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Chemical Compound Review

CHEMBL527515     2-(6,7-dimethoxy-3,4-dihydro- 1H...

Synonyms: TCMDC-131968, AC1Q6WCW, AR-1L5899, UK-52,046, UK-52046-27, ...
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Disease relevance of Abanoquil

  • With placebo, 4/6 dogs remained unchanged and 2 died: UK-52046 prevented arrhythmias in 2/6, 2 remained unchanged and 2 died (P = 0.29).(ABSTRACT TRUNCATED AT 400 WORDS)[1]
  • 5. In conclusion, significant alpha 1-adrenoceptor antagonism without marked reflex tachycardia or profound postural hypotension suggest that abanoquil has a different haemodynamic profile from that of 'classical' peripheral alpha 1-adrenoceptor antagonists [2].
  • 1. The haemodynamic effects of a new cardioselective postsynaptic alpha 1-adrenoceptor antagonist UK-52,046, were evaluated in 25 patients with stable coronary disease, with or without impaired left ventricular function [3].
  • Abanoquil at concentrations of 0.03, 0.1 and 0.3 microM tended to reduce the incidence of reperfusion-induced ventricular fibrillation (VF) in a dose-dependent manner from 75% in controls to 58, 33 and 25%, but this effects did not achieve statistical significance [4].
 

Psychiatry related information on Abanoquil

 

High impact information on Abanoquil

  • The pressor response to adrenaline was attenuated (P less than 0.05) by UK-52046, but resting blood pressure was unaffected by the different treatments [1].
  • An increase (P less than 0.01) in heart rate was associated with both UK-52046 and the combination [1].
  • 2. In a group of 6 dogs with multiventricular ectopic beats 24 h after coronary artery ligation (CAL), UK-52046, 32 micrograms kg-1, increased the number of sinus beats in each 5 min period from 137 +/- 47 to 662 +/- 99 (P less than 0.01); this was associated with a significant (P less than 0.01) fall in blood pressure [1].
  • 3. Abanoquil 0.25, 0.5 and 1 mg increased the PS20 in a dose-dependent manner with effects which were maximal at 2 to 8 h and lasted for 24 to 48 h (P less than 0.05) [6].
  • Studies with abanoquil (UK-52,046) a novel quinoline alpha 1-adrenoceptor antagonist: II. Duration of action, pharmacokinetics and concentration-effect relationships in normotensive subjects [7].
 

Chemical compound and disease context of Abanoquil

  • Effects of the myocardial-selective alpha 1-adrenoceptor antagonist UK-52046 and atenolol, alone and in combination, on experimental cardiac arrhythmias in dogs [1].
  • 1. Adrenaline-induced arrhythmias in anaesthetized dogs respired with halothane were attenuated in 3 groups of 6 dogs by either UK-52046, 3.8 +/- 1.4 micrograms kg-1 (mean +/- s.e.mean), atenolol 14.6 +/- 2.1 micrograms kg-1, or a combination containing equal amounts of the two drugs of 0.36 +/- 0.1 microgram kg-1 [1].
 

Biological context of Abanoquil

 

Associations of Abanoquil with other chemical compounds

  • Just prior to onset of VF, heart rate was not significantly different in the control and in the abanoquil tests (237 +/- 45 and 253 +/- 34 beats/min, respectively), whereas it was higher (P < 0.05) with prazosin (288 +/- 40 beats/min) [10].
  • 3. In the first study, abanoquil at a dose of 0.4 micrograms kg-1 i.v. (as a bolus or by increments) produced significant alpha 1-adrenoceptor antagonism (with rightward shifts of more than two-fold in the phenylephrine pressor dose-response curves) but no significant effects on supine or erect blood pressure and heart rate [2].
 

Analytical, diagnostic and therapeutic context of Abanoquil

References

  1. Effects of the myocardial-selective alpha 1-adrenoceptor antagonist UK-52046 and atenolol, alone and in combination, on experimental cardiac arrhythmias in dogs. Uprichard, A.G., Harron, D.W., Wilson, R., Shanks, R.G. Br. J. Pharmacol. (1988) [Pubmed]
  2. Studies with abanoquil (UK-52,046) a novel quinoline alpha 1-adrenoceptor antagonist: I. Effects on blood pressure, heart rate and pressor responsiveness in normotensive subjects. Schafers, R.F., Elliott, H.L., Howie, C.A., Reid, J.L. British journal of clinical pharmacology. (1991) [Pubmed]
  3. Haemodynamic dose-response effects of UK-52,046 in ischaemic disease with or without impaired left ventricular function. Silke, B., Zezulka, A.V., Verma, S.P., Tham, T.C., Taylor, S.H. British journal of clinical pharmacology. (1990) [Pubmed]
  4. Effects of selective alpha 1A-adrenoceptor antagonists on reperfusion arrhythmias in isolated rat hearts. Yasutake, M., Avkiran, M. Mol. Cell. Biochem. (1995) [Pubmed]
  5. Abanoquil, a new alpha-1 adrenoceptor antagonist. In vitro and in vivo effect on erectile tissue. Giraldi, A., Wyllie, M., Wagner, G. Int. J. Impot. Res. (2000) [Pubmed]
  6. Dose-dependent alpha 1-adrenoceptor antagonist activity of the anti-arrhythmic drug, abanoquil (UK-52,046), without reduction in blood pressure in man. Tham, T.C., Guy, S., Shanks, R.G., Harron, D.W. British journal of clinical pharmacology. (1992) [Pubmed]
  7. Studies with abanoquil (UK-52,046) a novel quinoline alpha 1-adrenoceptor antagonist: II. Duration of action, pharmacokinetics and concentration-effect relationships in normotensive subjects. Schafers, R.F., Elliott, H.L., Meredith, P.A., Miller, S.H., Reid, J.L. British journal of clinical pharmacology. (1991) [Pubmed]
  8. Effect of UK-52,046, an alpha 1-adrenoceptor antagonist, on baroreflex function in man. McKaigue, J.P., Harron, D.W. British journal of clinical pharmacology. (1990) [Pubmed]
  9. The sensitive determination of abanoquil in blood by high-performance liquid chromatography/atmospheric pressure ionization mass spectrometry. Kaye, B., Clark, M.W., Cussans, N.J., Macrae, P.V., Stopher, D.A. Biol. Mass Spectrom. (1992) [Pubmed]
  10. Alpha 1-adrenergic blockade and sudden cardiac death. Vanoli, E., Hull, S.S., Foreman, R.D., Ferrari, A., Schwartz, P.J. J. Cardiovasc. Electrophysiol. (1994) [Pubmed]
  11. Duration of action and effect on baroreflex function of the anti-arrhythmic alpha 1 antagonist UK-52,046. Spiers, J.P., Harron, D.W., Wilson, R. J. Pharm. Pharmacol. (1991) [Pubmed]
  12. Influence of acute alpha 1-adrenergic antagonism on heart rate variability in patients with old myocardial infarction. Toivonen, L. J. Cardiovasc. Pharmacol. (1994) [Pubmed]
 
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