The effects of 14 days of treatment with the alpha2-adrenoceptor antagonist yohimbine on cardiovascular parameters (blood pressure and heart rate), plasma catecholamines, insulin and non-esterified fatty acids (NEFA), and the number of alpha2-adrenoceptors on platelets have been evaluated.
The treatment increased plasma noradrenaline but not adrenaline and did not change the other cardiovascular, metabolic or routine blood parameters. It caused a decrease in the velocity of adrenaline-induced platelet aggregation, although [3H]-yohimbine binding to platelets remained unchanged. Acute administration of yohimbine before the experiment led to a significant increase in plasma noradrenaline and NEFA levels. After the 15 day treatment, acute administration of the same dose of yohimbine had less effect on plasma NEFA and there was no significant change in plasma noradrenaline.
The acute lipid-mobilizing effect of yohimbine in healthy volunteers persisted after the 14 days of treatment with no change in other parameters. The prolonged alpha2-adrenoceptor blockade with yohimbine did not induce any change in platelet alpha2-adrenoceptors.
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Aaron RD, Molinoff PB (1982) Changes in the density of beta adrenergic receptors in rat lymphocytes, heart and lung after chronic treatment with propanolol. J Pharmacol Exp Ther 221: 439–443
Berlan M, Lafontan M (1980) Identification of alpha2-adrenergic receptors in human fat cell membranes by 3H-clonidine binding. Eur J Pharmacol 67: 481–484
Berlin I, Stalla-Bourdillon A, Thuillier F, Rosenblatt JI, Gary M (1987) Absence d'efficacité de la yohimbine dans le traitement de l'obésité. J Pharmacol (Paris) 17: 343–347
Berlin I, Crespo-Laumonnier B, Turpin G, Puech AJ (1989) The alpha2-adrenoceptor antagonist yohimbine does not facilitate weight loss but blocks adrenaline-induced platelet aggregation in obese subjects. Therapie 44: 301
Brodde OE, Wang XL (1988) Beta-adrenoceptor changes in blood lymphocytes and altered drug responsiveness. Ann Clin Res 20: 311–323
Brodde OE, Zerkowski MR, Doetsch N, Khamssi M (1989) Subtype-selective up-regulation of human saphenous vein beta2-adrenoceptors by chronic beta-adrenoceptor antagonist treatment. Naunyn-Schmiedeberg's Arch Pharmacol 339: 479–482
Burns TW, Langley PE, Terry BE, Bylund DB (1983) Pharmacological characterization and regulation of adrenergic receptors in human adipocytes. In: Angel A, Hollenberg CH, Roncari DAK (eds) The adipocyte and obesity: cellular and molecular mechanisms. Raven, New York, pp 235–244
Charney DS, Heninger GR, Redmond DE (1983) Yohimbine induced anxiety and increased noradrenergic function in humans: effects of diazepan and clonidine. Life Sci 33: 19–29
Chatelut E, Rispail Y, Berlan M, Montastruc JL (1989) Yohimbine increases human salivary secretion. Br J Clin Pharmacol 28: 366–368
Connacher AA, Jung RT, Mitchell (1988) Weight loss in obese subjects on a restricted diet given BRL 26830 A, a new atypical β adrenoceptor agonist Br Med J 296: 1217–1220
Damase-Michel C, Valet P, Montastruc JL (1987) Nicardipine causes sympathetic activation that does not involve baroreceptor reflex tachycardia in conscious sino-aortic denervated dogs. Eur J Pharmacol 142: 145–149
Diquet B, Lacomblez L, Douare L, Berlin I, Bergougnan L, Simon P (1985) Etude pharmacocinetique de la yohimbine chez l'homme. J Pharmacol (Paris) 16: 540
