Disease relevance of Conducton hydrochloride

• Carazolol is a beta1/beta2 adrenoceptor antagonist of high potency used in the treatment of hypertension [1].
• Injection of 10 micrograms/kg body weight, 105 minutes before slaughter, resulted in carazolol contents in kidneys ranging from 11 to 25 micrograms/kg (n = 8) [2].
• In two groups of patients with well-defined obstructive lung disease - a group of bronchitics according to WHO criteria and a group of patients with extrinsic allergic asthma - the effect of carazolol, a so-called non-cardioselective beta-blocking drug, was investigated [3].
• Carazolol increased bronchial resistance in the bronchitic group but not in the asthmatic group; with the exception of 1 patient in whom carazolol induced a status asthmaticus [3].

High impact information on Conducton hydrochloride

• Characterization of the binding domain of the beta-adrenergic receptor with the fluorescent antagonist carazolol. Evidence for a buried ligand binding site [4].
• The fluorescence properties of carazolol are dominated by the emission of the carbazole group, with the fine structure of the spectrum, but not the quantum yield, sensitive to the environment of the probe [4].
• Dose-dependent competition showed that carazolol binds in vivo to beta 1 and to beta 2 subtypes [5].
• Kidney samples (2.5 g) were extracted with dichloromethane and applied to a competitive enzyme immunoassay using three polyclonal antibodies raised in rabbits against azaperol, propionylpromazine and carazolol conjugates [6].
• For regulatory control purposes, tolerances for azaperone and carazolol have been set by the European Union as 100 and 25 [micro sign]g kg(-1), respectively [6].

Biological context of Conducton hydrochloride

• Furthermore, in murine adipocyte-like 3T3-F442A cells, which express beta 3-adrenoceptor naturally, carazolol induced lipolysis [1].
• Treatment with 3 mg of carazolol alone caused parturition to commence within 2.6 +/- .23 (SEM) h after injection [7].
• This response was partly blocked by a beta-adrenoreceptor antagonist (carazolol), but not by naloxone, although the latter tended to lead to overall increases in heart rate [8].
• The beta-adrenoceptor antagonist carazolol has been labelled with fluorine-18 in the isopropyl group via a reductive alkylation by [18F]-fluoroacetone of the corresponding (S)-desisopropyl compound according to a known procedure [9].
• Pharmacokinetics of intravenously, intramuscularly and intra-adiposely administered carazolol in pigs [10].

Anatomical context of Conducton hydrochloride

• Catecholamine-induced stimulation of adenylyl cyclase in ventricular membranes of kitten and Xenopus laevis was antagonized competitively by carazolol [11].
• The aim of this study was to determine the influence of alpha- and beta-stimulators (alpha-stimulator: detomidinum HCl) as well as blockers (alpha1-blocker: doxazosin, alpha2-blocker: yohimbinum HCL, beta-blocker: carazolol) on bovine granulosa cells culture from preovulatory follicles [12].
• The effect of vit C and E as vagal stimulators was clearly visible, whereas carazolol and Mg clearly blocked the sympathetic pathways of the autonomic nervous system [13].

Associations of Conducton hydrochloride with other chemical compounds

• To identify receptor amino acids that contribute to the beta2AR antagonist binding site, we identified the precise amino acid photoinsertion site of a novel carazolol-like fluorenone antagonist photoaffinity label, [125I]iodoaminoflisopolol ([125I]IAmF) [14].
• We conclude that by applying carazolol 20 h after a prostaglandin analog, parturition in swine may be terminated very effectively [7].

Gene context of Conducton hydrochloride

• The apparent KD values for (-)-isoprenaline were 1560 and 2720 nmol/l in the presence of carazolol and CYP, but only 32 nmol/l in the presence of CGP 12177 [15].

Analytical, diagnostic and therapeutic context of Conducton hydrochloride

• Determination of tranquilisers and carazolol residues in animal tissue using high-performance liquid chromatography with electrochemical detection [16].
• Development of a rapid screening test for veterinary sedatives and the beta-blocker carazolol in porcine kidney by ELISA [6].
• In this study carazolol pharmacokinetics were investigated in a randomized three-way cross-over design in five pigs [10].

References