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TZB-30878

Chemical Structure : TZB-30878

CAS No.: 864385-95-5

TZB-30878 (TZB30878)

Catalog No.: PC-47113Not For Human Use, Lab Use Only.

TZB-30878 is a potent, selective, orally bioavailable 5-HT1A agonist and 5-HT3 antagonist, selectively binds to human 5-HT1A and 5-HT) receptors with Kd values of 0.68 and 8.90 nM, respectively.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

TZB-30878 is a potent, selective, orally bioavailable 5-HT1A agonist and 5-HT3 antagonist, selectively binds to human 5-HT1A and 5-HT) receptors with Kd values of 0.68 and 8.90 nM, respectively.
Systemic administration of TZB-30878 inhibited 5-HT-induced bradycardia in a dose-dependent manner in rats, TZB-30878 produced signs of 5-HT syndrome in rats in behavioral assays.
TZB-30878 (1-10 mg/kg p.o.) normalized stress-induced defecation in a dose-dependent manner in IBS-like model in rats.

Physicochemical Properties

M.Wt 432.572
Formula C25H32N6O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
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Solubility

10 mM in DMSO

Chemical Name/SMILES

3-Amino-5,6,7,8-tetrahydro-2-[4-[4-(quinolin-2-yl)piperazin-1-yl]butyl]quinazolin-4(3H)-one

References

1. Tamaoki S, et al. J Pharmacol Exp Ther. 2007 Sep;322(3):1315-23.

2. Asagarasu A, et al. J Med Chem. 2010 Nov 11;53(21):7549-63.

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