Talk:Baclofen: Difference between revisions

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Similarly to [[phenibut]] (β-phenyl-GABA), as well as [[pregabalin]] (β-isobutyl-GABA), which are close analogues of baclofen, baclofen (β-(4-chlorophenyl)-GABA) has been found to block α2δ subunit-containing voltage-gated calcium channels (VGCCs). However, it is weaker relative to phenibut in this action (Ki = 23 and 39 μM for R- and S-phenibut and 156 μM for baclofen). Moreover, baclofen is in the range of 100-fold more potent by weight as an agonist of the [[GABA]]<sub>B</sub> receptor in comparison to [[phenibut]], and in accordance, is used at far lower relative dosages. As such, the actions of baclofen on α2δ subunit-containing VGCCs are likely not clinically-relevant.<ref>R-phenibut binds to the α2-δ subunit of voltage-dependent calcium channels and exerts gabapentin-like anti-nociceptive effects. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/26234470</ref>

The drug is rapidly absorbed after oral administration and is widely distributed throughout the body. Biotransformation is low: the drug is predominantly excreted unchanged by the kidneys.<ref>Plasma and urinary excretion kinetics of oral baclofen in healthy subjects. (link.springer.com / SpringerLink) | https://link.springer.com/article/10.1007/BF00558228</ref>

==Subjective effects==

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 Similarly to [[phenibut]] (β-phenyl-GABA), as well as [[pregabalin]] (β-isobutyl-GABA), which are close analogues of baclofen, baclofen (β-(4-chlorophenyl)-GABA) has been found to block α2δ subunit-containing voltage-gated calcium channels (VGCCs). However, it is weaker relative to phenibut in this action (Ki = 23 and 39 μM for R- and S-phenibut and 156 μM for baclofen). Moreover, baclofen is in the range of 100-fold more potent by weight as an agonist of the [[GABA]]<sub>B</sub> receptor in comparison to [[phenibut]], and in accordance, is used at far lower relative dosages. As such, the actions of baclofen on α2δ subunit-containing VGCCs are likely not clinically-relevant.<ref>R-phenibut binds to the α2-δ subunit of voltage-dependent calcium channels and exerts gabapentin-like anti-nociceptive effects. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/26234470</ref>
+The drug is rapidly absorbed after oral administration and is widely distributed throughout the body. Biotransformation is low: the drug is predominantly excreted unchanged by the kidneys.<ref>Plasma and urinary excretion kinetics of oral baclofen in healthy subjects. (link.springer.com / SpringerLink) | https://link.springer.com/article/10.1007/BF00558228</ref>
 ==Subjective effects==