DT-Web

DB01463 - Fencamfamine


Identification
Name Fencamfamine
Accession Number DB01463
Type small molecule
Description Fencamfamine (Glucoenergan, Reactivan) is a stimulant which was developed in the 1960s as an appetite suppressant, but was later withdrawn for this application due to problems with dependence and abuse. It is around half the potency of dexamphetamine, and is prescribed at a dose of 10-60mg, although abusers of the drug tend to rapidly develop tolerance and escalate their dose. Reactivan is still rarely used for treating depressive day-time fatigue, lack of concentration and lethargy, particularly in individuals who have chronic medical conditions, as its favourable safety profile makes it the most suitable drug in some cases. [Wikipedia]
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 215.3339
Groups illicit
Monoisotopic Weight 215.167399677
Pharmacology
Indication For the the treatment of depressive fatigue in convalescence and other debilitated states as well as in the treatment of depressive day-time fatigue, lack of concentration and lethargy.
Mechanism of action Fencamfamine acts as an indirect dopamine agonist. It releases dopamine by a similar mechanism to amphetamines, but is 10x less potent than dexamphetamine at producing this effect. The drug seems to inhibit the dopamine transporter (DAT) that removes dopamine from the synapses. This inhibition of DAT blocks the reuptake of dopamine and norepinephrine into the presynaptic neuron, increasing the amount of dopamine in the synapse. It also stimulates the release of dopamine and norepinephrine into the synapse. Finally, it increases the magnitude of dopamine release after a stimulus, increasing the salience of stimulus. Also unlike amphetamines, fencamfamine does not inhibit the action of monoamine oxidase enzymes and so is somewhat safer. Some experiments also suggest a role for opioid receptors in the activity of fencamfamine, as low doses can cause paradoxical sedation, and some effects of the drug are blocked by naloxone.
Absorption Not Available
Protein binding Not Available
Biotransformation Not Available
Route of elimination Not Available
Toxicity Overdosage is characterised by nausea, agitation and restlessness, dryness of the mouth, dizziness and tremor. In gross overdosage the above symptoms may also be associated with dyspnoea, tachycardia, disorientation and convulsions.
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions Not Available
Food Interactions Not Available

Targets


Sodium-dependent dopamine transporter
Name Sodium-dependent dopamine transporter
Gene Name SLC6A3
Pharmacological action yes
Actions inhibitor
References
  • Seyfried CA: Dopamine uptake inhibiting versus dopamine releasing properties of fencamfamine: an in vitro study. Biochem Pharmacol. 1983 Aug 1;32(15):2329-31. - Pubmed
  • Li SM, Campbell BL, Katz JL: Interactions of cocaine with dopamine uptake inhibitors or dopamine releasers in rats discriminating cocaine. J Pharmacol Exp Ther. 2006 Jun;317(3):1088-96. Epub 2006 Feb 14. - Pubmed
DTHybrid score 0.3505

Predictions


Id Partner name Gene Name Score
540 Sodium-dependent noradrenaline transporter SLC6A2 0.1333
824 Sodium-dependent serotonin transporter SLC6A4 0.0891
4119 Cytochrome P450 2D6 CYP2D6 0.0503
131 Synaptic vesicular amine transporter SLC18A2 0.0422
3941 Amine oxidase [flavin-containing] A MAOA 0.0325
492 Histamine H1 receptor HRH1 0.0292
3939 Amine oxidase [flavin-containing] B MAOB 0.0284
632 Alpha-1B adrenergic receptor ADRA1B 0.0279
4512 Cytochrome P450 3A4 CYP3A4 0.0234
556 Alpha-1A adrenergic receptor ADRA1A 0.0234
1636 Trace amine-associated receptor 1 TAAR1 0.0192
6016 Cytochrome P450 2C19 CYP2C19 0.0182
318 Alpha-2A adrenergic receptor ADRA2A 0.018
4200 Cytochrome P450 1A2 CYP1A2 0.0164
198 Sodium channel protein type 10 subunit alpha SCN10A 0.0153
6030 Cytochrome P450 2B6 CYP2B6 0.0153
4757 Cytochrome P450 2C9 CYP2C9 0.0148
103 Muscarinic acetylcholine receptor M1 CHRM1 0.0127
706 Glutamate [NMDA] receptor subunit 3A GRIN3A 0.0122
341 5-hydroxytryptamine 3 receptor HTR3A 0.0121
502 5-hydroxytryptamine 2A receptor HTR2A 0.0117
982 Cocaine- and amphetamine-regulated transcript protein CARTPT 0.0095
3923 Cholinesterase BCHE 0.0094
6147 Solute carrier family 22 member 3 SLC22A3 0.0084
4118 Cytochrome P450 3A5 CYP3A5 0.0083
1588 Multidrug resistance protein 1 ABCB1 0.0081
1181 Alpha-1-acid glycoprotein 1 ORM1 0.0078
118 Organic cation/carnitine transporter 2 SLC22A5 0.0074
1656 CYP2B protein CYP2B 0.0074
629 Alpha-2B adrenergic receptor ADRA2B 0.0073
458 Neuronal acetylcholine receptor subunit alpha-10 CHRNA10 0.0073
590 5-hydroxytryptamine 2C receptor HTR2C 0.0067
6144 Solute carrier family 22 member 2 SLC22A2 0.0063
193 Beta-1 adrenergic receptor ADRB1 0.0062
766 Beta-2 adrenergic receptor ADRB2 0.0061
1757 Myeloperoxidase MPO 0.006
5718 Cytochrome P450 2A6 CYP2A6 0.0058
6107 Cytochrome P450 3A7 CYP3A7 0.0057
813 Neuronal acetylcholine receptor subunit alpha-2 CHRNA2 0.0057
4120 NADPH--cytochrome P450 reductase POR 0.0057
378 Alpha-2C adrenergic receptor ADRA2C 0.0053
436 5-hydroxytryptamine 2B receptor HTR2B 0.0052
6145 Solute carrier family 22 member 1 SLC22A1 0.0042
6013 Cytochrome P450 2E1 CYP2E1 0.004
320 5-hydroxytryptamine 1A receptor HTR1A 0.0039
215 Sodium channel protein type 11 subunit alpha SCN11A 0.0039
6079 Neuronal acetylcholine receptor subunit alpha-3 CHRNA3 0.0038
1517 Beta-3 adrenergic receptor ADRB3 0.0037
23 D(1A) dopamine receptor DRD1 0.0035
4924 Cytochrome P450 2C8 CYP2C8 0.0035
6164 POU domain, class 5, transcription factor 1 POU5F1 0.0033
831 D(2) dopamine receptor DRD2 0.0032
1732 ATP-binding cassette sub-family G member 2 ABCG2 0.0026
153 Dopamine beta-hydroxylase DBH 0.0025
220 Sodium channel protein type 5 subunit alpha SCN5A 0.0022
3810 Catechol O-methyltransferase COMT 0.002
163 D(1B) dopamine receptor DRD5 0.0019
617 Muscarinic acetylcholine receptor M2 CHRM2 0.0019
432 D(4) dopamine receptor DRD4 0.0018
638 D(3) dopamine receptor DRD3 0.0018
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