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LY3154207 

Cat. No. M28747
LY3154207  Structure
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Biological Activity

LY3154207 is a potent, subtype selective, and orally available human dopamine D1 receptor positive allosteric modulator (PAM) with minimal allosteric agonist activity (EC50=3 nM).

Chemical Information
Molecular Weight 450.4
Formula C24H29Cl2NO3
CAS Number 1638667-79-4
Form Solid
Solubility (25°C) DMSO 110 mg/mL (ultrasonic)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Andrew P McCarthy, et al. J Pharmacol Exp Ther. The Dopamine D1 Receptor Positive Allosteric Modulator Mevidalen (LY3154207) Enhances Wakefulness in the Humanized D1 Mouse and in Sleep-Deprived Healthy Male Volunteers

[2] Darren Wilbraham, et al. Clin Pharmacol Drug Dev. Safety, Tolerability, and Pharmacokinetics of Mevidalen (LY3154207), a Centrally Acting Dopamine D1 Receptor-Positive Allosteric Modulator, in Patients With Parkinson Disease

[3] Chichun Sun, et al. Behav Sci (Basel). Treatment of Parkinson's Disease with Cognitive Impairment: Current Approaches and Future Directions

[4] Darren Wilbraham, et al. Clin Pharmacol Drug Dev. Safety, Tolerability, and Pharmacokinetics of Mevidalen (LY3154207), a Centrally Acting Dopamine D1 Receptor-Positive Allosteric Modulator (D1PAM), in Healthy Subjects

[5] Junliang Hao, et al. J Med Chem. Synthesis and Pharmacological Characterization of 2-(2,6-Dichlorophenyl)-1-((1 S,3 R)-5-(3-hydroxy-3-methylbutyl)-3-(hydroxymethyl)-1-methyl-3,4-dihydroisoquinolin-2(1 H)-yl)ethan-1-one (LY3154207), a Potent, Subtype Selective, and Orally Available Positi䲧瘀Ỵ瘁㧀痿羹皘的郘ࡎţࡎð�皚嶁皖

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