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The novel alpha2-adrenoceptor agonist [3H]mivazerol binds to non-adrenergic binding sites in human striatum membranes that are distinct from imidazoline receptors

par Flamez, Anja;De Backer, Jean Paul;Vauquelin, Georges;Gillard, Michel;Noyer, Jean-Max
Référence Neurochemistry international, 31, 1, page (125-129)
Publication Publié, 1997-07

Article révisé par les pairs

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Résumé :

The alpha2 adrenergic agonist [3H]mivazerol labelled two populations of binding sites in membranes from the human striatum. Forty per cent of the sites labelled by 3 nM [3H]mivazerol corresponded to alpha2 adrenergic receptors as they displayed a high affinity for (-)-adrenaline and for rauwolscine. The remaining binding was displaced by mivazerol with a pIC50 of 6.5 ± 0.1. These sites displayed higher affinity for dexmedetomidine (pIC50 = 7.1 ± 0.1), but much lower affinity for clonidine (pIC50 < 5.0) and for idazoxan (pIC50 = 5.1 ± 0.1). Mivazerol also showed low affinity for the [3H]clonidine-labelled I1 imidazoline receptors and for the [3H]idazoxan-labelled I2 receptors (pIC50 = 5.1 and 3.9, respectively). These results suggest that the non-adrenergic [3H]mivazerol binding sites are distinct from the imidazoline receptors in the human striatum.