Fen-Phen

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.