157561-22-3Relevant academic research and scientific papers
New Synthesis of 1-Substituted 3-(2-Aminoethyl)indoles
Guengoer, Timur,Malabre, Patrice,Teulon, J.M.
, p. 2247 - 2256 (2007/10/02)
A number of 1-substituted 3-(2-aminoethyl)indoles were prepared, in one step, by alkylation of the corresponding 3-(2-aminoethyl)indoles (tryptamines) in the presence of NaH.
N6-Substituted Adenosine Receptor Agonists. Synthesis and Pharmacological Activity as Potent Antinociceptive Agents
Guengoer, Timur,Malabre, Patrice,Teulon, Jean-Marie,Camborde, Francoise,Meignen, Joelle,et al.
, p. 4307 - 4316 (2007/10/02)
Novel N6-(indol-3-yl)alkyl derivatives of adenosine were synthesized.The adenosine receptor affinity and the antinociceptive activity of these compounds were assessed in binding studies and the phenylbenzoquinone-induced writhing test.Most of these analogues exhibited a potent analgesic activity without side effects.Among them, compound 3c (UP 202-32) bound to A1 (Ki = 110 nM) and A2 (Ki = 350 nM) adenosine receptors in a specific manner since it did not interact with many other receptors, especially opioid binding sites.The antinociceptive activity in the phenylbenzoquinone assay (ED50 = 3.3 mg/kg po) was antagonized by 8-cyclopentyltheophylline, suggesting that an adenosinergic mechanism underlies the analgesic activity observed with this compound.The data obtained with these new N6-substituted adenosine receptor agonists emphasize the interest of such compounds in the treatment of pain.
