(E)-GABAB receptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC50 of 37.9 μM.GABAB receptor antagonist 1 is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors.
Xestospongins and araguspongins, marine natural products originally isolated from sponges in the Pacific basin, exhibit vasodilatory effects. Inositol phosphates (IP) serve as crucial signal transduction messengers, activating IP3 receptors to facilitate Ca2+ release from intracellular stores. Araguspongin B specifically hinders the calcium-releasing function of inositol 1,4,5-trisphosphate at the receptor level within cerebral microsomes, demonstrating an inhibition concentration (IC50) of 0.6 µM. This potency places it nearly on par with xestospongin C in obstructing the IP3 receptor's activity.