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2-Hydroxysaclofen 

Cat. No. M27881
2-Hydroxysaclofen  Structure
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Biological Activity

2-Hydroxysaclofen is a potent γ-amino-butyric-acid-B (GABAB) receptor antagonist. 2-Hydroxysaclofen can abolish nicotine-induced hypolocomotor effects and increases the antinociceptive effects. 2-Hydroxysaclofen can stimulate luteinizing hormone (LH) secretion in female rats.

Chemical Information
Molecular Weight 265.71
Formula C9H12ClNO4S
CAS Number 117354-64-0
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Andrés P Varani, et al. Eur J Pharmacol. Baclofen and 2-hydroxysaclofen modify acute hypolocomotive and antinociceptive effects of nicotine

[2] Florencio Miranda, et al. Pharmacol Biochem Behav. The GABA-B antagonist 2-hydroxysaclofen reverses the effects of baclofen on the discriminative stimulus effects of D-amphetamine in the conditioned taste aversion procedure

[3] Ken Kasamatsu, et al. Am J Physiol Regul Integr Comp Physiol. Depressor and bradycardic responses to microinjections of endomorphin-2 into the NTS are mediated via ionotropic glutamate receptors

[4] D I Kerr, et al. Eur J Pharmacol. The (S)-enantiomer of 2-hydroxysaclofen is the active GABAB receptor antagonist in central and peripheral preparations

[5] T Akema, et al. Brain Res. 2-Hydroxysaclofen, a potent GABAB receptor antagonist, stimulates luteinizing hormone secretion in female rats

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