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Chemical Compound Review

Azepexol     4-ethyl-10-oxa-4,8- diazabicyclo[5.3.0]deca...

Synonyms: azepoxol, Azepexole, Azepexolum, Lopac-B-161, CHEMBL149616, ...
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Disease relevance of B-HT 920

  • Pre-treatment of arteries with pertussis toxin inhibited responses to azepexole, but had no significant effect on tone induced by KPSS or noradrenaline.(ABSTRACT TRUNCATED AT 250 WORDS)[1]
  • As a positive control the alpha 2-adrenoceptor agonist B-HT 920 which is equipotent to St 587 with respect to peripheral vasopressor effects in rats was injected with 10 micrograms/kg intracisternally and facilitated the reflex bradycardia [2].
  • Studies on the protective effect of azepexole on ouabain-induced cardiac arrhythmias and lethality in guinea-pig [3].
  • The dopamine autoreceptor agonist B-HT 920 stimulates denervated postsynaptic brain dopamine receptors in rodent and primate models of Parkinson's disease: a novel approach to treatment [4].
  • Intravenous injections of B-HT 920 (0.32-10.0 micrograms/kg) and a DA2-agonist apomorphine (3.2-100.0 micrograms/kg) caused dose-dependent emesis [5].

Psychiatry related information on B-HT 920


High impact information on B-HT 920

  • These responses to azepexole show prominent differences as a function of age and gender but appear not to depend on common allelic variations at the ADRA2B receptor [10].
  • Men had less venodilation than women with low doses of azepexole but greater venoconstriction with higher doses (ANOVA, P = .036) [10].
  • The only significant effect on the locomotor activity of 10-day-old rats was an increase in activity after injection of APO, 0.01 mg/kg or higher, or B-HT 920, 0.01 mg/kg [11].
  • Yohimbine (10(-6) M) decreased slightly the response of ear arteries and increased that of femoral arteries to B-HT 920 [12].
  • The mode of action of NPY is different from those of B-HT 920, an alpha-2 adrenoceptor agonist, and omega-conotoxin, a neurotoxin that acts specifically on presynaptic calcium channels [13].

Chemical compound and disease context of B-HT 920


Biological context of B-HT 920


Anatomical context of B-HT 920

  • The authors' findings indicate that the effects of morphine and azepexole are additive, but that there is no direct interaction between the opioid and adrenergic receptors in the ileum [22].
  • Central alpha-2 adrenoceptor affinity, measured as the Ki for inhibition of [3H]rauwolscine binding to rat brain homogenates, correlated well with antagonist activity at peripheral postjunctional alpha-2 adrenoceptors as reflected by the KB against B-HT 920-induced contraction in canine saphenous vein [23].
  • ETYA also antagonized B-HT 920-induced contractions in the absence of endothelium [24].
  • 4. In contrast, bilateral 6-OHDA infusions into the nucleus accumbens resulted in a supersensitive (locomotor stimulant) response to a low dose of apomorphine (0.1 mg kg-1, s.c.), but not to B-HT 920 (0.01 and 0.1 mg kg-1) [25].
  • (+)-Nantenine (1 - 30 microM) reversed and competitively antagonized the inhibitory action induced by B-HT 920 in electrically-stimulated rat vas deferens [26].

Associations of B-HT 920 with other chemical compounds


Gene context of B-HT 920


Analytical, diagnostic and therapeutic context of B-HT 920

  • After electrical stimulation of the sympathetic outflow from the spinal cord to the heart, B-HT 920 induced an inhibition of the cardiac response, which was significant at stimulation frequencies up to 1 Hz in young SHR and WKY and up to 2 Hz in the adult animals [36].
  • In addition, this unfavourable effect of B-HT 920 on coronary perfusion after coronary dilator reserve has been exhausted may be further exacerbated by an increase in efferent sympathetic discharge [37].
  • After adrenalectomy performed 18-12 h previously, the vasopressor responses induced by stimulation of postjunctional alpha 2-adrenoceptors (agonist: B-HT 920) were attenuated in pithed normotensive rats in contrast to pressor responses mediated by postjunctional alpha 1-adrenoceptors (agonist: cirazoline) [38].
  • The central site of the hypotensive and bradycardiac action was demonstrated by the significantly greater effect after intracisternal ( than after intravenous injection of B-HT 920, 3 micrograms/kg [39].
  • The influence of unilateral ocular instillation of B-HT 920 (50 micrograms) on regional ocular, cerebral and peripheral blood flows was investigated with the labelled microsphere method in conscious and anaesthetized albino rabbits [40].


