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[3H]rauwolscine (alpha-yohimbine): a specific antagonist radioligand for brain alpha 2-adrenergic receptors.

Abstract：

:[3H]Rauwolscine, a specific and potent alpha 2-antagonist radioligand, was used to characterize alpha 2-receptor binding in bovine cerebral cortex. [3H]Rauwolscine binding was reversible, stereospecific, and saturable. Association, dissociation, and saturation studies revealed one site interactions (k -1/k+1 = 1.2 nM, KD = 2.5 nM, Bmax = 160 fmol/mg protein) and competition studies indicated that [3H]rauwolscine labeled the alpha 2-receptor. Agonists inhibited [3H]rauwolscine binding in a shallow, GTP-sensitive manner. These results suggest that [3H]rauwolscine specifically labels both the high and low affinity states of the alpha 2-receptor in brain membranes.

journal_name

Eur J Pharmacol

journal_title

European journal of pharmacology

authors

Perry BD,U'Prichard DC

doi

10.1016/0014-2999(81)90123-0

subject

Has Abstract

pub_date

1981-12-17 00:00:00

pages

461-4

issue

4

eissn

0014-2999

issn

1879-0712

pii

0014-2999(81)90123-0

journal_volume

76

pub_type

杂志文章

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