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Chemical Compound Review

CHEMBL114166     8-chloro-4-methyl-11-(3- methylbut-2-enoxy)...

Synonyms: AG-D-28602, SureCN8091302, ACMC-20mdr0, CHEBI:290658, C16H22ClNO, ...
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Disease relevance of Skf 104078


High impact information on Skf 104078


Biological context of Skf 104078


Anatomical context of Skf 104078

  • The high affinity of SK&F 104078 for postjunctional alpha-2 adrenoceptors in the canine saphenous vein was confirmed by its ability to inhibit [3H]rauwolscine binding to postjunctional alpha-2 adrenoceptors in this tissue [9].
  • The results indicate that vascular neuroeffector transmission in rat hindlimb is mediated by postjunctional alpha 1-adrenoceptors, and that SK&F 104078 is a selective antagonist of postjunctional alpha 2-adrenoceptor, and lacks the prejunctional alpha 2-adrenoceptor antagonist action of rauwolscine [7].
  • These findings imply a negative inotropic effect of SK&F 104078 in metabolically vasodilated myocardium in the vicinity of an acute ischemic region [10].
  • Regional myocardial performance was measured by ultrasonic crystals in the anterior wall perfused by the left anterior descending coronary artery (LAD) before and during postjunctional alpha-adrenergic antagonism (SK&F 104078 2 mg/kg) [10].
  • Pretreatment of iris root/ciliary bodies with SKF 104078 or rauwolscine reversed the inhibitory effect of UK on isoproterenol- and VIP-induced accumulation of cAMP [11].

Associations of Skf 104078 with other chemical compounds


Gene context of Skf 104078

  • SK&F 104078 had moderate affinity towards alpha 2-adrenoceptors (pKi 6.7) but displayed higher affinity at 5-HT1A (pKi 8.1) and 5-HT2 (pKi 7.6) receptors [6].

Analytical, diagnostic and therapeutic context of Skf 104078


  1. Cardiovascular effects of SKF 104078 in lambs. Chappell, B., Padbury, J., Martinez, A., Habib, D., Stein, H., Oyama, K. Developmental pharmacology and therapeutics. (1991) [Pubmed]
  2. Characterization of alpha 2 adrenoceptors and other adrenoceptors in membranes isolated from dog mesenteric nerve axons. Daniel, E.E., Gaspar, V., Berezin, I., Kwan, C.Y. J. Pharmacol. Exp. Ther. (1995) [Pubmed]
  3. Ability of SK&F 104078 and SK&F 104856 to identify alpha-2 adrenoceptor subtypes in NCB20 cells and guinea pig lung. Gleason, M.M., Hieble, J.P. J. Pharmacol. Exp. Ther. (1991) [Pubmed]
  4. Alpha 2-adrenoceptor blocking profile of SK&F 104078: further evidence for receptor subtypes. Akers, I., Coates, J., Drew, G.M., Sullivan, A.T. Br. J. Pharmacol. (1991) [Pubmed]
  5. No evidence for differences between pre- and postjunctional alpha 2-adrenoceptors in the periphery. Connaughton, S., Docherty, J.R. Br. J. Pharmacol. (1990) [Pubmed]
  6. The alpha 2-adrenoceptor antagonist SK&F 104078 has high affinity for 5-HT1A and 5-HT2 receptors. Kilpatrick, A.T., Brown, C.M., MacKinnon, A.C., Spedding, M. Eur. J. Pharmacol. (1989) [Pubmed]
  7. Characterization of alpha-adrenoceptors mediating sympathetic vasoconstriction in rat autoperfused hindlimb: effects of SK&F 104078. Medgett, I.C., Ruffolo, R.R. Eur. J. Pharmacol. (1987) [Pubmed]
  8. Cardiovascular effects of SK&F 104078, a novel alpha-adrenoceptor antagonist, in normotensive and hypertensive rats. Hieble, J.P., Sulpizio, A.C., Gutzait, L., Gombar, C.T. J. Cardiovasc. Pharmacol. (1990) [Pubmed]
  9. Evidence for heterogeneity between pre- and postjunctional alpha-2 adrenoceptors using 9-substituted 3-benzazepines. Daly, R.N., Sulpizio, A.C., Levitt, B., DeMarinis, R.M., Regan, J.W., Ruffolo, R.R., Hieble, J.P. J. Pharmacol. Exp. Ther. (1988) [Pubmed]
  10. Postjunctional alpha-adrenergic stimulation of inotropy in hypoperfused myocardium outside an acute infarct. Westby, J., Birkeland, S., Hexeberg, E., Lekven, J., Grong, K. J. Cardiovasc. Pharmacol. (1992) [Pubmed]
  11. Pharmacological evidence for heterogeneity of ocular alpha 2 adrenoceptors. Crosson, C.E., Heath, A.R., DeVries, G.W., Potter, D.E. Curr. Eye Res. (1992) [Pubmed]
  12. Evidence for heterogeneity of prejunctional alpha-2-adrenoceptors. Oriowo, M.A., Hieble, J.P., Ruffolo, R.R. Pharmacology (1991) [Pubmed]
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