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Chemical Compound Review

CHEMBL216097     2-(4,5-dihydro-1H-imidazol-2- ylmethyl)-1...

Synonyms: SureCN7596949, BRL-48553, BRL-48962, Brl-44408, AC1L3TIM, ...
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Psychiatry related information on Brl 48553


High impact information on Brl 48553

  • Rats underwent partial ligation of one sciatic nerve, and peri-neural saline, clonidine or a combination of clonidine and the alpha2A-adrenceptor-preferring antagonist, BRL44408, were administered before wound closure and, in some animals, also 24 and 48 h later [2].
  • In the porcine ciliary arteries BRL44408, ARC239, and prazosin caused concentration-dependent and parallel rightward shifts of the concentration-response curves for brimonidine [3].
  • In MAO-A KO mice, BRL 44408 (100 nm) increased evoked NA efflux on short trains while ARC 239 (100 nm) had no effect [4].
  • At 37 degrees C, alpha(2)-AR-induced vasoconstriction in distal arteries was inhibited by selective blockade of alpha(2A)-ARs (BRL-44408) but not by selective inhibition of alpha(2B)-ARs (ARC-239) or alpha(2C)-ARs (MK-912) [5].
  • The selective alpha(2)- versus alpha(1)-AR antagonists, atipamezole and BRL-44408 (a preferential alpha(2A)-AR antagonist), elevated levels of NE and DA but not 5-HT [6].

Biological context of Brl 48553

  • Alternative incubation in the presence of ARC 239 (50 nM) to mask alpha 2B-adrenoceptors or BRL 44408 (100 nM) to mask alpha 2D-adrenoceptors confirmed the existence of both alpha 2-adrenoceptor subtypes and a non-adrenoceptor imidazoline binding site [7].
  • The rank order of potency of antagonists in preventing dexmedetomidine- and oxymetazoline-evoked suppression of isoprenaline-induced lipolysis was (pA2-values): CH-38083 (7.69 and 7.48) congruent to idazoxan (7.5 and 7.41) > BRL44408 (7.23 and 7.19) congruent to WB4101 (7.13 and 7.12) > prazosin (5.18 and 5.17) > ARC-239 (4.72, 4.9) [8].

Anatomical context of Brl 48553

  • 2. The alpha 2B-selective adrenoceptor antagonists, prazosin, ARC 239 and HV 723 showed high, and the alpha 2A-selective antagonist BRL 44408 showed low, potency in human saphenous vein [9].
  • In agreement with the data of microdialysis and perfusion experiments, BRL 44408 displaced [3H]yohimbine from hippocampal and cortical membranes of rat brain with high affinity whereas ARC 239 was less effective [10].
  • The relatively non-selective alpha2-adrenoceptor antagonist yohimbine and the alpha2D-adrenoceptor selective antagonist BRL 44408 had potencies in rat atrium which were similar to their potencies in rat cerebral cortex [11].
  • In contrast, the antagonist BRL 44408 (alpha 2D selective, 1-10 mg/kg) did not increase the synthesis of dopa in cortex, and increased it modestly in hippocampus only [12].
  • The alpha 2B-selective adrenoceptor antagonists prazosin and ARC 239 showed significantly higher, and the alpha 2A-selective antagonist BRL 44408 showed significantly lower, potency in atrium than in vas deferens and submandibular gland [13].

Associations of Brl 48553 with other chemical compounds

  • The following antagonists were employed (potencies, pKB, in human saphenous vein in parentheses): chlorpromazine (6.98 +/- 0.24), BDF 8933 (7.60 +/- 0.06), prazosin (6.62 +/- 0.15), ARC 239 (7.19 +/- 0.15), yohimbine (7.23 +/- 0.09), HV 723 (7.52 +/- 0.14), WB 4101 (7.90 +/- 0.06), SKF 104078 (6.55 +/- 0.08), BRL 44408 (5.72 +/- 0.21) [14].
  • The same rank order was found for the affinities of these compounds for [3H]yohimbine binding in human platelet membranes, containing only alpha 2A-adrenoceptors, but does not correlate with the known affinities for alpha 2B-adrenoceptors (BRL-41992 > or = imiloxan > BRL-44408) [15].

Gene context of Brl 48553

  • The results indicate that BRL 44408 and ARC 239 recognize 5-HT1A receptors in addition to alpha 2-adrenoceptors [16].
  • Administration of the alpha2A-adrenoceptor antagonist BRL 44408 (1 mg/kg, i.p.) prevented amitriptyline and imipramine antinociception, whereas the alpha2B/C-adrenoceptor antagonist ARC 239 (10 mg/kg, i.p.) was ineffective [17].
  • The rank order of apparent EC50 values was BRL 44408 < BRL 41992 < WB-4101, and correlated best with constants for the alpha 2A-C10/alpha 2A adrenoceptor subtype [18].