Galitzky J, Taouis M, Berlan M, Riviere D, Garrigues M, Lafontan M (1988) Alpha2 antagonist compounds and lipid mobilization: evidence for a lipid mobilizing effect of oral yohimbine in healthy male volunteers. Eur J Clin Invest 18: 587–594
Goldberg MR, Robertson D (1983) Yohimbine: a pharmacological probe for study of the alpha2-adrenoceptor. Pharmacol Rev 35: 143–180
Goldberg MR, Hollister AS, Robertson D (1983) Influence of yohimbine on blood pressure, autonomic reflexes and plasma catecholamines in humans. Hypertension 5: 772–778
Henny C, Schutz Y, Buckert A, Meylan M, Jequier E, Felber JP (1987) Thermogenic effect of the new beta-adrenoceptor agonist RO 16-8714 in healthy male volunteers. Int J Obesity 11: 473–483
Lafontan M, Berlan M (1981) Alpha-adrenergic receptors and the regulation of lipolysis in adipose tissue. Trends Pharmacol Sci 2: 126–129
Leibel RL, Hirsch J (1987) Site- and- sex related differences in adrenoceptor status of human adipose tissue. J Clin Endocrinol Metab 64: 1205–1210
Lowry OH, Rosenbrough NJ, Farr AL, Randall RJ (1951) Protein measurement with the folin phenol reagent. J Biol Chem 193: 265–275
Mac Donald E, Ruskoaho H, Schenin M, Virtanen R (1988) Therapeutic applications of drugs acting on alpha-adrenoceptors. Ann Clin Res 20: 298–310
Mauriege P, Galitzky J, Berlan M, Lafontan M (1987) Heterogeneous distribution of beta and alpha2-adrenoceptor binding sites in human fat cells from various fat deposits: functional consequences. Eur J Clin Invest 16: 302–306
Owen JA, Nakatsu SL, Fenemore J, Condra M, Surridge DHC, Morales A (1987) The pharmacokinetics of yohimbine in man. Eur J Clin Pharmacol 32: 577–582
Peskind ER, Weith RC, Dorsa DM, Gumbrecht F, Baskind MA (1989) Yohimbine increases cerebrospinal fluid and plasma norepinephrine but not arginine vasopressine in humans. Neuroendocrinol 50: 286–291
Reid K, Surridge DHC, Morales A, Condra M, Harris C, Owen J, Fenemore J (1987) Double-blind trial of yohimbine in treatment of psychogenic impotence. Lancet II: 421–423
Richelsen B (1986) Increased alpha2 but similar beta adrenergic receptor activities in subcutaneous gluteal adipocytes from females compared with males. Eur J Clin Invest 16: 302–306
Susset JG, Tessier CD, Wincze J, Bansal S, Malhotra C Schwacha (1989) Effect of yohimbine hydrochloride on erectile impotence: a double-blind study. J Urol 141: 1360–1363
Taouis M, Berlan M, Montastruc P, Lafontan M (1988) Mechanism of the lipid mobilizing effect of alpha2-adrenergic antagonists in the dog. J Pharmacol Exp Ther 247: 1172–1180
Van Zwieten PA, Timmermans PBMWM (1984) Central and peripheral alpha adrenoceptors. Adv Drug Res 13: 209–254
Valet P, Taouis M, Tran MA, Montastruc P, Lafontan M, Berlan M (1989) Lipomobilizing effects of procaterol and yohimbine in the conscious dog: comparison of endocrinological, metabolic and cardiovascular effects. Br J Pharmacol 97: 229–239
Villeneuve A, Berlan M, Lafontan M, Caranobe C, Boneu N, Rascol A, Montastruc JL (1985) Platelet alpha2-adrenoceptors in Parkinson's disease: decreased number and recovery after treatment. Eur J Clin Invest 15: 403–407
Zahorska-Markiewicz B, Kucio C, Piskorska D (1986) Adrenergic control of lipolysis and metabolic responses in obesity. Horm Metabol Res 18: 693–697
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Galitzky, J., Rivière, D., Tran, M.A. et al. Pharmacodynamic effects of chronic yohimbine treatment in healthy volunteers. Eur J Clin Pharmacol 39, 447–451 (1990). https://doi.org/10.1007/BF00280934
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