101832-75-1

Upstream product

• 104509-07-1 3-(2-amino-ethyl)-5-methylsulfanyl-indole-2-carboxylic acid 
• 16686-11-6 2-(3-chloropropyl)-1,3-dioxolane 
• 58626-97-4 [p-(methylthio)phenyl]hydrazine hydrochloride 
• 104996-59-0 6-methylsulfanyl-2,3,4,9-tetrahydro-β-carbolin-1-one 

Downstream Products

• 174727-74-3 2-[1-(2,5-Dimethyl-benzyl)-5-methylsulfanyl-1H-indol-3-yl]-ethylamine 
• 1054665-06-3 (3aS,4S,6R,6aR)-6-(6-{2-[1-(2,5-Dimethyl-benzyl)-5-methylsulfanyl-1H-indol-3-yl]-ethylamino}-purin-9-yl)-2,2-dimethyl-tetrahydro-furo[3,4-d][1,3]dioxole-4-carboxylic acid cyclopropylamide 

Relevant academic research and scientific papers

BETA-CARBOLINE DERIVATIVES AND THERI USE AS GHSR MODULATORS

The present invention relates to compounds of Formula (I): wherein R1 to R3 are as described herein, processes for preparing the compounds, pharmaceutical compositions comprising the compounds, and use of the compounds and compositions in the prophylaxis

N6-Substituted Adenosine Receptor Agonists. Synthesis and Pharmacological Activity as Potent Antinociceptive Agents

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.