  1. Effects of MDMA, MDA and MDEA on blood pressure, heart rate, locomotor activity and body temperature in the rat involve alpha-adrenoceptors. Bexis, S., Docherty, J.R. Br. J. Pharmacol. (2006) [Pubmed]
  2. Perioperative administration of the alpha2-adrenoceptor agonist clonidine at the site of nerve injury reduces the development of mechanical hypersensitivity and modulates local cytokine expression. Lavand'homme, P.M., Eisenach, J.C. Pain (2003) [Pubmed]
  3. Potent alpha(2A)-adrenoceptor-mediated vasoconstriction by brimonidine in porcine ciliary arteries. Wikberg-Matsson, A., Simonsen, U. Invest. Ophthalmol. Vis. Sci. (2001) [Pubmed]
  4. Different alpha(2) adrenoceptor subtypes control noradrenaline release and cell firing in the locus coeruleus of wildtype and monoamine oxidase-A knockout mice. Owesson, C.A., Seif, I., McLaughlin, D.P., Stamford, J.A. Eur. J. Neurosci. (2003) [Pubmed]
  5. Silent alpha(2C)-adrenergic receptors enable cold-induced vasoconstriction in cutaneous arteries. Chotani, M.A., Flavahan, S., Mitra, S., Daunt, D., Flavahan, N.A. Am. J. Physiol. Heart Circ. Physiol. (2000) [Pubmed]
  6. S18616, a highly potent spiroimidazoline agonist at alpha(2)-adrenoceptors: II. Influence on monoaminergic transmission, motor function, and anxiety in comparison with dexmedetomidine and clonidine. Millan, M.J., Lejeune, F., Gobert, A., Brocco, M., Auclair, A., Bosc, C., Rivet, J.M., Lacoste, J.M., Cordi, A., Dekeyne, A. J. Pharmacol. Exp. Ther. (2000) [Pubmed]
  7. [3H]RX821002 (2-methoxyidazoxan) binds to alpha 2-adrenoceptor subtypes and a non-adrenoceptor imidazoline binding site in rat kidney. Callado, L.F., Gabilondo, A.M., Meana, J.J. Eur. J. Pharmacol. (1996) [Pubmed]
  8. Functional evidence that alpha 2A-adrenoceptors are responsible for antilipolysis in human abdominal fat cells. Tarkovács, G., Blandizzi, C., Vizi, E.S. Naunyn Schmiedebergs Arch. Pharmacol. (1994) [Pubmed]
  9. Investigations of the subtype of alpha 2-adrenoceptor mediating contractions of the human saphenous vein. Smith, K., Connaughton, S., Docherty, J.R. Br. J. Pharmacol. (1992) [Pubmed]
  10. Subtype-specificity of the presynaptic alpha 2-adrenoceptors modulating hippocampal norepinephrine release in rat. Kiss, J.P., Zsilla, G., Mike, A., Zelles, T., Toth, E., Lajtha, A., Vizi, E.S. Brain Res. (1995) [Pubmed]
  11. Investigation of the subtypes of alpha2-adrenoceptor mediating prejunctional inhibition in rat atrium and cerebral cortex. Ho, S.L., Honner, V., Docherty, J.R. Naunyn Schmiedebergs Arch. Pharmacol. (1998) [Pubmed]
  12. Alpha 2-autoreceptors and alpha 2-heteroreceptors modulating tyrosine and tryptophan hydroxylase activity in the rat brain in vivo: an investigation into the alpha 2-adrenoceptor subtypes. Esteban, S., Lladó, J., García-Sevilla, J.A. Naunyn Schmiedebergs Arch. Pharmacol. (1996) [Pubmed]
  13. Investigations of prejunctional alpha 2-adrenoceptors in rat atrium, vas deferens and submandibular gland. Smith, K., Connaughton, S., Docherty, J.R. Eur. J. Pharmacol. (1992) [Pubmed]
  14. Alpha 2C-adrenoceptors mediate contractile responses to noradrenaline in the human saphenous vein. Gavin, K.T., Colgan, M.P., Moore, D., Shanik, G., Docherty, J.R. Naunyn Schmiedebergs Arch. Pharmacol. (1997) [Pubmed]
  15. Further studies on alpha 2-adrenoceptor subtypes involved in the modulation of [3H]noradrenaline and [3H]5-hydroxytryptamine release from rat brain cortex synaptosomes. Gobbi, M., Frittoli, E., Mennini, T. J. Pharm. Pharmacol. (1993) [Pubmed]
  16. The subtype-selective alpha 2-adrenoceptor antagonists BRL 44408 and ARC 239 also recognize 5-HT1A receptors in the rat brain. Meana, J.J., Callado, L.F., Pazos, A., Grijalba, B., García-Sevilla, J.A. Eur. J. Pharmacol. (1996) [Pubmed]
  17. Antinociception induced by amitriptyline and imipramine is mediated by alpha2A-adrenoceptors. Ghelardini, C., Galeotti, N., Bartolini, A. Jpn. J. Pharmacol. (2000) [Pubmed]
  18. Presynaptic alpha 2A-adrenoceptors regulate the 3H-noradrenaline secretion in the guinea-pig urethra. Alberts, P. Pharmacol. Toxicol. (1995) [Pubmed]
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