Dimiracetam
Bicyclic racetam studied for neuropathic pain; lowers NMDA-linked glutamate release, mostly preclinical data.
Pharmacology
Contents
WHAT IS DIMIRACETAM?
Detailed overview
Dimiracetam is a bicyclic racetam-related compound originally developed as a cognition enhancer (Pinza et al., 1993) and later studied in neuropathic pain research. Its main described action is reducing NMDA-receptor-driven glutamate release, chiefly in the spinal cord, and in animal models it produces a durable reduction of pain hypersensitivity (nerve injury, chemotherapy and osteoarthritis models). The effect accumulates with repeated dosing and persists after the compound has cleared. Human efficacy data are essentially unpublished: the compound entered Phase I/II clinical trials (HIV-associated and osteoarthritis pain), but the results are not available, so the evidence level is currently reference-only.
Mechanism
Reduces NMDA-linked glutamate release
Evidence
Mostly preclinical (animal models)
Legal status
Investigational; AU: prescription-only
Receptor profile
- NMDA receptors (GluN1 / GluN2A)Moderate
- Glutamatergic signalingModerate
- Neuropathic pain pathwaysModerate
- Learning / memory circuitsWeak
Safety
Side effects, stop signs, contraindications
Side effects · 4
- Described as well tolerated in animal studies; human safety is not fully established
- A detailed human side-effect profile is not published in the public literature
- As an NMDA-glutamatergic modulator, dose-dependent central nervous system effects (e.g. dizziness, headache) cannot be theoretically excluded
- No long-term human safety data are available
Contraindications · 4
- Pregnancy and breastfeeding: no safety data, should be avoided
- Hepatic or renal impairment: no human pharmacokinetic data, caution / medical supervision
- Investigational compound: not approved for self-medication outside a clinical trial
- Prescription-only in Australia (Schedule 4): a legal restriction applies
Related Nootropics
Same therapeutic category
Studies
Related research and clinical findings
Broad spectrum and prolonged efficacy of dimiracetam in models of neuropathic pain
Fariello RG, Ghelardini C, Di Cesare Mannelli L, Bonanno G, Pittaluga A, Milanese M, Misiano P, Farina C
Pharmacological Profile of MP-101, a Novel Non-racemic Mixture of R- and S-dimiracetam with Increased Potency in Rat Models of Cognition, Depression and Neuropathic Pain
Bonifacino T, Micheli L, Torazza C, Ghelardini C, Farina C, Bonanno G
A rat model of FOLFOX-induced neuropathy: effects of oral dimiracetam in comparison with duloxetine and pregabalin
Di Cesare Mannelli L, Maresca M, Micheli L, Farina C, Scherz MW, Ghelardini C
A model of neuropathic pain induced by sorafenib in the rat: Effect of dimiracetam
Di Cesare Mannelli L, Maresca M, Farina C, Scherz MW, Ghelardini C
Synthesis and pharmacological activity of a series of dihydro-1H-pyrrolo[1,2-a]imidazole-2,5(3H,6H)-diones, a novel class of potent cognition enhancers
Pinza M, Farina C, Cerri A, Pfeiffer U, Riccaboni MT, Banfi S
FAQ
FAQ
Bicyclic racetam studied for neuropathic pain; lowers NMDA-linked glutamate release, mostly preclinical data.
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Structure & chemistry
The information here is strictly for educational and scientific purposes. It does not replace medical advice or clinical consultation, and it does not encourage illegal substance or pharmaceutical use. Data is sourced. When in doubt, consult your doctor.