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SDZ SER 082 fumarate

Cat. No. M7287
SDZ SER 082 fumarate Structure
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Biological Activity

SDZ SER 082 富马酸盐是一种选择性 5-HT2B/2C 受体拮抗剂,对 5-HT1A 受体具有低亲和力。抑制[3H]-美舒肾上腺素与5-HT2C受体的结合,pKD为7.8。抑制大鼠眼底中5-HT2B介导的反应(pKB = 7.34)。

Chemical Information
Molecular Weight 344.41
Formula C15H20N2.C4H4O4
CAS Number 1417343-80-6
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] Beaujouan, et al. Br J Pharmacol. Higher potency of RP 67580, in the mouse and the rat compared with other nonpeptide and peptide tachykinin NK1 antagonists.

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