Heterocyclic aminopyrrolidine derivatives as melatoninergic agents.

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Sun LQ, Chen J, Mattson RJ, Epperson JR, Deskus JA, Li WS, Takaki K, Hodges DB, Iben L, Mahle CD, Ortiz A, Molstad D, Ryan E, Yeleswaram K, Xu C, Luo G

Heterocyclic aminopyrrolidine derivatives as melatoninergic agents.

Bioorg Med Chem Lett. 2003 Dec 15;13(24):4381-4.

PubMed ID

14643330 [ View in PubMed

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Abstract

A series of chiral heterocyclic aminopyrrolidine derivatives was synthesized as novel melatoninergic ligands. Binding affinity assays were performed on cloned human MT(1) and MT(2) receptors, stably expressed in NIH3T3 cells. Compound 16 was identified as an orally bioavailable agonist at MT(1) and MT(2) melatonin receptors with low vasoconstrictive activity.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Melatonin	Melatonin receptor type 1A	Ki (nM)	0.4	N/A	N/A	Details
Melatonin	Melatonin receptor type 1B	Ki (nM)	0.3	N/A	N/A	Details