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ABT-089 dihydrochloride

Cat. No. M8553
ABT-089 dihydrochloride Structure
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Biological Activity

ABT-089 (Pozanicline) is a subtype-selective neuronal nicotinic receptor partial agonist binding primarily to the α4β2 and also α6β2 subtypes. It has been investigated for alleviating symptoms of nicotine withdrawal including cognitive deficits and anxiety.

Chemical Information
Molecular Weight 265.18
Formula C11H16N2O · 2HCl
CAS Number 161416-61-1
Solubility (25°C) Water: 20 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] Chih-Liang Chin, et al. Pharmacokinetic modeling and [¹²³]5-IA-85380 single photon emission computed tomography imaging in baboons: optimization of dosing regimen for ABT-089

[2] Vinay Parikh, et al. Glutamatergic contributions to nicotinic acetylcholine receptor agonist-evoked cholinergic transients in the prefrontal cortex

[3] Lynne E Rueter, et al. ABT-089: pharmacological properties of a neuronal nicotinic acetylcholine receptor agonist for the potential treatment of cognitive disorders

[4] M A Prendergast, et al. Central nicotinic receptor agonists ABT-418, ABT-089, and (-)-nicotine reduce distractibility in adult monkeys

[5] M W Decker, et al. ABT-089 [2-methyl-3-(2-(S)-pyrrolidinylmethoxy)pyridine dihydrochloride]: II. A novel cholinergic channel modulator with effects on cognitive performance in rats and monkeys

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