data + articles · 2 listed
newest 1987spec sheet6 rows
Rolziracetam was developed as CI-911 during the 1980s racetam research wave that piracetam's success touched off across European and American pharma chemistry, one of many cyclic-imide/pyrrolidinone analogs screened for "amnesia-reversal" activity against scopolamine-induced memory deficits in rodents, the field's standard nootropic assay at the time. It performed in that classic screening model and had its metabolic disposition characterized in animal studies, but like most second-generation racetams it never accumulated the human efficacy data needed to reach market. The entire racetam class shared the same problem: a diffuse, hard-to-pin-down mechanism that made regulatory approval an uphill argument, and once the pharmaceutical industry's attention moved to more mechanistically defined drug classes, compounds like rolziracetam simply stopped being worth developing further.
- reversed electroconvulsive-shock amnesia in mice (dose-dependent, up to 92% reversal at 40 mg/kg)
- improved delayed-response task performance in aged rhesus monkeys
- rapid oral absorption (90%+) in animal pharmacokinetic studies
- demonstrated amnesia-reversal activity in classic scopolamine rodent models
- structurally part of the well-studied racetam/piracetam family
- metabolic disposition characterized in animal pharmacokinetic studies
- represents a documented branch of 1980s European/American nootropic drug chemistry
- Rolziracetam's elimination half-life after IV dosing in animals was under 25 minutes, one of the faster clearance rates among the racetams studied at Warner-Lambert.
- Rolziracetam is almost exclusively referenced in the literature under its development code, CI-911, rather than its generic name.
- It was one of many 1980s cyclic-imide racetam analogs screened in the same standard rat scopolamine-amnesia assay used to evaluate piracetam itself.
Mechanism
Pyrrolidinone racetam structurally related to piracetam; the specific molecular target was never firmly established, but it modulates cognitive performance in animal amnesia and aging models, broadly consistent with the racetam class's presumed and membrane-fluidity effects.
Safetyrisks and cautions, not medical advice
Rolziracetam (CI-911) is an early piracetam-family nootropic with a very thin published safety record; almost all data are preclinical (rats and aged monkeys), where it showed a wide margin of safety. It was reportedly evaluated in cognitively impaired human subjects, but no meaningful clinical trial or adverse-event data are published, so a documented human risk profile essentially does not exist. As a low-lipophilicity racetam its systemic exposure and off-target liabilities are not characterized, and racetams as a class are generally well tolerated with mild effects such as headache. Given the absence of controlled human safety data, it should be regarded as an unproven investigational compound rather than one with an established tolerability profile.
History
Synthesized and characterized in the 1980s under the code CI-911, part of the wave of piracetam analogs tested in scopolamine-amnesia rodent models; its metabolic disposition in animals was published in 1987; never advanced to human clinical development or market.
Subjective profileweighing the evidence above
A textbook second-generation racetam: active in the standard rat amnesia-reversal assay, mechanistically vague, and never commercially worth chasing past the animal lab.
Resources
This entry is here for reference.
Research
- 1.Metabolic disposition of Rolziracetam in laboratory animals
- 2.Amnesia-reversal activity of a series of cyclic imides
2 listed here; entry last updated July 2026
Reviews
My notesprivate to this device
FAQ
Was rolziracetam ever tested in humans?
No published human trial data exists; the compound stayed in animal pharmacology and metabolism studies before Warner-Lambert dropped it.
How is rolziracetam related to piracetam?
It is a pyrrolidinone racetam, chemically in the same family as piracetam, developed during the same 1980s wave of racetam analogs chasing a stronger cognitive-enhancement signal.
Was rolziracetam ever sold as a supplement or drug?
No. It stayed a research compound (CI-911) characterized in 1980s animal pharmacology and pharmacokinetic studies and never reached human trials, market, or commercial availability.
How is it related to piracetam?
It is a structurally related pyrrolidinone/cyclic-imide compound from the same broad racetam research family that piracetam originated, sharing the same diffuse, still-not-fully-defined proposed mechanism.
Limitations of the evidence
- no human safety data was ever published; the compound did not progress to clinical trials
- no human clinical trial data exists
- mechanism of action was never precisely resolved
- essentially unknown outside specialist racetam-chemistry literature
Notes and cautions
- never approved, marketed or commercially available