65006-86-2

Upstream product

• 61711-82-8 (3,5-dimethoxyphenoxy)ethanenitrile 
• 930523-82-3 C₁₀H₁₃NO₄ 
• 85262-44-8 1-bromo-2-(3,5-dimethoxyphenoxy)ethane 
• 500-99-2 3,5-dimethoxyphenol 

Downstream Products

• 65022-74-4 8-(2-propynyloxy)-5{3-[2-(3,5-dimethoxyphenoxy)ethylamino]-2-hydroxypropoxy}-3,4-dihydrocarbostyril hydrochloride 
• 89718-74-1 N-<2-(3,5-dimethoxyphenoxy)ethyl>benzamide 
• 89718-84-3 6,8-Dimethoxy-5-phenyl-2,3-dihydro-benzo[f][1,4]oxazepine 
• 1220748-15-1 C₂₆H₂₉NO₅ 

Relevant academic research and scientific papers

Synthesis and pharmacological activity of a new series of 1-(1H-indol-4-yloxy)-3-(2-(2-methoxyphenoxy)ethylamino)-propan-2-ol analogs

β-Adrenergic receptor antagonists are important therapeutics for the treatment of cardiovascular disorders. In the group of β-blockers, much attention is being paid to the third-generation drugs that possess important ancillary properties besides inhibiting β-adrenoceptors. Vasodilating activity of these drugs is produced through different mechanisms, such as nitric oxide (NO) release, β2-agonistic action, α1-blockade, antioxidant action, and Ca2t entry blockade. Here, a study on evaluation of the cardiovascular activity of five new compounds is presented. Compound 3a is a methyl and four of the tested compounds (3b–e) are dimethoxy derivatives of 1-(1H-indol-4-yloxy)-3-(2-(2-methoxyphenoxy)-ethylamino)propan-2-ol. The obtained results confirmed that the methyl and dimethoxy derivatives of 1-(1H-indol-4-yloxy)-3-(2-(2-methoxyphenoxy)ethylamino)propan-2-ol and their enantiomers possess α1- and β1-adrenolytic activities and that the antiarrhythmic and hypotensive effects of the tested compounds are related to their adrenolytic properties.

Discovery of a new series of 5-HT1A receptor agonists

Starting from compounds previously identified as α1-adrenoceptor antagonists that were also found to bind to the 5-HT1A receptor, in an attempt to separate the two activities, a new series of 5-HT1A receptor agonists was identified and shown to have high potency and/or high selectivity. Of these, compound 13, which combines high selectivity (5-HT1A/α1 = 151) and good agonist potency (pD2 = 7.82; Emax = 76), was found to be the most interesting.