389080-71-1
Chemical Structure
MLS6585
- CAS No.: 389080-71-1
- Formula:C19H23N3O2S
- Molecular Weight:357.47
IUPAC Name: N-(6-(tert-butyl)-3-carbamoyl-4,5,6,7-tetrahydrobenzo[b]thiophen-2-yl)isonicotinamide
InChIKey: IMEICQDRTCGLFX-UHFFFAOYSA-N
SMILES: O=C(N)C1=C(SC2=C1CCC(C2)C(C)(C)C)NC(=O)C=3C=CN=CC3
Biological Activity: MLS6585 is a selective D1 dopamine receptor (D1R) positive allosteric modulator that enhances Dopamine (HY-B0451)-stimulated G protein/β-arrestin signaling and affinity without intrinsic D1R agonist activity. MLS6585 is inactive at D2R, D3R, D4R, and β2-adrenergic receptors. MLS6585 partially restores signaling of loss-of-function DRD1 variants and enhances responses to multiple agonists[1][2][3][4].
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MLS6585 | MLS6585 is a selective D1 dopamine receptor (D1R) positive allosteric modulator that enhances Dopamine (HY-B0451)-stimulated G protein/β-arrestin signaling and affinity without intrinsic D1R agonist activity. MLS6585 is inactive at D2R, D3R, D4R, and β2-adrenergic receptors. MLS6585 partially restores signaling of loss-of-function DRD1 variants and enhances responses to multiple agonists. | |||||||||||||||||||||
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References
- [1]. Luderman KD, et al. Identification of Positive Allosteric Modulators of the D Dopamine Receptor That Act at Diverse Binding Sites. Molecular pharmacology. 2018 Oct;94(4):1197-1209. [Content Brief]
- [2]. Wu C, et al. Pharmacological Characterization of Dopamine Receptor DRD1 Variants and Exploration of Their Allosteric Activation. Biochemistry. 2025 May 20;64(10):2200-2211.
- [3]. Labouesse MA, et al. A chemogenetic approach for dopamine imaging with tunable sensitivity. Nature communications. 2024 Jul 02;15(1):5551.
- [4]. Hanson J N, et al. Characterization of the Binding Pocket for a Novel Positive Allosteric Modulator of the D1 Dopamine Receptor[J]. The Journal of Pharmacology and Experimental Therapeutics, 2024, 389: 344.
