Skip to main content

Therapeutic Applications of Agents Interacting with alpha-1 Adrenergic Receptors

  • Chapter
  • 239 Accesses

Part of the book series: The Receptors ((REC))

Abstract

In addition to the beta-1 adrenergic receptor that mediates an increase in cardiac rate and force of contraction, myocardial alpha-1 adrenergic receptors are known to mediate a positive inotropic response with little effect on cardiac rate (Wagner and Brodde, 1978; Shibata et al., 1980). The mechanism by which cardiac alpha-1 adrenergic receptors increase force of contraction has not been established, but it appears not to be associated with accumulation of cyclic AMP or stimulation of adenylate cyclase (Brodde et al., 1978). In this respect, the alpha-1 adrenergic receptors differ from myocardial beta-adrenergic receptors. Another difference between alpha-1 and beta-1 adrenergic receptors in cardiac tissue is the slower onset and washout for alpha-1-mediated responses (Schumann et al., 1975). Electrophysiologic differences resulting from alpha-1 and beta-1 receptor activation have also been observed (Govier et al., 1966; Govier, 1967). Although beta-1 adrrenergic receptor-mediated inotropic responses occur at all rates of contraction, the effect mediated by the myocardial alpha-1 adrenergic receptor is most prominent at low heart rates (Broadley, 1982).

This is a preview of subscription content, log in via an institution.

Buying options

Chapter
USD   29.95
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
eBook
USD   169.00
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
Softcover Book
USD   219.99
Price excludes VAT (USA)
  • Compact, lightweight edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info
Hardcover Book
USD   219.99
Price excludes VAT (USA)
  • Durable hardcover edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info

Tax calculation will be finalised at checkout

Purchases are for personal use only

Learn about institutional subscriptions

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  • Abrams, P. H., Shah, P. J. R., Stone, R., and Choa, R. G. (1982) Bladder outflow obstruction treated with phenoxybenzamine. Brit. J. Urol. 54, 527–530.

    Article  PubMed  CAS  Google Scholar 

  • Awan, N. A., Hermanovich, J., Vera, Z., Amsterdam, E., and Mason, D. T. (1982) Cardiocirculatory actions of triamzosin and sodium nitroprusside in ischemic heart disease. Clin. Pharmacol. Ther. 31, 290–296.

    Article  PubMed  CAS  Google Scholar 

  • Awan, N. A., Lee, G., DeMaria, A. N., and Mason, D. T. (1981) Ambulatory prazosin treatment of chronic congestive heart failure: Development of late tolerance reversible by higher dosage and interrupted substitution therapy. Am. Heart J. 101, 541–547.

    Article  PubMed  CAS  Google Scholar 

  • Awan, N. A., Miller, R. R., and Mason, D. T. (1978) Comparison of effects of nitroprusside and prazosin on left ventricular function and the peripheral circulation in chronic refractory congestive heart failure. Am. J. Cardiol. 40, 152–159.

    Google Scholar 

  • Awan, N. A., Miller, R.R., DeMaria, A. N., Maxwell, K. S., Neumann, A., and Mason, D. T. (1977) Efficacy of ambulatory systemic vasodilator therapy with oral prazosin in chronic refractory heart failure. Circulation 56, 346–354.

    PubMed  CAS  Google Scholar 

  • Beilin, L. J. and Juel-Jensen, B. E. (1982) Alpha- and beta-adrenergic blockade in hypertension. Lancet I, 979–982.

    Google Scholar 

  • Belis, J. A., Longhurst, P. A., and Westfall, D. P. (1983) Neurogenic activity of smooth muscle from hyperplastic human prostates. Am. Coll. of Surgeons Surgical Forum 34, 656–659.

    Google Scholar 

  • Bertel, O., Burkart, F., and Buhler, F. R. (1981) Sustained effectiveness of chronic prazosin therapy in severe chronic congestive heart failure. Am. Heart J. 101, 529–533.

    Article  PubMed  CAS  Google Scholar 

  • Bolli, P., Erne, P., Block, L. H., Ji, B. H., Kiowski, W., and Buhler, F. R. (1984) Adrenaline induces vasoconstriction through postjunctional alpha-2 adrenoceptor stimulation which is enhanced in essential hypertension. J. Hypertension 2 (suppl. 3), 115–118.

    Google Scholar 

  • Bolli, P., Erne, P., Kiowski, W., Ji, B. H., Amann, F. W., and Buhler, F. R. (1983) Important contribution of post-junctional alpha2-adrenoceptor mediated vasoconstriction to arteriolar tone in man. J. Hypertension. 1 (suppl. 2), 257–259.