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  2. Possible function of alpha 1-adrenoceptors in the CNS in anaesthetized and conscious animals. Pichler, L., Kobinger, W. Eur. J. Pharmacol. (1985) [Pubmed]
  3. Studies on the protective effect of azepexole on ouabain-induced cardiac arrhythmias and lethality in guinea-pig. Thomas, G.P. Eur. J. Pharmacol. (1995) [Pubmed]
  4. The dopamine autoreceptor agonist B-HT 920 stimulates denervated postsynaptic brain dopamine receptors in rodent and primate models of Parkinson's disease: a novel approach to treatment. Hinzen, D., Hornykiewicz, O., Kobinger, W., Pichler, L., Pifl, C., Schingnitz, G. Eur. J. Pharmacol. (1986) [Pubmed]
  5. The emetic effect of B-HT 920 and apomorphine in the dog: antagonism by haloperidol. Hsu, W.H., Schaffer, D.D., Dyer, D.C. Life Sci. (1986) [Pubmed]
  6. Evidence for postsynaptic dopamine agonist effects of B-HT 920 in the presence of the dopamine D-1 agonist SKF 38393. Meltzer, L.T., Wiley, J.N., Williams, A.E., Heffner, T.G. Psychopharmacology (Berl.) (1988) [Pubmed]
  7. The alpha 2-adrenoceptor antagonists idazoxan and yohimbine can unmask the postsynaptic dopamine agonist effects of B-HT 920. Meltzer, L.T., Wiley, J.N., Heffner, T.G. Eur. J. Pharmacol. (1989) [Pubmed]
  8. The dopamine autoreceptor agonist, B-HT 920, preferentially reduces brain dopamine release in vivo: biochemical indices of brain dopamine, noradrenaline and serotonin in ventriculocisternal perfusates in the cat. Pifl, C., Pichler, L., Kobinger, W., Hornykiewicz, O. Eur. J. Pharmacol. (1988) [Pubmed]
  9. Chronic electroconvulsive shock alters hypothermic response of B-HT 920 and SKF 38393 in rats. Verma, A., Kulkarni, S.K. J. Pharm. Pharmacol. (1991) [Pubmed]
  10. Human response to alpha2-adrenergic agonist stimulation studied in an isolated vascular bed in vivo: Biphasic influence of dose, age, gender, and receptor genotype. King, D., Etzel, J.P., Chopra, S., Smith, J., Cadman, P.E., Rao, F., Funk, S.D., Rana, B.K., Schork, N.J., Insel, P.A., O'Connor, D.T. Clin. Pharmacol. Ther. (2005) [Pubmed]
  11. Dopamine D2 autoreceptors in rats are behaviorally functional at 21 but not 10 days of age. Lin, M.Y., Walters, D.E. Psychopharmacology (Berl.) (1994) [Pubmed]
  12. Cooling and response to adrenoceptor agonists of rabbit ear and femoral artery: role of the endothelium. García-Villalón, A.L., Monge, L., Montoya, J.J., García, J.L., Fernández, N., Gómez, B., Diéguez, G. Br. J. Pharmacol. (1992) [Pubmed]
  13. An electrophysiological study on the effect of neuropeptide Y on sympathetic neurotransmission in guinea pig vas deferens. Cheung, D.W., Dukkipati, R. J. Pharmacol. Exp. Ther. (1991) [Pubmed]
  14. Effect of pertussis toxin on the interaction of azepexole and halothane. Puig, M.M., Turndorf, H., Warner, W. J. Pharmacol. Exp. Ther. (1990) [Pubmed]
  15. Modulation of motor activity by alpha 1- and alpha 2-adrenoceptor stimulation in mice. Pichler, L., Kobinger, W. Naunyn Schmiedebergs Arch. Pharmacol. (1981) [Pubmed]
  16. Cardiovascular responses to milrinone in pertussis toxin-pretreated pithed rats. Verrijk, R., De Wildt, D.J., Van Rooij, H.H., Wemer, J., Porsius, A.J. Eur. J. Pharmacol. (1990) [Pubmed]
  17. The influence of continuous infusion and sudden withdrawal of azepexole (B-HT 933) on blood pressure and heart rate in the spontaneously hypertensive and normotensive rat. Suppression of the withdrawal responses by morphine. Thoolen, M.J., Timmermans, P.P., van Zwieten, P.A. J. Pharmacol. Exp. Ther. (1981) [Pubmed]
  18. Imidazole has similar behavioural effects to yohimbine. Ferrari, F., Martinelli, R., Baggio, G. Psychopharmacology (Berl.) (1986) [Pubmed]
  19. Selective alpha 2-adrenergic agonists B-HT 920 and UK14304-18. Effects on aqueous humor dynamics in monkeys. Serle, J.B., Steidl, S., Wang, R.F., Mittag, T.W., Podos, S.M. Arch. Ophthalmol. (1991) [Pubmed]
  20. Effects of the irreversible alpha-adrenoceptor antagonists phenoxybenzamine and benextramine on the effectiveness of nifedipine in inhibiting alpha 1- and alpha 2-adrenoceptor mediated vasoconstriction in pithed rats. Timmermans, P.B., Thoolen, M.J., Mathy, M.J., Wilffert, B., de Jonge, A., van Zwieten, P.A. Naunyn Schmiedebergs Arch. Pharmacol. (1985) [Pubmed]
