DT-Web

DB01089 - Deserpidine


Identification
Name Deserpidine
Accession Number DB01089 (APRD00906)
Type small molecule
Description Deserpidine is an ester alkaloid drug isolated from Rauwolfia canescens (family Apocynaceae) with antipsychotic and antihypertensive properties that has been used for the control of high blood pressure and for the relief of psychotic behavior.
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 578.6527
Groups approved
Monoisotopic Weight 578.262816202
Pharmacology
Indication For the treatment of hypertension.
Mechanism of action Deserpidine's mechanism of action is through inhibition of the ATP/Mg2+ pump responsible for the sequestering of neurotransmitters into storage vesicles located in the presynaptic neuron. The neurotransmitters that are not sequestered in the storage vesicle are readily metabolized by monoamine oxidase (MAO) causing a reduction in catecholamines.
Absorption Not Available
Protein binding Not Available
Biotransformation Not Available
Route of elimination Not Available
Toxicity Symptoms of overdose include dizziness or drowsiness (severe), flushing of skin, pinpoint pupils of eyes and slowed pulse.
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
  • Sievert MK, Hajipour AR, Ruoho AE: Specific derivatization of the vesicle monoamine transporter with novel carrier-free radioiodinated reserpine and tetrabenazine photoaffinity labels. Anal Biochem. 2007 Aug 1;367(1):68-78. Epub 2007 May 3. - Pubmed
  • Naudon L, Leroux-Nicollet I, Raisman-Vozari R, Botton D, Costentin J: Time-course of modifications elicited by reserpine on the density and mRNA synthesis of the vesicular monoamine transporter, and on the density of the membrane dopamine uptake complex. Synapse. 1995 Sep;21(1):29-36. - Pubmed
  • Erickson JD, Eiden LE, Hoffman BJ: Expression cloning of a reserpine-sensitive vesicular monoamine transporter. Proc Natl Acad Sci U S A. 1992 Nov 15;89(22):10993-7. - Pubmed
  • Mandela P, Chandley M, Xu YY, Zhu MY, Ordway GA: Reserpine-induced reduction in norepinephrine transporter function requires catecholamine storage vesicles. Neurochem Int. 2010 May-Jun;56(6-7):760-7. Epub 2010 Feb 20. - Pubmed
  • Fulton SC, Healy MD: Comparison of the effectiveness of deserpidine, reserpine, and alpha-methyltyrosine on brain biogenic amines. Fed Proc. 1976 Dec;35(14):2558-62. - Pubmed
  • Loeffler LJ, Schran HF: Antibody specificity studies for reserpine, its metabolites, and synthetic reserpine congeners: radioimmunoassay. J Pharm Sci. 1979 Nov;68(11):1433-5. - 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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