DT-Web

DB00386 - Alseroxylon


Identification
Name Alseroxylon
Accession Number DB00386 (APRD00786)
Type small molecule
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
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight Not Available
Groups approved
Monoisotopic Weight Not Available
Pharmacology
Indication For the treatment of hypertension and as an adjunct in the management of angina pectoris.
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
Protein binding Not Available
Biotransformation Not Available
Route of elimination Not Available
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions
Drug Mechanism of 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


Synaptic vesicular amine transporter
Name Synaptic vesicular amine transporter
Gene Name SLC18A2
Pharmacological action yes
Actions inhibitor
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
DTHybrid score 0.5194

Predictions


Id Partner name Gene Name Score
1636 Trace amine-associated receptor 1 TAAR1 0.1025
713 Sodium-dependent dopamine transporter SLC6A3 0.0714
556 Alpha-1A adrenergic receptor ADRA1A 0.0659
540 Sodium-dependent noradrenaline transporter SLC6A2 0.053
824 Sodium-dependent serotonin transporter SLC6A4 0.0387
4119 Cytochrome P450 2D6 CYP2D6 0.032
3939 Amine oxidase [flavin-containing] B MAOB 0.0309
3941 Amine oxidase [flavin-containing] A MAOA 0.0308
318 Alpha-2A adrenergic receptor ADRA2A 0.027
5251 Carbonyl reductase [NADPH] 1 CBR1 0.0238
982 Cocaine- and amphetamine-regulated transcript protein CARTPT 0.0204
502 5-hydroxytryptamine 2A receptor HTR2A 0.0172
831 D(2) dopamine receptor DRD2 0.0149
6147 Solute carrier family 22 member 3 SLC22A3 0.0143
474 Acetylcholinesterase ACHE 0.0132
118 Organic cation/carnitine transporter 2 SLC22A5 0.0125
4120 NADPH--cytochrome P450 reductase POR 0.0123
3923 Cholinesterase BCHE 0.0121
378 Alpha-2C adrenergic receptor ADRA2C 0.0114
629 Alpha-2B adrenergic receptor ADRA2B 0.0112
436 5-hydroxytryptamine 2B receptor HTR2B 0.011
590 5-hydroxytryptamine 2C receptor HTR2C 0.0097
776 Bile salt export pump ABCB11 0.0095
632 Alpha-1B adrenergic receptor ADRA1B 0.0095
6144 Solute carrier family 22 member 2 SLC22A2 0.0087
6145 Solute carrier family 22 member 1 SLC22A1 0.0084
1735 Canalicular multispecific organic anion transporter 1 ABCC2 0.0082
1517 Beta-3 adrenergic receptor ADRB3 0.0079
6030 Cytochrome P450 2B6 CYP2B6 0.0076
5718 Cytochrome P450 2A6 CYP2A6 0.0074
4118 Cytochrome P450 3A5 CYP3A5 0.007
1588 Multidrug resistance protein 1 ABCB1 0.0063
193 Beta-1 adrenergic receptor ADRB1 0.0057
4512 Cytochrome P450 3A4 CYP3A4 0.0056
766 Beta-2 adrenergic receptor ADRB2 0.0056
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