DrugBank: Alseroxylon (DB00386)

targets (1)

Identification

Name

Alseroxylon

Accession Number

DB00386 (APRD00786)

Type

small molecule

Groups

approved

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.

Structure

Synonyms

Not Available

Salts

Not Available

Brand names

Name	Company
Rautensin
Rauwiloid

Brand mixtures

Not Available

Categories

Adrenergic Uptake Inhibitors

CAS number

8001-95-4

Weight

Not Available

Chemical Formula

Not Available

InChI Key

Not Available

InChI

Not Available

IUPAC Name

Not Available

SMILES

Not Available

Mass Spec

Not Available

Taxonomy

Kingdom

Not Available

Classes

Not Available

Substructures

Not Available

Pharmacology

Indication

For the treatment of hypertension and as an adjunct in the management of angina pectoris.

Pharmacodynamics

Alseroxylon 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 action

The 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.

Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism

Not Available

Route of elimination

Not Available

Half life

Not Available

Clearance

Not Available

Toxicity

Not Available

Affected organisms

Humans and other mammals

Pathways

Not Available

Pharmacoeconomics

Manufacturers

Novartis consumer health inc
3m pharmaceuticals inc

Packagers

Not Available

Dosage forms

Form	Route	Strength
Tablet	Oral

Prices

Not Available

Patents

Not Available

Properties

State

solid

Experimental Properties

Not Available

Predicted Properties

Not Available

References

Synthesis Reference

Not Available

General Reference

Not Available

External Links

Resource	Link
Therapeutic Targets Database	DAP001243
PharmGKB	PA164746411

ATC Codes

Not Available

AHFS Codes

Not Available

PDB Entries

Not Available

FDA label

Not Available

MSDS

Not Available

Interactions

Drug Interactions

Drug	Interaction
Epinephrine	Increased arterial pressure
Fenoterol	Increased arterial pressure
Orciprenaline	Increased arterial pressure
Phenylephrine	Increased arterial pressure
Phenylpropanolamine	Increased arterial pressure
Pseudoephedrine	Increased arterial pressure
Terbutaline	Increased arterial pressure

Food Interactions

Not Available

Targets
1. Synaptic vesicular amine transporter Pharmacological action: yes Actions: inhibitor Involved in the ATP-dependent vesicular transport of biogenic amine neurotransmitters. Pumps cytosolic monoamines including dopamine, norepinephrine, serotonin, and histamine into synaptic vesicles. Requisite for vesicular amine storage prior to secretion via exocytosis Organism class: human UniProt ID: Q05940 Gene: SLC18A2 Protein Sequence: FASTA Gene Sequence: FASTA SNPs: SNPJam Report References: Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed 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 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 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 Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed

Targets

1. Synaptic vesicular amine transporter

Pharmacological action: yes
Actions: inhibitor

Involved in the ATP-dependent vesicular transport of biogenic amine neurotransmitters. Pumps cytosolic monoamines including dopamine, norepinephrine, serotonin, and histamine into synaptic vesicles. Requisite for vesicular amine storage prior to secretion via exocytosis

Organism class: human
UniProt ID: Q05940 Link_out

Gene: SLC18A2 Link_out

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:

Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
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
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
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
Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed

Comments

Drug created on June 13, 2005 07:24 / Updated on February 14, 2012 11:41