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Piclamilast (RP-73401) is a highly potent, subnanomolar pan-PDE4 inhibitor used mainly as a pharmacological reference tool and high-affinity rolipram-binding-site ligand. It was explored for COPD and asthma but never developed. Its most cognition-relevant finding is a 2022 mouse study in which post-ischemia piclamilast was neuroprotective and preserved memory through CREB, an effect abolished by a CREB inhibitor. There is no human data.
- Subnanomolar, well-characterized PDE4 inhibition used as a research benchmark
- CREB-dependent neuroprotection and memory rescue in a rodent stroke model
- Clean mechanistic tool for studying the cAMP/PKA/CREB pathway
- Expected strong emetic/GI liability (PDE4 class)
- Piclamilast is used by scientists mainly as a yardstick; a reference PDE4 inhibitor to calibrate the potency of other compounds.
- In a 2022 stroke model, its memory-preserving effect vanished when CREB was blocked, pinpointing the pathway responsible.
- Despite subnanomolar potency, it was never tested in a single human trial.
Mechanism
An extremely potent competitive inhibitor of the PDE4 catalytic site (pan A/B/C/D) that raises , activating PKA and and increasing . In the stroke model, the neuroprotective benefit was shown to depend on CREB; blocking CREB abolished it.
receptor fingerprint
PDE4 (pan A/B/C/D)Inhibits
Activates (via cAMP/PKA)
Memory after ischemiaPreserves
Upregulates
Evidencehow good the literature is
Rodent: post-ischemia neuroprotection and memory rescue that is CREB-dependent. Ex-vivo and in-silico: a reference PDE4B ligand, less potent than rolipram or roflumilast in a ureteral assay. No human data of any kind.
Dosingtypical ranges, not medical advice
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Safetyrisks and cautions, not medical advice
There is no human safety data. As a potent non-selective PDE4 inhibitor, strong emetic and gastrointestinal liability would be expected. This is a research chemical, not a supplement or medicine.
History
Developed as an experimental PDE4 inhibitor and adopted by pharmacologists as a reference ligand for the high-affinity rolipram-binding-site conformer. It was investigated for respiratory disease but never advanced to clinical development.
Reputation
Within PDE4 research it is respected as a potent, well-characterized tool compound and benchmark ligand. It has no reputation as a therapeutic or nootropic because it was never tested in humans.
Resources
This entry is here for reference.
Research
- 1.Neuroprotective Effect of Piclamilast-Induced Post-Ischemia Pharmacological Treatment in Mice.
- 2.Inhibition of PDE-4 isoenzyme attenuates frequency and overall contractility of agonist-evoked ureteral phasic contractions.
- 3.Potential PDE4B inhibitors as promising candidates against SARS-CoV-2 infection.
3 listed here; entry last updated August 2026
Reviews
My notesprivate to this device
FAQ
Can I take piclamilast for memory?
No. It has never been tested in humans and has no established dose or safety profile; its neuroprotection data are entirely from rodents.
What is it used for?
It is a laboratory reference tool; a potent PDE4 inhibitor used to benchmark other compounds and study the cAMP/CREB pathway.
Is it safe?
Unknown in humans. As a potent PDE4 inhibitor it would be expected to cause the class's nausea and GI effects.
Limitations of the evidence
- No human safety data
- Not characterized for human use
Adverse effects
- Expected strong emetic/GI liability (PDE4 class)