| Description | Rauwolscine hydrochloride is a potent and specific α2 adrenergic receptor antagonist with a Ki of 12 nM. |
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| Related Catalog | Signaling Pathways >>GPCR/G Protein >>Adrenergic ReceptorResearch Areas >>Neurological Disease |
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| Target | Ki: 12 nM (α2 adrenergic receptor)[1] |
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| 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[1]. [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[2]. 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)[3]. 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) [4]. |
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| 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 minivials containing 3.0 mL of a 95% Econofluor/5% Protosol 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]. |
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| References | [1]. Perry BD, et al. [3H]rauwolscine (alpha-yohimbine): a specific antagonist radioligand for brain alpha 2-adrenergic receptors. Eur J Pharmacol. 1981 Dec 17;76(4):461-4. [2]. De Vos H, et al. [3H]rauwolscine behaves as an agonist for the 5-HT1A receptors in human frontal cortex membranes. Eur J Pharmacol. 1991 May 25;207(1):1-8. [3]. Wainscott DB, et al. [3H]Rauwolscine: an antagonist radioligand for the cloned human 5-hydroxytryptamine2b (5-HT2B) receptor. Naunyn Schmiedebergs Arch Pharmacol. 1998 Jan;357(1):17-24. [4]. Neylon CB, et al. [3H]-rauwolscine binding to alpha 2-adrenoceptors in the mammalian kidney: apparent receptor heterogeneity between species. Br J Pharmacol. 1985 Jun;85(2):349-59. |
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CHEMICAL IDENTIFICATION - RTECS NUMBER :
- ZG1035000
- CHEMICAL NAME :
- 20-alpha-Yohimban-16-beta-carboxylic acid, 17-alpha-hydroxy-, methyl ester, hydrochloride
- CAS REGISTRY NUMBER :
- 6211-32-1
- LAST UPDATED :
- 199203
- DATA ITEMS CITED :
- 5
- MOLECULAR FORMULA :
- C21-H26-N2-O3.Cl-H
- MOLECULAR WEIGHT :
- 390.95
- WISWESSER LINE NOTATION :
- T F6 D5 C666 EM ON&&TTTJ TQ UVO1 &GH
HEALTH HAZARD DATAACUTE TOXICITY DATA - TYPE OF TEST :
- LDLo - Lowest published lethal dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 125 mg/kg
- TOXIC EFFECTS :
- Behavioral - convulsions or effect on seizure threshold
- REFERENCE :
- LDBU** "Zur Pharmakologie der Yohimbealkaloide, Dissertation," Langer, J., Institute fuer Pharmakologie und Experimentelle Therapie der Universitat Breslau, Poland, 1932 Volume(issue)/page/year: -,-,1932
- TYPE OF TEST :
- LDLo - Lowest published lethal dose
- ROUTE OF EXPOSURE :
- Subcutaneous
- SPECIES OBSERVED :
- Mammal - dog
- DOSE/DURATION :
- 20 mg/kg
- TOXIC EFFECTS :
- Behavioral - general anesthetic Behavioral - muscle contraction or spasticity Lungs, Thorax, or Respiration - dyspnea
- REFERENCE :
- LDBU** "Zur Pharmakologie der Yohimbealkaloide, Dissertation," Langer, J., Institute fuer Pharmakologie und Experimentelle Therapie der Universitat Breslau, Poland, 1932 Volume(issue)/page/year: -,-,1932
- TYPE OF TEST :
- LDLo - Lowest published lethal dose
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Rodent - rabbit
- DOSE/DURATION :
- 2 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- LDBU** "Zur Pharmakologie der Yohimbealkaloide, Dissertation," Langer, J., Institute fuer Pharmakologie und Experimentelle Therapie der Universitat Breslau, Poland, 1932 Volume(issue)/page/year: -,-,1932
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intraperitoneal
- SPECIES OBSERVED :
- Rodent - guinea pig
- DOSE/DURATION :
- 162 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- BSPHAV Bulletin des Sciences Pharmacologiques. (Paris, France) V.1-49, 1899-1942. For publisher information, see APFRAD. Volume(issue)/page/year: 47,33,1940
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Parenteral
- SPECIES OBSERVED :
- Amphibian - frog
- DOSE/DURATION :
- 200 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- BSPHAV Bulletin des Sciences Pharmacologiques. (Paris, France) V.1-49, 1899-1942. For publisher information, see APFRAD. Volume(issue)/page/year: 47,33,1940
|
| isoyohimbine |
| 20α-Yohimban-16β-carboxylic acid, 17α-hydroxy-, methyl ester, monohydrochloride (8CI) |
| EINECS 228-279-6 |
| rauwolscine |
| Yohimban-16-carboxylic acid, 17-hydroxy-, methyl ester, (15ξ,16β,17α,20α)-, hydrochloride (1:1) |
| Methyl (15ξ,16β,17α,20α)-17-hydroxyyohimban-16-carboxylate hydrochloride (1:1) |
| Methyl (1S,2S,4aS,13bS,14aS)-2-hydroxy-1,2,3,4,4a,5,7,8,13,13b,14,14a-dodecahydroindolo[2',3':3,4]pyrido[1,2-b]isoquinoline-1-carboxylate hydrochloride |
| Methyl-(1S,2S,4aS,13bS,14aS)-2-hydroxy-1,2,3,4,4a,5,7,8,13,13b,14,14a-dodecahydroindolo[2',3':3,4]pyrido[1,2-b]isochinolin-1-carboxylathydrochlorid |
| mesoyohimbine |
| Methyl (16β,17α,20α)-17-hydroxyyohimban-16-carboxylate hydrochloride (1:1) |
| Methyl (16β,17α,20α)-17-hydroxyyohimban-16-carboxylate hydrochloride |
| (16β,17α,20α)-17-Hydroxyyohimban-16-carboxylate de méthyle chlorhydrate |
| rauwolfscine hydrochloride |
| 20α-Yohimban-16β-carboxylic acid, 17α-hydroxy-, methyl ester, monohydrochloride |
| Methyl-(16β,17α,20α)-17-hydroxyyohimban-16-carboxylathydrochlorid |
| (1S,2S,4aS,13bS,14aS)-2-Hydroxy-1,2,3,4,4a,5,7,8,13,13b,14,14a-dodécahydroindolo[2',3':3,4]pyrido[1,2-b]isoquinoléine-1-carboxylate de méthyle chlorhydrate |
| rauwolscine hcl |
| Yohimban-16-carboxylic acid, 17-hydroxy-, methyl ester, (16β,17α,20α)-, hydrochloride (1:1) |
| Rauwolscine (hydrochloride) |