    CAS  Google Scholar 

  • Bolli, R., Brandon, T. A., Fisher, D. J., and Miller, R. R. (1983) Comparative analysis of the effects of alpha-adrenergic antagonists in acute myocardial ischemia. Clin. Res. 31, 169A.

    Google Scholar 

  • Bolli, R., Fisher, D. J., Taylor, A. A., Young, J. B., and Miller, R. R. (1984) Effect of alpha-adrenergic blockade on arrhythmias induced by acute myocardial ischemia and reperfusion in the dog. J. Mol. Cell. Cardiol. 16, 1101–1117.

    Article  PubMed  CAS  Google Scholar 

  • Breckenridge, A. (1982) Vasodilators in heart failure. Br. Med. J. 284, 765–766.

    Article  CAS  Google Scholar 

  • Brittain, R. T. and Levy, G. P. (1976) A review of the animal pharmacology of labetolol, a combined alpha and beta-adrenoceptor blocking drug. Br. J. Clin. Pharmacol. 34, (suppl. 3), 681–684.

    Google Scholar 

  • Broadley, K. J. (1982) Cardiac adrenoceptors. J. Auton. Pharmacol. 2, 119–145.

    Article  CAS  Google Scholar 

  • Brodde, O. E., Motomura, S., Endoh, M., and Schumann, H. J. (1978) Lack of correlation between the positive inotropic effect evoked by alpha-adrenoceptor stimulation and the levels of cyclic AMP and/or cyclic GMP in the isolated ventricle strip of the rabbit. J. Molec. Cell. Cardiol. 10, 207–219.

    Article  CAS  Google Scholar 

  • Caine, M., Perlberg, S., and Meretyk, S. (1978) A placebo-controlled double blind study of the effect of phenoxybenzamine in benign prostatic obstruction. Br. J. Urol. 50, 551–554.

    Article  PubMed  CAS  Google Scholar 

  • Caine, M., Perlberg, S., and Shapiro, A. (1981) Phenoxybenzamine for benign prostatic obstruction: Review of 200 cases. Urology 17, 542–546.

    Article  PubMed  CAS  Google Scholar 

  • Caine, M., Pfau, A., and Perlberg, S. (1976) The use of alpha-adrenergic blockers in benign prostatic obstruction. Br. J. Urol. 48, 255–263.

    PubMed  CAS  Google Scholar 

  • Caine, M., Raz, S., and Ziegler, M. (1975) Adrenergic and cholinergic receptors in the human prostate, prostatic capsule and bladder neck. Br. J. Urol. 47, 193–202.

    Article  PubMed  CAS  Google Scholar 

  • Caine, M. (1986) Clinical experience with alpha-adrenoceptor antagonists in benign prostatic hypertrophy. Fed. Proc. 45, 2604–2608.

    PubMed  CAS  Google Scholar 

  • Cohn, J. N., Archibald, D. G., Ziesche, S., Franciosa, J. A., Harston, W. E., Tristani, F. E., Dunkman, W. B., Jacobs, W., Francis, G. S., Flohr, K. H., Goldman, S., Cobb, F. R., Shah, P. M., Saunders, R., Fletcher, R. D., Loeb, H. S., Hughes, V. C., and Baker, B. (1986) Effect of vasodilator therapy on mortality in chronic congestive heart failure. N. Eng. J. Med. 314, 1547–1552.

    Article  CAS  Google Scholar 

  • Cohn, J. N., Levine, T. B., Olivari, M. T., Garberg, V., Lura, D., Francis, G. S., Simon, A. B., and Rector, T. (1984) Plasma norepinephrine as a guide to prognosis in patients with chronic congestive heart failure. N. Eng. J. Med. 311, 819–823.

    Article  CAS  Google Scholar 

  • Colucci, W. S. (1982) Alpha-adrenergic receptor blockade with prazosin. Ann. Int. Med. 97, 67–77.

    PubMed  CAS  Google Scholar 

  • Constantine, J. W., Lebel, W., and Archer, R. (1982) A dog saphenous vein preparation with functional postsynaptic alpha2- but not alpha1-adrenoceptors. Eur. J. Pharmacol. 85, 325–329.

    Article  PubMed  CAS  Google Scholar 

  • Corr, P. B. and Crafford, W. A. (1981) Enhanced alpha-adrenergic responsiveness in ischemic myocardium: Role of alpha-adrenergic blockade. Am. Heart J. 102, 605–612.

    Article  PubMed  CAS  Google Scholar 

  • Davey, M. J. (1980) Relevant features of the pharmacology of prazosin. J. Cardiovasc. Pharmacol. 2, (suppl. 3), S287-S301.

