Pineal gland-mediated melatonin secretion controls mammalian circadian rhythm. Melatonin is synthesized from serotonin, a product of tryptophan metabolism.
Synthesis involves an enzyme called arylalkylamine N-acetyltransferase, AKA 2.3.1.87 AKA AANAT AKA melatonin rhythm enzyme, which is inhibited by cannabinoids (THC, CBD, cannabinol) in a direct fashion, not involving the cannabinoid receptors.
Potheads with a sleep related disorder could benefit from melatonin supplementation; it has quite poor bioavailability (30-50%), though. It's metabolized (deaminated) by the monoamine-oxidase A enzyme in the stomach so IMO administration of less than 0,5 mg sublingually or intranasally earlier than an hour before bed-time would be the way to go.
Caution:
Among other effects (1, 2, 3) , melatonin has an antidopaminergic effect, acting a bit like haloperidol, so large dosages and chronic use could theoretically lead to antipsychotic effects, and nobody would want to be a zombie on purpose, right?
Cannabinoids could enhance dopaminergic signalling a bit through this route.
Some refs by name or a bit of relevant significance of them, in form:
- Cannabinoids attenuate norepinephrine-induced melatonin biosynthesis in the rat pineal gland by reducing arylalkylamine N-acetyltransferase activity without involvement of cannabinoid receptors
- Acetylcholine has been demonstrated to exert various effects in the mammalian pineal gland, including an inhibitory action on the norepinephrine-induced stimulation of melatonin production.
- Melatonin modulates cholinergic transmission by blocking nicotinic channels in the guinea-pig submucous plexus
- Results got from the study of effects of melatonin on behavioral dopaminergic supersensitivity support previous evidence of antidopaminergic effects of melatonin and demonstrate that repeated administration of this hormone modifies the plasticity of behaviors mediated by central dopaminergic systems.
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