target/GABA_Receptor/7

GABA receptor Antagonist 1 (compound 7w) effectively inhibits the Px RDL1 GABAR at an IC50 of 7.08 nmol/L and demonstrates insecticidal efficacy against P. xylostella, S. frugiperda, S. exigua, and S. litura with respective LC50 values of 0.09, 0.84, 0.87, and 0.68 mg/L. Moreover, this compound exhibits moderate toxicity to honeybees (48 h, ID50 = 2.22 μg/adult) and low toxicity to zebrafish (LC50: 42.4 mg/L) [1].

RXFP1 receptor agonist-7 (Example 2) serves as an RXFP1 receptor agonist, effectively inhibiting cAMP production in HEK293 cells that stably express the human RXFP1, achieving an EC50 of 4.2 nM [1].

APJ receptor agonist 7 (compound 37) is an orally active APJ (apelin receptor) agonist (Ki: 0.059 μM). arrestin (EC50: 0.063 μM).

Compound 24, also known as Mu opioid receptor antagonist 7, is a potent, centrally-acting µ-opioid receptor (µOR) antagonist with an inhibitory concentration (IC50) of 29 ± 3.0 nM. It is valuable for pain and opioid use disorder research [1].

Estrogen Receptor Modulator 7 is a potent modulator of estrogen receptors, utilized in cancer research [1].

Compound (S)-10a, a GluN2B subunit-selective NMDA receptor antagonist, exhibits a K i of 93 nM and an IC 50 of 72 nM. It is potentially useful for research into neurodegenerative diseases [1].

GLP-1 receptor agonist 7 is a potent glucagon-like peptide-1 (GLP-1) agonist and has shown research potential for GLP-1 related diseases, disorders and conditions, including diabetes.

Estrogen Receptor Antagonist 7 (Compound 13) is a potent antagonist of estrogen receptors (ER), demonstrating antiproliferative effects against breast and ovarian cancer cells, along with anticancer and anti-uterotrophic activities [1].

GABAA receptor agent 7 (compoud 5c) has anticonvulsant activity both in vitro and in vivo with low neurotoxicity which can be used in epilepsy research. GABAA receptor agent 7 is a potent positive modulator of GABAA receptor [1].