    Google Scholar 

  • DeCree, J., Leempoels, J., DeCock, W., Geukens, H., and Verhaegen, H. (1981) The antihypertensive effects of a pure and selective serotonin-receptor blocking agent (R41468) in elderly patients. Angiology 32, 137–144.

    Article  CAS  Google Scholar 

  • Dukes, I. D. and Vaughan-Williams, E. M. (1984) Electrophysiological effects of alpha-adrenoceptor antagonists in rabbit sino-atrial node, cardiac Purkinje cells and papillary muscles. Br. J. Pharmacol. 83, 419–426.

    PubMed  CAS  Google Scholar 

  • Eltze, M. (1979) Investigations on the mode of action of a new antihypertensive drug, urapadil, in the isolated rat vas deferens. Eur. J. Pharmacol. 59, 1–9.

    Article  PubMed  CAS  Google Scholar 

  • Ettinger, S., Gould, L., Carmichael, J. A., and Tashjian, R. J. (1969) Phentolamine: Use in digitalis-induced arrhythmias. Am. Heart J. 77, 636–640.

    Article  PubMed  CAS  Google Scholar 

  • Feldman, R. C., Ball, R. M., Winchester, M. A., Jaillon, P., Kates, R E., and Harrison, D. C. (1981) Beneficial hemodynamic response to chronic prazosin therapy in congestive heart failure. Am. Heart J. 101, 534–540.

    Article  PubMed  CAS  Google Scholar 

  • Flamenbaum, W. (1985) Propranolol vs labetolol: Interesting differences in efficacy. J. Natl Med. Assoc. 77, (suppl.), 14–29.

    PubMed  Google Scholar 

  • Fozard, J. R. (1982) Mechanism of the antihypertensive effect of ketanserin. J. Cardiovas. Pharmacol. 4, 829–838.

    Article  CAS  Google Scholar 

  • Freissmuth, M., Tuisl, E., Steurer, G., and Schutz, W. (1984) Interaction of the antihypertensive drug Urapidil with cardiac beta-adrenoceptors. Eur. J. Pharmacol. 104, 169–172.

    Article  PubMed  CAS  Google Scholar 

  • Giudice, P. A. (1980) Nuove vedute di terapia della syndrome di Raynaud. Minerva Medica 71, 1459–1460.

    PubMed  CAS  Google Scholar 

  • Goldstein, D. S. (1983) Plasma catecholamines and essential hypertension: An analytical review. Hypertension 5, 86–99.

    PubMed  CAS  Google Scholar 

  • Gould, L. and Reddy, C. V. R. (1976) Phentolamine. Am. Heart J. 92, 397–402.

    Article  PubMed  CAS  Google Scholar 

  • Gould, L., Reddy, C. V. R., Weinstein, T., and Gomprecht, R. F. (1975) Antiarrhythmic prophylaxis with phentolamine in acute myocardial infarction. J. Clin. Pharmacol. 15, 191–197.

    Google Scholar 

  • Govier, W. C. (1967) Prolongation of the myocardial functional refractory period by phenylephrine. Life Sci. 6, 1367–1371.

    Article  PubMed  CAS  Google Scholar 

  • Govier, W. C., Mosal, N. C., Whittington, P., and Broom, A. H. (1966) Myocardial alpha- and beta-adrenergic receptors as demonstrated by atrial functional refractory period changes. J. Pharmacol Exp. Ther. 154, 255–263.

    CAS  Google Scholar 

  • Graham, R. M. and Mulvihill-Wilson, J. (1980) Clinical pharmacology of prazosin used alone or in combination in the therapy of hypertension. J. Cardiovasc. Pharmacol. 2, (suppl. 3), S87-S98.

    Google Scholar 

  • Hedlund, H., Andersson, K. E., and Ek, A. (1983) Effects of prazosin in patients with benign prostatic obstruction. J. Urol. 130, 275–278.

    PubMed  CAS  Google Scholar 

  • Hieble, J. P., Caine, M., and Zalaznik, E. (1985a) In vitro characterization of the alpha-adrenoceptors in human prostate. Eur. J. Pharmacol. 107, 111–117.

    Article  PubMed  CAS  Google Scholar 

  • Hieble, J. P., Roesler, J. M., Fowler, P. J., Matthews, W. D., and DeMarinis, R. M. (1985b) A New Approach to Antihypertensive Therapy via Blockade of the Postjunctional alpha2-Adrenoceptor, in Vascular Neuroeffector Mechanisms (Bevan, J. A., Godfraind, T., Maxwell, R. A., Stoclet, J. C., and Worcel, M., eds.) Elsevier, Amsterdam.

