Rhodium (Chief Bee)
07-12-04 22:46
No 518956
      Analgesic N-acyl-Melatonins?     

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.

The Hive - Clandestine Chemists Without Borders
 
 
 
 
    Saddam_Hussein
(Newbee)
07-14-04 23:43
No 519437
      Also     

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.

President of the Iraqi Chemical Weapons of Mass Destruction Development Society