(+)-Razpipadon ((+)-PW0464) is a selective D1 dopamine receptor agonist belonging to non-catechol compounds. (+)-Razpipadon activates the G protein pathway, while restricting β-arrestin coupling through the proximity effect of fluoromethyl-TM5, thereby achieving specific regulation of downstream pathways. (+)-Razpipadon can be used in studies related to Parkinson's disease [1] [2].
In Vitro, (+)-Razpipadon is a G protein-biased agonist of human D1R that activates the G protein signaling pathway. Its potency is slightly lower than that of Tavapadon, but it cannot effectively activate the β-arrestin pathway[1].
References:
[1]. Teng X, et al. Ligand recognition and biased agonism of the D1 dopamine receptor. Nat Commun. 2022;13(1):3186. Published 2022 Jun 8.
[2]. Sibley D R, et al. Novel Cryo-EM structures of the D1 dopamine receptor unlock its therapeutic potential[J]. Signal Transduction and Targeted Therapy, 2021, 6(1): 205.
[3]. Kumar S, et al. Discovery and structure - activity relationships of 2,4,5-trimethoxyphenyl pyrimidine derivatives as selective D5 receptor partial agonists. Bioorg Chem. 2024;153:107809.
In Vitro, (+)-Razpipadon is a G protein-biased agonist of human D1R that activates the G protein signaling pathway. Its potency is slightly lower than that of Tavapadon, but it cannot effectively activate the β-arrestin pathway[1].
References:
[1]. Teng X, et al. Ligand recognition and biased agonism of the D1 dopamine receptor. Nat Commun. 2022;13(1):3186. Published 2022 Jun 8.
[2]. Sibley D R, et al. Novel Cryo-EM structures of the D1 dopamine receptor unlock its therapeutic potential[J]. Signal Transduction and Targeted Therapy, 2021, 6(1): 205.
[3]. Kumar S, et al. Discovery and structure - activity relationships of 2,4,5-trimethoxyphenyl pyrimidine derivatives as selective D5 receptor partial agonists. Bioorg Chem. 2024;153:107809.