    Google Scholar 

  • Higginbotham, M. B., Morris, K. G., Bramlet, D. A., Coleman, R. E., and Cobb, F. R. (1983) Long-term ambulatory therapy with prazosin versus placebo for chronic heart failure: Relation between clinical response and left ventricular function at rest and during exercise. Am. J. Cardiol. 52, 782–788.

    Article  PubMed  CAS  Google Scholar 

  • Jie, K., van Brummelen, P., Vermey, P., Timmermans, P. B. M. W. M., and van Zwieten, P. A. (1986) Alpha-1 and alpha-2 adrenoceptor mediated vasoconstriction in the forearm of normotensive and hypertensive subjects. J. Cardiovasc. Pharmacol. 8, 190–196.

    Article  PubMed  CAS  Google Scholar 

  • Kalkman, H. O., Harms, Y. M., van Gelderen, E. M., Batink, H. D., Timmermans, P. B. M. W. M., and van Zwieten, P. A. (1983) Hypotensive activity of serotonin antagonists: Correlation with alpha1-adrenoceptor and serotonin receptor blockade. Life Sci. 32, 1499–1505.

    Article  PubMed  CAS  Google Scholar 

  • Kalkman, H. O., Timmermans, P. B. M. W. M., and van Zwieten, P. A. (1982) Characterization of the antihypertensive properties of ketanserin (R41468) in rats. J. Pharmacol. Exp. Ther. 222, 227–231.

    PubMed  CAS  Google Scholar 

  • Kaumann, A. J. (1981) In kitten ventricular myocardium, the inotropic potency of an agonist is determined by both its intrinsic activity for the adenyl cyclase and its affinity for the beta-adrenoceptors. Naunyn Schmiedebergs Arch. Pharmacol. 317, 13–18.

    Article  PubMed  CAS  Google Scholar 

  • Kelly, D. T., Delgado, C. E., Taylor, D. T., Pitt, B., and Ross, R. S. (1973) Use of phentolamine in acute myocardial infarction associated with hypertension and left ventricular failure. Circulation 47, 729–735.

    PubMed  CAS  Google Scholar 

  • Kenakin, T. P. (1981) An in vitro quantitative analysis of the alpha-adrenoceptor partial agonist activity of dobutamine and its relevance to inotropic selectivity. J. Pharmacol. Exp. Ther. 216, 210–219.

    PubMed  CAS  Google Scholar 

  • Kiowski, W., Hulthen, U. L., Ritz, R., and Buhler, F. R. (1983) Alpha2-adrenoceptor mediated vasoconstriction in human arterial vessels. Clin. Pharmacol. Ther. 34, 565–569.

    Article  PubMed  CAS  Google Scholar 

  • Lardennois, B., Khansa, A. E., Amory, J. P., Coulon, J. M., and Lemaire, P. (1981) La phenoxybenzamine en pathologie prostatique. Ann. Urol. 15, 399–402.

    Google Scholar 

  • Leier, C. V. and Unverferth, D. V. (1983) Dobutamine. Ann. Intern. Med. 99, 490–496.

    PubMed  CAS  Google Scholar 

  • Leimdorfer, A. (1952) Prevention and abolition of cardiac arrhythmias by regitine. Am. J. Physiol. 171, 742.

    Google Scholar 

  • Lemke, R., Trompler, A., Kaltenbach, M., and Bussman, W. D. (1979) Wirkung von prazosin bei der therapierefraktaren chronis chem herzinsuffizienz. Deutsche Med. Wochen. 104, 1769–1773.

    Article  CAS  Google Scholar 

  • Lepor, H. and Shapiro, E. (1984) Characterization of alpha1 adrenergic receptors in human benign prostatic hyperplasia. J. Urol. 132, 1226–1229.

    PubMed  CAS  Google Scholar 

  • Longhurst, P. A., Belis, J. A., and Westfall, D. P. (1983) Contractile response of human prostatic strips. Fed. Prod. 42, 735.

    Google Scholar 

  • Lopez-Sendon, J., Coma Canella, I., Lombera, F., and Martin, J. (1979) Hemodynamic effect of prazosin in congestive cardiac insufficiency of acute degree. Rev. Exp. Cardiol. 32, 253–259.

    CAS  Google Scholar 

  • Lund-Johansen, P. and Bakke, O. M. (1979) Haemodynamic effects and plasma concentration of labetolol during long-term treatment of essential hypertension. Br. J. Clin. Pharmacol. 7, 169–174.

