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Alaproclate is one of the earliest selective serotonin reuptake inhibitors (SSRIs), developed by Astra AB in the 1970s as a candidate antidepressant. It was discontinued due to liver toxicity observed in animal studies and was never marketed.
- One of the earliest compounds to demonstrate selective serotonin reuptake inhibition, informing later SSRI development
- Studied as a candidate antidepressant in the 1970s
- Hepatotoxicity (liver complications) observed in animal studies, which ended its development
- NMDA channel-blocking activity showed partial PCP-like effects in animal discrimination models
Overview
A pioneering early SSRI, developed alongside zimelidine and indalpine, that got shelved over liver safety concerns before SSRIs became mainstream.
Mechanism
Alaproclate selectively inhibits the reuptake of () into presynaptic neurons, increasing serotonin availability, the same core mechanism used by later approved SSRIs. It also acts as a non-competitive at the -coupled ion channel, blocking -induced responses without the phencyclidine-like discriminative stimulus effects seen with dedicated NMDA channel blockers.
receptor fingerprint
transporter (SERT)Inhibitor
channelAntagonist
Safetyrisks and cautions, not medical advice
Development was discontinued after liver complications (hepatotoxicity) were observed in rodent studies, before the compound reached wide clinical use. Its NMDA channel-blocking activity produced only partial substitution for phencyclidine (PCP) in animal discrimination studies, suggesting a lower abuse-related liability than dedicated PCP-like NMDA antagonists.
Subjective profileweighing the evidence above
Historically important as an early proof that selective serotonin reuptake inhibition works, and rightly abandoned once liver toxicity showed up in animals. Its value now is as SSRI history; the approved drugs this line made possible are the ones with an actual safety record.
Resources
This entry is here for reference.
Research
- 1978first citedInhibitors of neuronal monoamine uptake. 2. Selective inhibition of 5-hydroxytryptamine uptake…
- 2003most recentEvaluation of the phencyclidine-like discriminative stimulus effects of novel NMDA channel bloc…
- 1.Inhibitors of neuronal monoamine uptake. 2. Selective inhibition of 5-hydroxytryptamine uptake by alpha-amino acid esters of phenethyl alcohols
- 2.Alaproclate acts as a potent, reversible and noncompetitive antagonist of the NMDA receptor coupled ion flow
- 3.Evaluation of the phencyclidine-like discriminative stimulus effects of novel NMDA channel blockers in rats
3 listed here; entry last updated August 2026
Reviews
My notesprivate to this device
FAQ
What is Alaproclate used for?
It was investigated in the 1970s as an antidepressant, one of the first SSRIs developed, but it was never marketed due to liver toxicity concerns.
How does Alaproclate work?
It selectively blocks the reuptake of serotonin, increasing serotonin levels at nerve synapses, and it also non-competitively blocks NMDA receptor channels.
Is Alaproclate well-researched?
It has published pharmacology from its original development era and later NMDA-receptor characterization studies, but it never underwent modern-scale clinical trials.
Adverse effects
- Hepatotoxicity (liver complications) observed in animal studies, which ended its development
- NMDA channel-blocking activity showed partial PCP-like effects in animal discrimination models