Compound Code |
KAT-5HT-DA-01 |
Pharmacological Tag |
Dual monoaminergic anorectic |
Structural Class |
Fenfluramine: substituted phenethylamine
Phentermine: α-methylated amphetamine
|
Mechanism (Putative) |
Fenfluramine:
→ SERT substrate → serotonin efflux
→ 5-HT2C receptor agonism → satiety signaling
→ VMAT2 interaction → vesicular depletion
Phentermine:
→ DAT/NET inhibition
→ Dopaminergic elevation → hunger suppression
→ Sympathomimetic excitation
|
Functional Role |
Serotonin-mediated appetite suppression
Dopamine-driven vigilance and metabolic activation
Anorectic synergy: satiety + stimulation
|
Structural Analogues |
Dexfenfluramine
Methamphetamine
MDMA
Sibutramine
Mazindol
|
Predicted Onset |
Oral: 20–40 min (combined) |
Predicted Duration |
6–8 hours (dose-dependent) |
Affinity Profile |
SERT >>> DAT > NET
Minimal affinity for adrenergic or histaminergic targets
|
Computational Predictions |
CNS Activity: High
BBB Penetration: Positive (both components)
5-HT2B Agonism (Fenfluramine): Present → valvular risk
Mutagenicity: Low
Neurotoxicity Risk: High (monoamine depletion at supratherapeutic doses)
Metabolism:
→ Fenfluramine → norfenfluramine (active)
→ Phentermine → hydroxylation + N-dealkylation
|
Interpretation |
A dual molecule program designed to cancel appetite by both inducing satiety and suppressing seeking
behavior.
Strategically banned, pharmacologically instructive.
Fen-Phen is a historic neurochemical system: metabolic totalitarianism via neurotransmitter orthodoxy.
Proof of concept: desire can be disabled.
|