  21. The antiinflammatory action of guanabenz is mediated through 5-lipoxygenase and cyclooxygenase inhibition. Chang, J., Blazek, E., Skowronek, M., Marinari, L., Carlson, R.P. Eur. J. Pharmacol. (1987) [Pubmed]
  22. Effects of azepexole on opioid receptors and endogenous opioid release in the guinea pig ileum. Puig, M.M., Turndorf, H., Warner, W. Anesthesiology (1990) [Pubmed]
  23. 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]
  24. Endothelial mediated inhibition of contraction and increase in cyclic GMP levels evoked by the alpha-adrenoceptor agonist B-HT 920 in rat isolated aorta. Miller, R.C., Mony, M., Schini, V., Schoeffter, P., Stoclet, J.C. Br. J. Pharmacol. (1984) [Pubmed]
  25. Effects of B-HT 920 on nigrostriatal and mesolimbic dopamine systems in normosensitive and supersensitive rats. Clarke, P.B., Wyder, K.J., Jakubovic, A., Fibiger, H.C. Br. J. Pharmacol. (1990) [Pubmed]
  26. Pharmacological effects of (+)-nantenine, an alkaloid isolated from Platycapnos spicata, in several rat isolated tissues. Orallo, F. Planta Med. (2003) [Pubmed]
  27. Postjunctional alpha 2-adrenoceptors mediate venoconstriction in the hindquarters circulation of anaesthetized cats. Bentley, G.A., Widdop, R.E. Br. J. Pharmacol. (1987) [Pubmed]
  28. Prejunctional alpha 2-adrenoceptor mediated inhibitory action of clonidine and B-HT 920, but not urapidil in guinea pig ileum. Shebuski, R.J., Zimmerman, B.G. Proc. Soc. Exp. Biol. Med. (1985) [Pubmed]
  29. Pharmacological characterization of spinal alpha adrenoceptors related to blood pressure control in rats. Kubo, T., Nagura, J., Misu, Y. J. Pharmacol. Exp. Ther. (1987) [Pubmed]
  30. Electroencephalographic correlates of the sedative effects of dopamine agonists presumably acting on autoreceptors. Kropf, W., Kuschinsky, K. Neuropharmacology (1991) [Pubmed]
  31. Decrease of prolactin secretion via stimulation of pituitary dopamine D-2 receptors after application of talipexole and SND 919. Domae, M., Yamada, K., Hanabusa, Y., Matsumoto, S., Furukawa, T. Eur. J. Pharmacol. (1990) [Pubmed]
  32. Dopamine D-2 receptor agonist-induced behavioural depression: critical dependence upon postsynaptic dopamine D-1 function. A behavioural and biochemical study. Jackson, D.M., Ross, S.B., Larsson, L.G. Naunyn Schmiedebergs Arch. Pharmacol. (1989) [Pubmed]
  33. Effects of the selective beta 1-adrenoceptor antagonist, nebivolol, on cardiovascular parameters in the pithed normotensive rat. Schneider, J., Fruh, C., Wilffert, B., Peters, T. Pharmacology (1990) [Pubmed]
  34. Suppressive effect of the dopamine D2 receptor agonist B-HT 920 on rat grooming. Ferrari, F., Pelloni, F., Giuliani, D. Eur. J. Pharmacol. (1992) [Pubmed]
  35. B-HT 920--a novel dopamine autoreceptor agonist in the treatment of patients with schizophrenia. Wiedemann, K., Benkert, O., Holsboer, F. Pharmacopsychiatry (1990) [Pubmed]
  36. Effect of age on the prejunctional alpha-adrenoceptor-mediated feedback in the heart of spontaneously hypertensive rats and normotensive Wistar Kyoto rats. Evidence for a physiological role of prejunctional alpha 2-adrenoceptors. de Jonge, A., Santing, P.N., Timmermans, P.B., van Zwieten, P.A. Naunyn Schmiedebergs Arch. Pharmacol. (1983) [Pubmed]
  37. Alpha 2-adrenoceptor-mediated coronary vasoconstriction persists after exhaustion of coronary dilator reserve. Deussen, A., Heusch, G., Thämer, V. Eur. J. Pharmacol. (1985) [Pubmed]
  38. Effect of adrenalectomy and demedullation of the adrenals on vasopressor responses to stimulation of postjunctional alpha 2-adrenoceptors. Van Meel, J.C., Qian, J., Wilffert, B., De Jonge, A., Timmermans, P.B., Van Zwieten, P.A. Eur. J. Pharmacol. (1983) [Pubmed]
  39. Centrally mediated cardiovascular effects of B-HT 920 (6-allyl-2-amino-5,6,7,8-tetrahydro-4H-thiazolo-[4,5-d]-azepine dihydrochloride), a hypotensive agent of the "clonidine type". Pichler, L., Kobinger, W. J. Cardiovasc. Pharmacol. (1981) [Pubmed]
  40. Effects of B-HT 920 in the eye and on regional blood flows in anaesthetized and conscious rabbits. Thörig, L., Bill, A. Curr. Eye Res. (1986) [Pubmed]
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