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Rauwolscine hydrochloride

SKU: orb1221947

Description

Rauwolscine, a natural alkaloid, is a specific and reversible α2-adrenergic receptor antagonist (Ki: 12 nM). It is a stereoisomer of yohimbine, which potently antagonizes both α1- and α2-adrenergic receptors. Rauwolscine also acts as a receptor antagonist at the serotonin 5-HT2B receptor (Ki: 14.3 nM) and as a weak partial agonist at 5-HT1A (IC50: 1.3 μM). The α2-adrenergic receptor has diverse physiological functions and antagonists like rauwolscine have numerous applications, including the modulation of mood and behavior.(In Vitro):[3H]Rauwolscine binding to α2 adrenergic receptor is reversible, stcreospccific, and saturable. [3H]Rauwolscine specifically labels both the high and low affinity states of the α2 adrenergic receptor in brain membranes. [3H]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 [3H]5-HT as a radioligand, rauwolscine is determined to have relatively high affinity for the human receptor (Ki human=14.3 nM, Ki rat=35.8 nM). Saturation studies shows that the affinity of [3H]Rauwolscine is similar in mouse, rat, rabbit, dog (2.33-3.03 nM) except man where it is significantly higher (0.98 nM) .

Images & Validation

Key Properties

CAS Number6211-32-1
MW390.9
Purity>98% (HPLC)
FormulaC21H27ClN2O3
SMILESCl.[H][C@]12CC[C@H](O)[C@@H](C(=O)OC)[C@@]1([H])C[C@]1([H])N(CCc3c1[nH]c1ccccc31)C2
TargetMicrotubule/Tubulin
SolubilityDMSO : 6 mg/mL 15.35 mM; H2O : 5 mg/mL 12.79 mM

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

α-Yohimbine hydrochloride | Isoyohimbine hydrochloride

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Rauwolscine hydrochloride (orb1221947)

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