You are using an unsupported browser. Please upgrade your browser to a newer version to get the best experience on DrugBank.
Identification
NameAlseroxylon
Accession NumberDB00386  (APRD00786)
Typesmall molecule
Groupswithdrawn
Description

A fat-soluble alkaloidal fraction extracted from the root of Rauwolfia serpentina, containing reserpine and other nonadrenolytic amorphous alkaloids; used as a sedative in psychoses, in mild hypertension, and as an adjunct to more potent hypotensive drugs. Alseroxylon has been discontinued in the US market.

Structure
Thumb
Synonyms
SynonymLanguageCode
AlseroxylonNot AvailableJAN
EgalinNot AvailableNot Available
Rau-TabNot AvailableNot Available
RautensinNot AvailableNot Available
RauwiloidNot AvailableNot Available
SaltsNot Available
Brand namesNot Available
Brand mixturesNot Available
CategoriesNot Available
CAS number8001-95-4
WeightNot Available
Chemical FormulaNot Available
InChI KeyNot Available
InChINot Available
IUPAC NameNot Available
SMILESNot Available
Mass SpecNot Available
Taxonomy
KingdomNot Available
SuperclassNot Available
ClassNot Available
SubclassNot Available
Direct parentNot Available
Alternative parentsNot Available
SubstituentsNot Available
Classification descriptionNot Available
Pharmacology
IndicationFor the treatment of hypertension and as an adjunct in the management of angina pectoris.
PharmacodynamicsAlseroxylon is a purified extract of Rauwolfia serpentina, containing reserpine and other amorphous alkaloids. Alseroxylon is an indole alkaloid antipsychotic and antihypertensive drug known to irreversibly bind to storage vesicles of neurotransmitters such as dopamine, norepinephrine, and serotonin. This leads to depletion of the neurotransmitters and subsequent depression in humans.
Mechanism of actionThe antihypertensive actions of alseroxylon are a result of its ability to deplete catecholamines from peripheral sympathetic nerve endings. Alseroxylon almost irreversibly blocks the accumulation of noradrenaline and dopamine into synaptic vesicles by inhibiting the Vesicular Monoamine Transporters (VMAT). This depletion ultimately affects the carotid pressoreceptors which leads to a decrease in vascular pressure.
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
Metabolism
Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
Property Value Probability
Human Intestinal Absorption Not Available Not Available
Blood Brain Barrier Not Available Not Available
Caco-2 permeable Not Available Not Available
P-glycoprotein substrate Not Available Not Available
P-glycoprotein inhibitor I Not Available Not Available
P-glycoprotein inhibitor II Not Available Not Available
Renal organic cation transporter Not Available Not Available
CYP450 2C9 substrate Not Available Not Available
CYP450 2D6 substrate Not Available Not Available
CYP450 3A4 substrate Not Available Not Available
CYP450 1A2 substrate Not Available Not Available
CYP450 2C9 substrate Not Available Not Available
CYP450 2D6 substrate Not Available Not Available
CYP450 2C19 substrate Not Available Not Available
CYP450 3A4 substrate Not Available Not Available
CYP450 inhibitory promiscuity Not Available Not Available
Ames test Not Available Not Available
Carcinogenicity Not Available Not Available
Biodegradation Not Available Not Available
Rat acute toxicity Not Available Not applicable
hERG inhibition (predictor I) Not Available Not Available
hERG inhibition (predictor II) Not Available Not Available
Pharmacoeconomics
Manufacturers
  • Novartis consumer health inc
  • 3m pharmaceuticals inc
PackagersNot Available
Dosage forms
FormRouteStrength
TabletOral
PricesNot Available
PatentsNot Available
Properties
Statesolid
Experimental PropertiesNot Available
Predicted PropertiesNot Available
Spectra
SpectraNot Available
References
Synthesis ReferenceNot Available
General ReferenceNot Available
External Links
ResourceLink
Therapeutic Targets DatabaseDAP001243
PharmGKBPA164746411
ATC CodesNot Available
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
EpinephrineIncreased arterial pressure
FenoterolIncreased arterial pressure
OrciprenalineIncreased arterial pressure
PhenylephrineIncreased arterial pressure
PhenylpropanolamineIncreased arterial pressure
PseudoephedrineIncreased arterial pressure
TerbutalineIncreased arterial pressure
Food InteractionsNot Available

Targets

1. Synaptic vesicular amine transporter

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: inhibitor

Components

Name UniProt ID Details
Synaptic vesicular amine transporter Q05940 Details

References:

  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed
  3. FORD RV, MOYER JH: Rauwolfia toxicity in the treatment of hypertension; comparative toxicity of reserpine and alseroxylon. Postgrad Med. 1958 Jan;23(1):41-8. Pubmed
  4. SCHLAGEL CA, NELSON JW: Rauwolfia hypotension. II. Action of the alseroxylon alkaloids and epinephrine on the carotid pressoreceptors. J Am Pharm Assoc Am Pharm Assoc (Baltim). 1957 Feb;46(2):103-9. Pubmed
  5. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed

Comments
comments powered by Disqus
Drug created on June 13, 2005 07:24 / Updated on March 14, 2014 15:42