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Chloro-APB hydrobromide

Cat. No. M7693
Chloro-APB hydrobromide Structure
Synonym:

(±)-SKF 82958; Chloro-AP

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Biological Activity

Chloro-APB hydrobromide is a selective dopamine D1 receptor agonist and induces dopamine D1 receptor-dependent adenylate cyclase activity in rat striatal membranes (EC50=491 nM).

Chemical Information
Molecular Weight 410.73
Formula C19H20ClNO2 · HBr
CAS Number 80751-65-1
Solubility (25°C) Water 3.7 mg/mL
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] Yi Zhang, et al. Dopamine D1 Receptor in the Nucleus Accumbens Modulates the Emergence from Propofol Anesthesia in Rat

[2] G N Andrianov, et al. Dopaminergic modulation of afferent synaptic transmission in the semicircular canals of frogs

[3] Domokos Ger, et al. Oxidant-induced cardiomyocyte injury: identification of the cytoprotective effect of a dopamine 1 receptor agonist using a cell-based high-throughput assay

[4] E S Nisenbaum, et al. Selective blockade of a slowly inactivating potassium current in striatal neurons by (+/-) 6-chloro-APB hydrobromide (SKF82958)

[5] E F Domino, et al. Talipexole or pramipexole combinations with chloro-APB (SKF 82958) in MPTP-induced hemiparkinsonian monkeys

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Keywords: Chloro-APB hydrobromide, (±)-SKF 82958; Chloro-AP supplier, Dopamine Receptor, inhibitors, activators

 
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