Functional characterization of central α-adrenoceptors by yohimbine diastereomers

Hedler, L; Stamm, Gilbert G.; Weitzell, Rudolf; Starke, Klaus

doi:10.1016/0014-2999(81)90430-1

Cited by 98 publications

(22 citation statements)

References 26 publications

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“…In the dog, as in the rat (Pfister & Keeton, 1988) and in man (Galitzky et al, 1988), yohimbine enhances sympathetic activity as indicated by the increased plasma catecholamine levels. This effect can be attributed to a peripheral action either on sympathetic nerve endings (blockade of presynaptic X2-adrenoceptors) or to a central action (Wemer et al, 1979;Hedler et al, 1981), or both. Procaterol increases plasma noradrenaline levels while leaving adrenaline concentration unchanged.…”

Section: Discussionmentioning

confidence: 99%

Lipomobilizing effects of procaterol and yohimbine in the conscious dog: comparison of endocrinological, metabolic and cardiovascular effects

Valet¹,

Taouis²,

Tran³

et al. 1989

British J Pharmacology

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provoked an equivalent increase in plasma non-esterified fatty acids (+ 100%). Procaterol, but not yohimbine, induced hyperglycaemia (+ 120%). Plasma insulin was weakly enhanced by yohimbine (+ 120%) as compared to the increase given by procaterol (+ 500%). 4 Both drugs stimulated sympathetic nervous system activity, as indicated by the increased plasma noradrenaline concentration, but only yohimbine increased the plasma adrenaline level. 5 Cardiovascular measurements indicated that procaterol strongly enhances heart rate and transiently decreases mean blood pressure. Yohimbine exhibits a weaker effect on heart rate and slightly increases mean blood pressure. 6 The present work clearly indicates that lipid mobilization is enhanced during fasting in the dog by selective fl2-adrenoceptor stimulation or by Cc2-adrenoceptor blockade. This enhanced lipolytic effect may result either from a direct action of the drugs on the adrenoceptors of fat cells or from an activation of the sympathetic nervous system. Procaterol suffers major limitations since it strongly increases heart rate, immunoreactive insulin and glycaemia. On the other hand, yohimbine induces only minor modifications both in cardiovascular and endocrinological parameters.

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Section: Discussionmentioning

confidence: 99%

Lipomobilizing effects of procaterol and yohimbine in the conscious dog: comparison of endocrinological, metabolic and cardiovascular effects

Valet¹,

Taouis²,

Tran³

et al. 1989

British J Pharmacology

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“…To date, various studies have been performed using yohimbine isomers to characterize the aO/a2 selectivity of adrenergic physiological responses (Hedler et al, 1981). Timmermans et al (1981) and Tanaka & Starke (1980) have proposed the use of yohimbine isomers to determine the al-or a2-selectivity of radiolabelled ligand.…”

Section: Discussionmentioning

confidence: 99%

“…Although yohimbine and two of its isomers, corynanthine and x-yohimbine (or rauwolscine), have been widely used to characterize the al/M2 specificity of various ligands and physiological responses (Tanaka & Starke, 1980;Hedler, Stamm, Weitzell & Starke, 1981; Timmermans, Schoop, Kwa & Van Zwieten, 1981), the affinity of the isomers for the al-and x2-adrenoceptors has not been determined by in vitro binding studies.…”

Section: Introductionmentioning

confidence: 99%

Binding of yohimbine stereoisomers to α‐adrenoceptors in rat liver and human platelets

Ferry

Goodhardt

Hanoune

et al. 1983

British J Pharmacology

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Displacement of tritiated prazosin binding to rat liver plasma membranes and tritiated yohimbine human platelet membranes shows that (+)‐yohimbine, alloyohimbine and α‐yohimbine (rauwolscine) are selective α2‐adrenoceptor antagonists (KDα1/KDα2:635, 46.6 and 112 respectively) whereas corynanthine is more α1‐selective (KDα1/KDα2:0.036). 11‐Methoxy derivatives of α‐yohimbine and epi‐α‐yohimbine are very weak α‐adrenoceptor blockers. It is concluded that the aromatic A ring, the Nb atom, and the carboxymethyl moiety are important for the binding of yohimbine to the α‐adrenoceptor, the carboxymethyl group being important for the α1/α2 specificity of the molecule.

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“…Receptores que controlam o armazenamento e/ou a liberação de dopamina neuronal central e noradrenalina são adrenorreceptores alfa 2 (HEDLER et al, 1981).…”

Section: Sistema Nervoso Central (Snc)unclassified

Contenção farmacológica em primatas não-humanos com emprego de ketamina e xilazina. Uma revisão bibliográfica

Miranda¹,

Cabala²,

Atan³

et al. 2011

Pubvet

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Functional characterization of central α-adrenoceptors by yohimbine diastereomers

Cited by 98 publications

References 26 publications

Lipomobilizing effects of procaterol and yohimbine in the conscious dog: comparison of endocrinological, metabolic and cardiovascular effects

Lipomobilizing effects of procaterol and yohimbine in the conscious dog: comparison of endocrinological, metabolic and cardiovascular effects

Binding of yohimbine stereoisomers to α‐adrenoceptors in rat liver and human platelets

Contenção farmacológica em primatas não-humanos com emprego de ketamina e xilazina. Uma revisão bibliográfica

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