    PubMed  CAS  Google Scholar 

  • Maccarrone, C., Malta, E., and Raper, C. (1984) Beta-adrenoceptor selectivity of dobutamine. In vivo and in vitro studies. J. Cardiovasc. Pharmacol. 6, 132–141.

    Article  PubMed  CAS  Google Scholar 

  • Martorana, G., Gilberti, C., Damonte, P., Ciprandi, G., Dirienzo, W., and Giuliani, L. (1984) The effect of prazosin in benign prostatic hypertrophy, a placebo controlled double blind study. IRCS Med. Sci. 12, 11–12.

    Google Scholar 

  • Maze, S. S., Opie, L. H., and Lloyd, E. A. (1982) The role of coronary artery spasm in anginal syndromes. S. Afr. Med. J. 61, 161–164.

    PubMed  CAS  Google Scholar 

  • Miller, S. I., Ford, R. V., and Moyer, J. H. (1953) Dibenzyline: Results of therapy in patients with hypertension and comparisons with hexamethonium, 1-hydrazinophthalazine and semipurified extracts of Veratrum. N. Eng. J. Med. 248, 576–582.

    Article  CAS  Google Scholar 

  • Mulvihill-Wilson, J., Gaffney, F. A., Pettinger, W. A., Blomqvist, C. G., Anderson, S. A., and Graham, R. M. (1983) Hemodynamic and neuroendocrine responses to acute and chronic alpha-adrenergic blockade with prazosin and phenoxybenzamine. Circulation 67, 383–393.

    Article  PubMed  CAS  Google Scholar 

  • Murphy, B. F., Whitworth, J. A., and Kincaid-Smith, P. (1985) Ketanserin in the acute management of severe hypertension. J. Cardiovasc. Pharmacol. 7, (suppl. 7), S168-S171.

    Article  PubMed  Google Scholar 

  • Northover, B. J. (1983) A comparison of the electrophysiological actions of phentolamine with those of some other antiarrhythmic drugs on tissues isolated from the rat heart. Br. J. Pharmacol. 80 85–93.

    PubMed  CAS  Google Scholar 

  • Ogasawara, B., Ogawa, K., Hayashi, H., and Sassa, H. (1981) Plasma renin activity and plasma concentration of norepinephrine and cyclic nucleotides in heart failure after prazosin. Clin. Pharmacol. Ther. 29, 464–471.

    Article  PubMed  CAS  Google Scholar 

  • Penny, W. J. and Sheridan, D. J. (1982) The effects of phentolamine on arrhythmias and cellular electrophysiology during myocardial ischemia and reperfusion in the guinea pig. J. Physiol. 326, 64P.

    Google Scholar 

  • Perret, C. L., Gardez, J. P., and Reynaert, M. (1975) Phentolamine for vasodilator therapy in left ventricular failure complicating acute myocardial infarction. Br. Heart J. 37, 640–646.

    Article  PubMed  CAS  Google Scholar 

  • Pogwizd, S. M., Sharma, A. D., and Corr, P. B. (1982) Influences of labetolol, a combined alpha- and beta-adrenergic blocking agent on the dysrhythmias induced by coronary artery occlusion and reperfusion. Cardiovasc. Res. 16, 398–407.

    Article  PubMed  CAS  Google Scholar 

  • Raz, S., Ziegler, M., and Caine, M. (1973) Pharmacological receptors in the prostate. Br. J. Urol. 45, 663–667.

    Article  PubMed  CAS  Google Scholar 

  • Roesler, J. M., McCafferty, J. P., DeMarinis, R. M., Matthews, W. D., and Hieble, J. P. (1986) Characterization of the antihypertensive activity of SK&F 86466, a selective alpha-2 antagonist, in the rat. J. Pharmacol. Exp. Ther. 236, 1–7.

    PubMed  CAS  Google Scholar 

  • Rubin, S. A., Chatterjee, K., Gelberg, H. J. M., Ports, T. A., Brundage, B. H., and Parmley, W. W. (1979) Paradox of improved exercise but not resting hemodynamics with short-term prazosin in congestive heart failure. Am. J. Cardiol. 43, 810–815.

    Article  PubMed  CAS  Google Scholar 

  • Ruffolo, R. R. (1984) Alpha-Adrenoceptors, in Neuroreceptors in Health and Disease, Monographs in Neural Sciences vol. 10 (Cohen, M. M., ed.) Karger, Basel.

    Google Scholar 

  • Ruffolo, R. R., Jr. and Messick, K. (1985a) Inotropic selectivity of dobutamine enantiomers in the pithed rat. J. Pharmacol. Exp. Ther. 235, 344–348.

