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Chemical Compound Review

Lopac-B-003     N-[2,6-dichloro-4-[(2- chloroethyl-methyl...

Synonyms: CHEMBL326967, SureCN4107963, CCG-204290, Lopac0_000195, AC1L2XTB, ...
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Disease relevance of Chlorethylclonidine


Psychiatry related information on Chlorethylclonidine


High impact information on Chlorethylclonidine


Chemical compound and disease context of Chlorethylclonidine

  • In the non-PC groups, those with CEC (3 mg/kg, n = 7), 5-MU (3 mg/kg, n = 7), BN (0.3 mg/kg, n = 7), POB (4 mg/kg, n = 7), or placebo saline (n = 10) were pretreated before 30-min sustained ischemia [10].

Biological context of Chlorethylclonidine


Anatomical context of Chlorethylclonidine

  • Selective inactivation of alpha 1b receptors by chloroethylclonidine almost completely blocked the effects of norepinephrine in hepatocytes [15].
  • Preincubation of the membranes with chlorethylclonidine did not alter significantly the binding parameters for 5-[3H]methylurapidil [16].
  • Although other alkylating agents inactivated all of the alpha 1-adrenergic receptor-binding sites labeled with 125IBE 2254 in membrane preparations of cerebral cortex, chlorethylclonidine (CEC) potently and selectively inactivated only half of these sites [17].
  • To identify the responsible alpha1-AR subtype, we first documented the selectivity of two alpha1-AR subtype antagonists, BMY 7378 (alpha1D-AR antagonist) and chloroethylclonidine (CEC; alpha1B-AR antagonist), using Rat-1 fibroblasts stably transfected with the three different rodent alpha1-AR cDNAs [18].
  • Treatment of intact transfected COS-7 cells with chlorethylclonidine resulted in the inactivation of 19% of the alpha 1c-ARs, in contrast to 72% and 85% inactivation of the alpha 1a/d- and alpha 1b-ARs, respectively [19].

Associations of Chlorethylclonidine with other chemical compounds


Gene context of Chlorethylclonidine


Analytical, diagnostic and therapeutic context of Chlorethylclonidine


  1. Receptor-effector coupling pathway for alpha 1-adrenergic modulation of abnormal automaticity in 'ischemic' canine Purkinje fibers. Anyukhovsky, E.P., Steinberg, S.F., Cohen, I.S., Rosen, M.R. Circ. Res. (1994) [Pubmed]
  2. Alpha 1-adrenoceptor subtype affinities of drugs for the treatment of prostatic hypertrophy. Evidence for heterogeneity of chloroethylclonidine-resistant rat renal alpha 1-adrenoceptor. Michel, M.C., Büscher, R., Kerker, J., Kraneis, H., Erdbrügger, W., Brodde, O.E. Naunyn Schmiedebergs Arch. Pharmacol. (1993) [Pubmed]
  3. Chloroethylclonidine increases the incidence of lethal arrhythmias during coronary occlusion in anesthetized dogs. Geller, J.C., Cua, M., Prieto, L., Guo, S.D., Danilo, P., Rosen, M.R. Eur. J. Pharmacol. (1995) [Pubmed]
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  10. Infarct size-reducing effect of ischemic preconditioning is related to alpha1b-adrenoceptors but not to alpha1a-adrenoceptors in rabbits. Kariya, T., Minatoguchi, S., Ohno, T., Yamashita, K., Uno, Y., Arai, M., Koshiji, M., Fujiwara, T., Fujiwara, H. J. Cardiovasc. Pharmacol. (1997) [Pubmed]
  11. The alpha 1A-adrenergic receptor subtype mediates biochemical, molecular, and morphologic features of cultured myocardial cell hypertrophy. Knowlton, K.U., Michel, M.C., Itani, M., Shubeita, H.E., Ishihara, K., Brown, J.H., Chien, K.R. J. Biol. Chem. (1993) [Pubmed]
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  33. Characterization of alpha1-adrenoceptor subtypes mediating noradrenaline-induced contraction of rat epididymal vas deferens in calcium-free medium. Amobi, N.I., Sugden, D., Smith, I.C. Life Sci. (1999) [Pubmed]
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