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D1R antagonist 1

Cat. No. M41805
D1R antagonist 1 Structure
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Biological Activity

D1R antagonist 1 is a D1R antagonist, involved in G-protein- and β-arrestin-based signaling.

Chemical Information
Molecular Weight 448.35
Formula C22H26BrNO4
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] Hari K Namballa et al. Bioorg Chem. Fluoroalkoxylated C-3 and C-9 (S)-12-bromostepholidine analogues with D1R antagonist activity

[2] Rajan Giri et al. Molecules. Structure-Activity Relationship Studies on 6-Chloro-1-phenylbenzazepines Leads to the Identification of a New Dopamine D1 Receptor Antagonist

[3] Hua-Chun Miao et al. Biochem Biophys Res Commun. Expression changes of c-Fos and D1R/p-ERK1/2 signal pathways in nucleus accumbens of rats after ketamine abuse

[4] Rajan Giri et al. Bioorg Chem. Further studies on C2'-substituted 1-phenylbenzazepines as dopamine D1 receptor ligands

[5] D C Borcherding et al. Oncogene. Expression and therapeutic targeting of dopamine receptor-1 (D1R) in breast cancer

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