    PubMed  CAS  Google Scholar 

  • Ruffolo, R. R. and Messick, K. (1985b) Effects of dopamine, (±)-dobutamine and the (+) and (-)-enantiomers of dobutamine on cardiac function in pithed rats. J. Pharmacol. Exp. Ther. 235, 558–565.

    PubMed  CAS  Google Scholar 

  • Ruffolo, R. R. and Morgan, E. L. (1984) Interaction of the novel inotropic agent ASL-7022, with alpha- and beta-adrenoceptors in the cardiovascular system of the pithed rat: Comparison with dobutamine and dopamine. J. Pharmacol. Exp. Ther. 229, 363–371.

    Google Scholar 

  • Ruffolo, R. R. and Yaden, E. L. (1983) Vascular effects of the stereoisomers of dobutamine. J. Pharmacol. Exp. Ther. 224, 46–50.

    PubMed  CAS  Google Scholar 

  • Ruffolo, R. R. and Zeid, R. L. (1985) Relationship between alpha adrenoceptor occupancy and response for the alpha-1 adrenoceptor agonist, cirazoline, and the alpha-2-adrenoceptor agonist, B-HT 933, in canine saphenous vein. J. Pharmacol. Exp. Ther. 235, 636–643.

    PubMed  CAS  Google Scholar 

  • Ruffolo, R. R., Messick, K., and Horng, J. S. (1984) Interactions of three inotropic agents, ASL-7022, dobutamine and dopamine with alpha- and beta-adrenoceptors in vitro. Naunyn Schmiedebergs Arch. Pharmacol. 326, 317–326.

    Article  PubMed  CAS  Google Scholar 

  • Ruffolo, R. R., Spradlin, T. A., Pollock, G. D., Waddell, J. E., and Murphy, P. J. (1981) Alpha- and beta-adrenergic effects of the stereoisomers of dobutamine. J. Pharmacol. Exp. Ther. 219, 447–452.

    PubMed  CAS  Google Scholar 

  • Sanders, K. H. and Jurna, I. (1985) Effects of Urapidil, Clonidine, prazosin and propranolol on autonomic nerve activity, blood pressure and heart rate in anaesthetized rats and cats. Eur. J. Pharmacol. 110, 181–190.

    Article  PubMed  CAS  Google Scholar 

  • Sanders, K. H., Eltze, M, and Killian, U. (1984) Discrepancy Between In Vitro alpha1 Adrenoceptor Antagonism and In Vivo Antihypertensive Action, in IUPHAR Ninth International Congress of Pharmacology (Macmillan, London).

    Google Scholar 

  • Sanders, K. H., Killian, U., Kolassa, N., and Schoetensack, W. (1983) Influence of Urapidil on pre- and postsynaptic alpha-adrenoceptors in pithed rats. Naunyn Schmiedebergs Arch. Pharmacol. 324, (suppl.), R15.

    Article  Google Scholar 

  • Schoetensack, W., Bruckschen, E. G., and Zech, K. (1983) Urapidil, in New Drugs Annual: Cardiovascular Drugs vol. 1 (Scriabine, A., ed.) Raven, New York.

    Google Scholar 

  • Schumann, H. J., Endoh, M, and Brodde, O. E. (1975) The time course of the effects of beta- and alpha-adrenoceptor stimulation by isoprenaline and methoxamine on the contractile force and cAMP level of the isolated rabbit papillary muscle. Naunyn Schmiedebergs Arch. Pharmacol. 289, 291–302.

    Article  PubMed  CAS  Google Scholar 

  • Schumann, H. J., Wagner, J., Knoor, A., Reidemaster, J. C., Sadony, V., and Schramm, G. (1978) Demonstration in human atrial preparations of alpha-adrenoceptors mediating positive inotropic effects. Naunyn Schmiedebergs Arch. Pharmacol. 302, 333–336.

    Article  PubMed  CAS  Google Scholar 

  • Shapiro, E. and Lepor, H. (1985) A new receptor in human and canine prostate: The alpha2 adrenergic receptor. J. Urol. 133, 133A.

    Google Scholar 

  • Shapiro, A., Mazouz, B., and Caine, M. (1981) The alpha-adrenergic blocking effect of prazosin on the human prostate. Urol. Res. 9, 17–20.

    Article  PubMed  CAS  Google Scholar 

  • Sharma, A. D., Saffitz, J. E., Lee, B. I., Sobel, B. E., and Corr, P. B. (1983) Alpha adrenergic-mediated accumulation of calcium in reperfused myocardium. J. Clin. Invest. 72, 802–818.

