4-Methylpregabalin
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4-Methylpregabalin is a drug developed by
However these drugs are still of relatively low potency, and scientists have struggled for years to come up with an improvement on pregabalin, with increasing pressure to find a suitably improved replacement before the
This explained the previous failures, as most alterations to the pregabalin molecule which increase affinity for the α2δ channels and therefore increase apparent potency in the test tube, were found to also dramatically reduce binding to the system L transporter, and with no assisted transport into the brain, blood–brain barrier penetration was minimal and the drugs were inactive in animals. However, after extensive searching it was discovered that one enantiomer of the relatively simple derivative 4-methylpregabalin, was both 4× higher in binding affinity to α2δ channels than pregabalin, and also retained similar affinity for the system L transporter. This was tested in animals and as hoped, was found to have similar effectiveness to pregabalin as an analgesic and with around 2–3× the potency.[2]
It remains unclear at this stage whether (3R,4R)-4-methylpregabalin will now be further developed for medical use in humans however, given the recent development of several competing drugs from the same family which are much further advanced in clinical trials.
See also
- Atagabalin
- Gabapentin enacarbil
- PD-217,014
- CD98 – large neutral amino acid transporter (LAT1)
References
- ^ "Fee Transmittal for FY 2005" (PDF). Food and Drug Administration. Archived from the original (PDF) on 2011-08-20. Retrieved 2013-06-02.
- PMID 15801823.