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GR 55562 dihydrochloride

Cat. No. M41747
GR 55562 dihydrochloride Structure
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Biological Activity

GR 55562 (dihydrochloride) is a selective 5-HT1B receptor antagonist.

Chemical Information
Molecular Weight 448.39
Formula C23H27Cl2N3O2
CAS Number 159533-25-2
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] Feng-Yu Liu et al. J Pharmacol Exp Ther. Roles of 5-hydroxytryptamine (5-HT) receptor subtypes in the inhibitory effects of 5-HT on C-fiber responses of spinal wide dynamic range neurons in rats

[2] Chang Young Jeong et al. Eur J Pharmacol. Roles of serotonin receptor subtypes for the antinociception of 5-HT in the spinal cord of rats

[3] L E O'Dell et al. J Pharmacol Exp Ther. Serotonin1B receptors in the ventral tegmental area modulate cocaine-induced increases in nucleus accumbens dopamine levels

[4] Małgorzata Filip et al. Eur J Pharmacol. Effects of 5-HT1B receptor ligands microinjected into the ventral tegmental area on cocaine discrimination in rats

[5] Boris Mlinar et al. Br J Pharmacol. Pharmacological characterization of 5-HT(1B) receptor-mediated inhibition of local excitatory synaptic transmission in the CA1 region of rat hippocampus

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