    Article  PubMed  CAS  Google Scholar 

  • Shebuski, R. J. and Zimmerman, B. G. (1985) Prejunctional alpha2-adrenoceptor mediated inhibitory action of Clonidine and B-HT 920 but not urapadil in guinea pig ileum. Proc. Soc. Exp. Biol. Med. 178, 133–138.

    PubMed  CAS  Google Scholar 

  • Shebuski, R. J. and Zimmerman, B. G. (1984) Suppression of reflex tachycardia following alpha-adrenoceptor blockade in conscious dogs: Comparison of urapadil with prazosin. J. Cardiovasc. Pharmacol. 6, 188–194.

    Article  Google Scholar 

  • Sheridan, D. J., Penkoske, P. A., Sobel, B. E., and Corr, P. B. (1980) Alpha adrenergic contributions to dysrhythmia during myocardial ischemia and reperfusion in cats. J. Clin. Invest. 65, 161–171.

    Article  PubMed  CAS  Google Scholar 

  • Shibata, S., Seriguchi, D. G., Iwadare, S., Ishida, Y., and Shibata, T. (1980) The regional and species differences on the activation of myocardial alpha-adrenoceptors by phenylephrine and methoxamine. Gen. Pharmacol. 11, 173–180.

    Article  CAS  Google Scholar 

  • Sioufi, A., Pommier, F., Mangoni, P., Gauvon, S., and Metayer, J. P. (1981) Gas chromatographic determination of phentolamine (Regitine) in human plasma and urine. J. Chromatog. 222, 429–435.

    Article  CAS  Google Scholar 

  • Stanaszek, W. F., Kellerman, D., Brogden, R. N., and Romankiewicz, J. A. (1983) Prazosin Update: A review of its pharmacological properties and therapeutic use in hypertension and congestive heart failure. Drugs 25, 339–384.

    Article  PubMed  CAS  Google Scholar 

  • Stene-Larsen, G. (1980) Characterization of the atrial alpha-receptor of the rat as a subgroup of the postsynaptic alpha-adrenoceptor. Gen. Pharmacol. 11, 575–581.

    Article  PubMed  CAS  Google Scholar 

  • Stewart, J. R., Burmeister, W. E., Burmeister, J., and Lucchesi, B. R. (1980) Electrophysiologic and antiarrhythmic effects of phentolamine in experimental coronary artery occlusion and reperfusion in the dog. J. Cardiovasc. Pharmacol 2, 77–91.

    Article  PubMed  CAS  Google Scholar 

  • Stokes, G. S. and Marwood, J. F. (1984) Review of the use of alpha-adrenoceptor antagonists in hypertension. Meth. Find. Exp. Clin. Pharmacol 6, 197–204.

    CAS  Google Scholar 

  • Takita, T., Otani, T., Knodo, A., and Mitsuya, H. (1983) Urodynamic study of lower urinary tract. XII. The effect of prazosin hydrochloride in the treatment of prostatic obstruction. Japan J. Urol. 74, 1–14.

    CAS  Google Scholar 

  • Taylor, C. R., Leader, J. P., Singleton, W., Munster, E. W., Falkner, F. C., and O’Neil, J. A. (1983) Profile of triamzosin: An effective and safe antihypertensive agent. Am. Heart J. 106, 1269–1281.

    Article  PubMed  CAS  Google Scholar 

  • Thandroyen, F. T., Worthington, M. G., Higginson, L. M., and Opie, L. H. (1983) The effect of alpha- and beta-adrenoceptor antagonist agents on reperfusion ventricular fibrillation and metabolic status in the isolated perfused rat heart. J. Am. Coll. Cardiol. 1, 1056–1066.

    Article  PubMed  CAS  Google Scholar 

  • Thomas, J. A. and Marks, B. H. (1978) Plasma norepinephrine in congestive heart failure. Am. J. Cardiol 41, 233–243.

    Article  PubMed  CAS  Google Scholar 

  • Van der Starre, P. J. A., Scheijgrond, H. W., Reneman, R. S., and Kolling, J. B. (1983) The use of ketanserin, a 5-hydroxytryptamine receptor antagonist, for treatment of postoperative hypertension following coronary artery bypass surgery. Anesthes. Analges. 62, 63–69.

    Google Scholar 

  • Vanhoutte, P. M. and Janssens, W. J. (1980) Thermosensitivity of cutaneous vessels and Raynaud’s disease. Am. Heart J. 100, 263–265.

    Article  PubMed  CAS  Google Scholar 

  • Vanhoutte, P. M., Cooke, J. P., Linblad, L. E., Shepherd, J. T., and Flavahan, N. A. (1985) Modulation of postjunctional alpha-adrenergic responsiveness by local changes in temperature. Clin. Sci. 68, (suppl. 10), 121s–123s.

