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Chemical Compound Review

Carazolol     1-(9H-carbazol-4-yloxy)-3- (propan-2...

Synonyms: Conducton, Suacron, Carazololum, Conducton (TN), SureCN77901, ...
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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


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


  1. Carazolol: a potent, selective beta 3-adrenoceptor agonist. Méjean, A., Guillaume, J.L., Strosberg, A.D. Eur. J. Pharmacol. (1995) [Pubmed]
  2. Simple fluorimetric screening for carazolol in swine kidneys by means of Sep-Pak cartridges. Engelsma, J.W., Simons, J. The Veterinary quarterly. (1985) [Pubmed]
  3. beta 1 Selectivity of drugs: quality of the drug or quality of the patient? von Wichert, P., Perkow, I., Teufel, W. Respiration; international review of thoracic diseases. (1980) [Pubmed]
  4. Characterization of the binding domain of the beta-adrenergic receptor with the fluorescent antagonist carazolol. Evidence for a buried ligand binding site. Tota, M.R., Strader, C.D. J. Biol. Chem. (1990) [Pubmed]
  5. Specific beta-adrenergic receptor binding of carazolol measured with PET. Berridge, M.S., Nelson, A.D., Zheng, L., Leisure, G.P., Miraldi, F. J. Nucl. Med. (1994) [Pubmed]
  6. Development of a rapid screening test for veterinary sedatives and the beta-blocker carazolol in porcine kidney by ELISA. Cooper, J., Delahaut, P., Fodey, T.L., Elliott, C.T. The Analyst. (2004) [Pubmed]
  7. Control of prostaglandin-induced parturition in sows by injection of the beta-adrenergic blocking agent carazolol or carazolol and oxytocin. Holtz, W., Schmidt-Baulain, R., Meyer, H., Welp, C. J. Anim. Sci. (1990) [Pubmed]
  8. Stereotypic behavior and heart rate in pigs. Schouten, W., Rushen, J., De Passillé, A.M. Physiol. Behav. (1991) [Pubmed]
  9. (S,S)- and (S,R)-1'-[18F]fluorocarazolol, ligands for the visualization of pulmonary beta-adrenergic receptors with PET. Elsinga, P.H., Vos, M.G., van Waarde, A., Braker, A.H., de Groot, T.J., Anthonio, R.L., Weemaes, A.A., Brodde, O.E., Visser, G.M., Vaalburg, W. Nucl. Med. Biol. (1996) [Pubmed]
  10. Pharmacokinetics of intravenously, intramuscularly and intra-adiposely administered carazolol in pigs. Kadir, F., Zuidema, J., Pijpers, A., Melendez, R., Vulto, A., Verheijden, J.H. J. Vet. Pharmacol. Ther. (1990) [Pubmed]
  11. High affinity of carozolol for beta-adrenoceptors coupled to the adenylyl cyclase in ventricular myocardium of kitten and Xenopus laevis. Morris, T.H., Birnbaumer, L., Kaumann, A.J. Naunyn Schmiedebergs Arch. Pharmacol. (1978) [Pubmed]
  12. Adrenergic stimulation and blocking of hormonal secretion activity of cultured cow granulosa cells. Gajewski, Z., Faundez, R., Thun, R., Pawliński, B. J. Physiol. Pharmacol. (2006) [Pubmed]
  13. Influence of supplemental magnesium, tryptophan, vitamin C, and vitamin E on stress responses of pigs to vibration. Peeters, E., Neyt, A., Beckers, F., De Smet, S., Aubert, A.E., Geers, R. J. Anim. Sci. (2005) [Pubmed]
  14. Tyr199 in transmembrane domain 5 of the beta2-adrenergic receptor interacts directly with the pharmacophore of a unique fluorenone-based antagonist. Wu, Z., Thiriot, D.S., Ruoho, A.E. Biochem. J. (2001) [Pubmed]
  15. Competitive and non-competitive interactions between specific ligands and beta-adrenoceptors in living cardiac cells. Porzig, H., Becker, C., Reuter, H. Naunyn Schmiedebergs Arch. Pharmacol. (1982) [Pubmed]
  16. Determination of tranquilisers and carazolol residues in animal tissue using high-performance liquid chromatography with electrochemical detection. Rose, M.D., Shearer, G. J. Chromatogr. (1992) [Pubmed]
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