124998-75-0

Upstream product

• 57311-67-8 4-(1H-indol-3-yl)-1-piperidineethanamine 
• 124956-14-5 (2E,4E)-5-[3-Chloro-4-(2-methoxy-ethoxymethoxy)-phenyl]-penta-2,4-dienoic acid 
• 124956-08-7 Ethyl 5-[3-chloro-4-{(2-methoxyethoxy)methoxy}phenyl]-(2E, 4E)-2, 4-pentadienoate 
• 57311-64-5 N-(2-(4-(1H-indol-3-yl)piperidin-1-yl)ethyl)phthalimide 
• 17403-09-7 3-(4-piperidinyl)-1H-indole 
• 2420-16-8 4-hydroxy-3-chlorobenzaldehyde 
• 124956-02-1 3-Chloro-4-[(2-methoxyethoxy)methoxy]benzaldehyde 

Relevant academic research and scientific papers

(2E,4E)-N-(4-(1H-indol-3-yl)piperidin-1-yl)alkyl-5-(substituted phenyl)-2,4-pentadienamides as antiallergic agents with antihistaminic and anti slow-reacting substance (SRS) activities

As an extension of our study aiming to discover a novel compound with dual activities against histamine and slow-reacting substance (SRS), we synthesized two types of indolylpiperidine derivatives, 3 and 4-20. Testing for in vivo antianaphylactic activity and for in vitro anti-SRS activity revealed that (2E,4E)-5-(3,5-dimethoxy-4-hydroxyphenyl)-N-(2-(4-(1H-indol-3-yl)piper idin-1-yl)ethyl)-2,4-pentadienamide (11) exhibited potent dual activities with ED50 = 0.89 mg/kg and IC50 = 1.43 μM, respectively. However, the plasma concentration of unchanged 11 was very low when administered orally in guinea pigs. This result can be explained by fast formation of a glucuronic acid conjugate.