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Rauwolscine hydrochloride

Rauwolscine hydrochloride
Rauwolscine hydrochloride (Isoyohimbine hydrochloride) , a natural alkaloid, is a specific and reversible α2-adrenergic receptor antagonist (Ki: 12 nM) [1]. It is a stereoisomer of yohimbine, which potently antagonizes both α1- and α2-adrenergic receptors [1]. Rauwolscine hydrochloride 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) [3]. The α2-adrenergic receptor has diverse physiological functions and antagonists like rauwolscine have numerous applications, including the modulation of mood and behavior [5].
Catalog No. T4429Cas No. 6211-32-1
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Purity:100%
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Rauwolscine hydrochloride

Purity: 99.95%
Catalog No. T4429Alias α-Yohimbine hydrochloride, Isoyohimbine hydrochloride, Corynanthidine hydrochlorideCas No. 6211-32-1

Rauwolscine hydrochloride (Isoyohimbine hydrochloride) , a natural alkaloid, is a specific and reversible α2-adrenergic receptor antagonist (Ki: 12 nM) [1]. It is a stereoisomer of yohimbine, which potently antagonizes both α1- and α2-adrenergic receptors [1]. Rauwolscine hydrochloride 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) [3]. The α2-adrenergic receptor has diverse physiological functions and antagonists like rauwolscine have numerous applications, including the modulation of mood and behavior [5].
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Pack SizePriceAvailabilityQuantity
50 mg$30In Stock
100 mg$42In Stock
500 mg$98In Stock
1 mL x 10 mM (in DMSO)$30In Stock
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Product Introduction

Bioactivity
Description
Rauwolscine hydrochloride (Isoyohimbine hydrochloride) , a natural alkaloid, is a specific and reversible α2-adrenergic receptor antagonist (Ki: 12 nM) [1]. It is a stereoisomer of yohimbine, which potently antagonizes both α1- and α2-adrenergic receptors [1]. Rauwolscine hydrochloride 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) [3]. The α2-adrenergic receptor has diverse physiological functions and antagonists like rauwolscine have numerous applications, including the modulation of mood and behavior [5].
Targets&IC50
α2-adrenoceptor:12 nM (Ki)
In vitro
[3H]Rauwolscine binding to the 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[1]. [3H]Rauwolscine also behaves as a 5-HT1A receptor agonist, indicating that rauwolscine (as well as yohimbine) has agonistic properties at the level of 5-HT autoreceptors[2]. When using [3H]5-HT as a radioligand, rauwolscine is determined to have a relatively high affinity for the human receptor (Ki: 14.3/35.8 nM, for human and rat)[3]. Saturation studies show that the affinity of [3H]Rauwolscine is similar in mouse, rabbit, rat, dog (2.33-3.03 nM) except man where it is significantly higher (0.98 nM) [4].
Kinase Assay
Fresh bovine frontal cortex is incubated in triplicate with [3H]Rauwolscine (82 Ci/mM, diluted). Incubation is terminated by filtration under reduced pressure over filters, which are then rinsed with ice-cold Tris-HCl buffer, dried overnight and added to disposable glass mini vials containing 3.0 mL of a 95% Econofluor/5% Protocol solution. Samples are counted by liquid scintillation spectrometry with an efficiency of 32%. (-)- [3H]Epinephrine binding to bovine cortex membranes is conducted at 25°C[1].
Aliasα-Yohimbine hydrochloride, Isoyohimbine hydrochloride, Corynanthidine hydrochloride
Chemical Properties
Molecular Weight390.9
FormulaC21H27ClN2O3
Cas No.6211-32-1
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 13.75 mg/mL (35.18 mM), Heating is recommended.
H2O: 5 mM, Heating is recommended.
Solution Preparation Table
H2O/DMSO
1mg5mg10mg50mg
1 mM2.5582 mL12.7910 mL25.5820 mL127.9100 mL
5 mM0.5116 mL2.5582 mL5.1164 mL25.5820 mL
DMSO
1mg5mg10mg50mg
10 mM0.2558 mL1.2791 mL2.5582 mL12.7910 mL
20 mM0.1279 mL0.6395 mL1.2791 mL6.3955 mL

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