Melatonin
Melatonin, a sleep compound. MT1/MT2 agonist; entrains the circadian clock bmal1 per cry circadian rhythm. Oral half-life 0.7 h.
MT1/MT2 agonist; entrains the Circadian clock circadian rhythm.
Lower doses (0.3mg) often outperform high doses for sleep onset. PO has heavy first-pass; SL bypasses much of it. MT1 Ki ~80 pM = 0.0000186 mg/L, MT2 Ki ~270 pM = 0.0000626 mg/L (melatonin MW 232 g/mol). Therapeutic plasma at 0.5 mg PO peaks ~80-100 pg/mL = ~1e-4 mg/L, well above both receptor EC50s — both are saturated within minutes of dosing. PK: THE STORED VOLUME WAS THE SOLVER DEFAULT WEARING A CITATION. 35 L is exactly 0.5 L/kg at the seventy-kilogram reference — the value resolvePk substitutes when the field is ABSENT — and this record cited abstract states no volume at all. Removing it is NUMERICALLY A NO-OP, since the resolver now supplies the identical number; what changes is that the record stops asserting a measurement it does not have, and the defaulted-volume lint begins counting it as the open gap it is. This is the batch-11 finding running backwards: there a deletion silently became a default, here a default had silently become a datum.
Pharmacokinetics
- Oral — t½ 42 min · F 15%
- Sublingual — t½ 30 min · F 50% · ka 6 h⁻¹
Sources: PMID:11487664, PMID:37438493, PMID:26008214, PMID:9380773