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- W2038841020 abstract "(−)-[ 3 H]Dihydroalprenolol((−)-[ 3 H]DHA) binding in the rat hypothalamus appears to possess all the characteristics expected of physiologically relevant β-adrenergic receptors. Binding of (−)-[ 3 H]DHA to the hypothalamic sites was rapid (k 1 = 1.3 × 10 7 min −1 M −1 ) and also rapidly reversible. Binding was saturable at low concentrations of ligand( ~ 50–100 nM). The dissociation constant (K D ) of (−)-[ 3 H]DHA binding determined by equilibrium analysis was 19 nM. Binding displayed β-adrenergic specificity. β-Adrenergic agonists inhibited binding in the following order of potency: (−)-isoproterenol [Formula: see text] (−)-epinephrine > (−)-norepinephrine. Specific β-adrenergic antagonists (−)-propranol and (−)-alprenolol inhibited binding at low concentrations (K D = 25–50 nM) whereas the α-antagonist phentolamine inhibited binding at very high concentrations (K D = 42 μM). Interactions of both agonists and antagonists with the sites showed stereoselectivity. The (−)-isomers of all β-adrenergic agents tested were more potent than their respective (+)-isomers. These results suggest that specific receptor sites for β-adrenergic catecholamines are present in rat hypothalamus." @default.
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- W2038841020 date "1977-07-01" @default.
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- W2038841020 title "Identification of β-adrenergic receptors in rat hypothalamus" @default.
- W2038841020 doi "https://doi.org/10.1139/o77-100" @default.
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