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Anyone know anything about these? To what extent are they analgesic, and by what mechanism?
Synthesis and analgesic activity of N-(N-acetyl-L-amino-acyl)-5-methoxytryptamines.
Dongmei H, Chao W, Ming Z, Shiqi P., Prep Biochem Biotechnol. 30(1), 39-47 (2000)
Medline (PMID=10701451) (http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=10701451&dopt=Abstract)
Abstract
5-Methoxytryptamine was acylated with N-acetyl-L-amino acids to give rise the corresponding N-(N-acetyl-L-amino acyl)-5-methoxytryptamines. The analgesic activity was evaluated by the tail flick test. Among the 6 compounds, the analgesic potency of N-(N-acetyl-tryptophanyl)-5-methoxytryptamine (5e) and N-(N-acetyl-glycyl)-5-methoxytryptamine (5a) are much more potent than that of melatonin.
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Of possible interest as well:
Medline (PMID=10919562) (http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=10919562&dopt=Abstract)
Synthesis and analgesic activity of N,N'-dicarbonyltryptamines.
Dongmei H, Chao W, Ming Z, Shiqi P.
5-Methoxytryptamine and L-tryptophan methyl ester were acylated with malonic acid, dimethyl malonate, or succinic anhydride to produce the corresponding N,N'-dicarbonyltryptamine derivatives. The analgesic activity was evaluated by the tail flick test. All of the compounds exhibited desirable analgesic potency. This result is consistent with that of N-(N-acetyl-L-tryptophanyl)-5-methoxytryptamine and confirmed that introducing substituted tryptamine into the amide chain of melatonin does enhance analgesic potency.