Pharmacodynamics + GABA and analoguesat biological targets Compound GABAB GABAA 0.08 0.12 >100 >100 1.10 1.38<unk>  9.6 >100 4-F-phenibut 1.70 >100 Baclofen 0.13 >100 (R)-Baclofen 0.13 >100 (S)-Baclofen 74.0 >100 Values are IC50 (μM) in rat brain.<unk>  acts as a full agonist of the GABAB receptor, similarly to baclofen. It has between 30- to 68-fold lower affinity for the GABAB receptor than baclofen, and, in accordance, is used at far higher doses in comparison. (R)-Phenibut has more than 100-fold higher affinity for the GABAB receptor than does (S)-phenibut; hence, (R)-phenibut is the active enantiomer at the GABAB receptor. +<unk>  and analoguesat biological targets Compound GABAB<unk>  177 (R)-Phenibut 23 92 (S)-Phenibut 39 >1,000 Baclofen 156 6 Gabapentin 0.05 >1,000 Values are Ki (μM) in rat brain.<unk>  also binds to and blocks α2δ subunit-containing VDCCs, similarly to gabapentin and pregabalin, and hence is a gabapentinoid. Both (R)-phenibut and (S)-phenibut display this action with similar affinity (Ki = 23 and 39 μM, respectively). Pharmacokinetics Little information thus far has been published on the clinical pharmacokinetics of<unk> . The drug is reported to be well-absorbed. It distributes widely throughout the body and across the blood–brain barrier. Approximately 0.1% of an administered dose of<unk>  reportedly penetrates into the brain, with this said to occur to a much greater extent in young people and the elderly. Following a single 250 mg dose in healthy volunteers, its elimination half-life was approximately 5.3 hours and the drug was largely (63%) excreted in the urine unchanged. Some limited information has been described on the pharmacokinetics of<unk>  in recreational users taking much higher doses (e.g., 1–3 grams) than typical clinical doses. In these individuals, the onset of action of<unk>  has been reported to be 2 to 4 hours orally and 20 to 30 minutes rectally, the peak effects are described as occurring 4 to 6 hours following oral ingestion, and the total duration for the oral route has been reported to be 15 to 24 hours (or about 3 to 5 terminal half-lives).
Phenibut
Cromoglicic acid
Squalene
Bolesatine
Beta-Zearalenol
Desmethylchlorotrianisene
Chlormerodrin
Truenat