    PubMed  Google Scholar 

  • Van Neuten, J. M., Janssen, P. A. J., Van Beek, J., Xhonneux, R., Verbeuren, T. J., and Vanhoutte, P. M. (1981) Vascular effects of ketanserin (R41468), a novel antagonist of 5-HT2 serotonergic receptors. J. Pharmacol. Exp. Ther. 218, 217–230.

    Google Scholar 

  • Verberne, A. J. M. and Rand, M. J. (1985) Effect of urapadil on beta-adrenoceptors of rat atria. Eur. J. Pharmacol 108, 193–196.

    Article  PubMed  CAS  Google Scholar 

  • Verberne, A. J. M. and Rand, M. J. (1984) Pharmacological activities of the antihypertensive drug urapadil in the rat. Clin. Exp. Pharmacol Physiol 11, 407–412.

    Article  PubMed  CAS  Google Scholar 

  • Wagner, J. and Brodde, O. E. (1978) On the presence and distribution of alpha-adrenoceptors in the heart of various mammalian species. Naunyn Schmiedebergs Arch. Pharmacol. 302, 239–254.

    Article  PubMed  CAS  Google Scholar 

  • Wagner, J., Schumann, H. J., Knorr, A., Rohm, N., and Reidemeister, J. C. (1980) Stimulation by adrenaline and dopamine but not by noradrenaline of myocardial alpha-adrenoceptors mediating positive inotropic effects in human atrial preparations. Naunyn Schmiedebergs Arch. Pharmacol. 312, 99–102.

    Article  PubMed  CAS  Google Scholar 

  • Waldo, R. (1979) Prazosin relieves Raynaud’s vasospasm. J. Am. Med. Assoc. 241, 1037.

    Article  CAS  Google Scholar 

  • Walinsky, P., Chatterjee, K., Forrester, J., Parmley, W. W., and Swan, H. J. C. (1974) Enhanced left ventricular performance with phentolamine in acute myocardial infarction. Am. J. Cardiol 33, 37–41.

    Article  PubMed  CAS  Google Scholar 

  • Weber, M. A., Drayer, J. I., and Kaufman, C. A. (1984) The combined alpha and beta-adrenergic blocker labetolol and propranolol in the treatment of high blood pressure. Similarities and differences. J. Clin. Pharmacol. 24, 103–112.

    PubMed  CAS  Google Scholar 

  • Wenting, G. J., Man in’t Veld, A. J., Woittiez, A. J., Boomsma, F., and Schalekamp, M. A. D. H. (1982) Treatment of hypertension with ketanserin, a new selective 5-HT2 receptor antagonist. Br. Med. J. 284, 537–539.

    Article  CAS  Google Scholar 

  • Williams, B. J., Griffith, W. H., and Albrecht, C. M. (1978) The protective effect of phentolamine against cardiac arrhythmias in the rat. Eur. J. Pharmacol. 49, 7–14.

    Article  PubMed  CAS  Google Scholar 

  • Woittiez, A. J. J., Wenting, G. J., Man in’t Veld, A. J., Boomsma, F., and Schalekamp, M. A. D. H. (1985) Ketanserin: A possible tool for studying the role of serotonin in hypertension. J. Cardiovasc. Pharmacol. 7, (suppl. 7), S130-S136.

    Article  PubMed  Google Scholar 

  • Zabludowski, J. R., Ball, S. G., and Robertson, J. I. S. (1985) Ketanserin and alpha1-adrenergic antagonism in humans. J. Cardiovasc. Pharmacol 7, (suppl. 7), S123-S125.

    Article  PubMed  Google Scholar 

Download references

Authors

Editor information

Editors and Affiliations

Rights and permissions

Reprints and permissions

Copyright information

© 1987 The Humana Press Inc.

About this chapter

Cite this chapter

Hieble, J.P., Ruffolo, R.R. (1987). Therapeutic Applications of Agents Interacting with alpha-1 Adrenergic Receptors. In: Ruffolo, R.R. (eds) The alpha-1 Adrenergic Receptors. The Receptors. Humana Press. https://doi.org/10.1007/978-1-4612-4582-7_12

Download citation

  • DOI: https://doi.org/10.1007/978-1-4612-4582-7_12

  • Publisher Name: Humana Press

  • Print ISBN: 978-1-4612-8936-4

  • Online ISBN: 978-1-4612-4582-7

  • eBook Packages: Springer Book Archive

Publish with us

Policies and ethics