Mutual Cooperativity of Three Allosteric Sites on the Dopamine D1 Receptor

• Published in: Molecular pharmacology Vol. 103; no. 3; pp. 176 - 187
• Main Authors: Wang, Xushan, Hembre, Erik J., Goldsmith, Paul J., Beck, James P., Svensson, Kjell A., Willard, Francis S., Bruns, Robert F.
• Format: Journal Article
• Language: English
• Published: United States Elsevier Inc 01.03.2023
• Subjects: Allosteric Regulation - physiology; Allosteric Site - physiology; Dopamine - metabolism; Humans; Receptors, Dopamine D1 - metabolism; Receptors, G-Protein-Coupled; GPCR; ICL2; NAM; CRC; PAM; ECL

An amine-containing molecule called Compound A has been reported by a group from Bristol-Myers Squibb to act as a positive allosteric modulator (PAM) at the dopamine D1 receptor. We synthesized the more active enantiomer of Compound A (BMS-A1) and compared it with the D1 PAMs DETQ and MLS6585, which...