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Rauwolscine hydrochloride is a potent and specific α2 adrenergic receptor antagonist with a K_i of 12 nM.

[H]Rauwolscine binding to α2 adrenergic receptor is reversible, stcreospccific, and saturable. [H]Rauwolscine specifically labels both the high and low affinity states of the α2 adrenergic receptor in brain membranes. [H]Rauwolscine also behaves as a 5-HT1A receptor agonist and this conclusion is compatible with earlier functional studies, indicating that rauwolscine (as well as yohimbine) has agonistic properties at the level of 5-HT autoreceptors. When using [H]5-HT as a radioligand, rauwolscine is determined to have relatively high affinity for the human receptor (K_i human=14.3 nM, K_i rat=35.8 nM). Saturation studies shows that the affinity of [H]Rauwolscine is similar in mouse, rat, rabbit, dog (2.33-3.03 nM) except man where it is significantly higher (0.98 nM) .

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