It is well known that cannabis is effective for treating neuropathic pain. Recent evidence suggests that these analgesic effects are mediated by the glycine receptor rather than the cannabinoid receptors. This means that pain relief and benefits in other indications should be possible without the psychiatric side effects associated with cannabis and its primary active constituent tetrahydrocannabinol (THC). We are applying our biocatalytic drug optimization platform to cannabinoids to prepare selective glycine receptor modulators devoid of undesirable side effects.