Author Topic: Analgesic N-acyl-Melatonins?  (Read 1428 times)

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Rhodium

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Analgesic N-acyl-Melatonins?
« on: July 12, 2004, 10:46:00 PM »
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)



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.


Saddam_Hussein

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Also
« Reply #1 on: July 14, 2004, 11:43:00 PM »
Of possible interest as well:

Medline (PMID=10919562)



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.