptor density as measured by [3H]prazosin binding (73 +/- 15 vs. 131 +/- 20 fmol/mg protein, P < 0.05); beta-adrenoceptor number, measured by (-)-[3H]dihydroalprenolol binding, increased by 93% (28 +/- 3.4 vs. 54 +/- 5.2 fmol/mg protein, P < 0.01). "
3.	Glioma (Gliomas) 03/01/1977 - "Use of (-)-[3H]dihydroalprenolol to study beta adrenergic receptor-adenylate cyclase coupling in C6 glioma cells: role of 5'-guanylylimidodiphosphate." 07/01/1986 - "The selectivity of [125I]iodopindolol, [125I]iodocyanopindolol, [125I]iodohydroxybenzylpindolol and [3H]dihydroalprenolol for beta-1 and beta-2 adrenergic receptors was assessed by inhibiting the binding of each radioligand with the beta-1-selective unlabeled ligand ICI 89,406 at increasing concentrations of the radioligand, using membranes prepared from C6 glioma cells, which have both beta-1 and beta-2 adrenergic receptors. " 12/09/1996 - "In neuroblastoma X glioma hybrid, NG1O8-15, cells transfected to stably express a constitutively active mutant (CAM) form of the human beta2-adrenoceptor, the beta-adrenoceptor ligands sotalol and betaxolol functioned as inverse agonists as they reduced basal adenylyl cyclase activity whereas the antagonists dihydroalprenolol and propranolol did not. "
4.	Tachycardia (Tachyarrhythmias) 01/01/1988 - "The pharmacological characterization of these compounds was performed in vitro by direct studies (3H-dihydroalprenolol was used as the specific ligand for beta-receptors), and by determining the beta-blocking capacity on isoproterenol (ISO)-induced increased heart rate (isolated guinea-pig atrium); and in vivo by evaluating the antagonism on ISO-induced hypotension and tachycardia, as well as the intrinsic sympathomimetic activity (ISA) on reserpinized and vagotomized rats. " 01/01/1981 - "Dexamethasone interfered with tyramine- and isoproterenol-induced tachycardia in the neonates but did not cause alterations in development of a marker for presynaptic sympathetic nerve terminals (synaptic vesicle uptake of [3H] norepinephrine) nor of postsynaptic beta adrenoceptor binding of [3H]dihydroalprenolol; the deficit was also unrelated to general cellular effects of the hormone. "
5.	Hypertension (High Blood Pressure) 02/01/1984 - "To study potential cardiac receptor alterations during the development of spontaneous hypertension, specific binding of [3H]-2-N(2,6-dimethoxyphenoxyethyl)amino-methyl-1,4-benzodioxane, (-)-[3H]dihydroalprenolol and (-)-[3H]quinuclidinyl benzilate in ventricles of Wistar Kyoto rats (WKY), spontaneously hypertensive rats (SHR) and stroke-prone SHR (SHRSP) at different ages was determined. " 01/01/1985 - "We studied adrenoreceptor density and affinity in the myocardial and pooled arterial smooth muscle membranes in a baboon model (Grollman 2-kidney, 2-figure-of-8) of hypertension, using tritiated prazosin (alpha 1-antagonist), yohimbine (alpha 2-antagonist) and dihydroalprenolol (beta-antagonist) as ligands. "

Related Drugs and Biologics

1.	beta Adrenergic Receptors
2.	Ligands
3.	Isoproterenol (Isoprenaline)
4.	Adrenergic beta-Antagonists (beta-Adrenergic Blocking Agents)
5.	Adenylyl Cyclases (Adenylyl Cyclase)
6.	Sympathomimetics (Sympathomimetic Amines)
7.	Quinuclidinyl Benzilate
8.	Hydrocortisone (Cortisol)
9.	Aldosterone
10.	Adrenergic Receptors (Adrenergic Receptor)

Related Therapies and Procedures

1.	Controlled Hypotension
2.	Ligation
3.	Denervation