GABAB receptor antagonist 1

Names

[ CAS No. ]:
797-17-1

[ Name ]:
GABAB receptor antagonist 1

Biological Activity

[Description]:

GABAB receptor antagonist 1 (compound 14) is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors. (E)-GABAB receptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC50 of 37.9 μM[1].

[Target]

GABAB[1]


[In Vitro]

(E)-GABAB receptor antagonist 1 (compound 14) decreases agonist GABA-induced maximal effect of IP3 production in HEK293 cells overexpressing GABAB receptors and Gqi9 proteins without changing the EC50[1].

[References]

[1]. Chen LH, et al. Discovery of a Negative Allosteric Modulator of GABAB Receptors. ACS Med Chem Lett. 2014 May 27;5(7):742-7.

Chemical & Physical Properties

[ Molecular Formula ]:
C18H24O4

[ Molecular Weight ]:
304.38

Related Compounds