rat gabaa

Lesogaberan is an effective and selective GABAB receptor agonist (EC50: 8.6 nM for human recombinant GABAB receptors). For rat brain GABAB and GABAA receptors, the binding affinity (Kis) is 5.1 nM and 1.4 μM, respectively.

Pivagabine (CXB-722) 是疏水性 4-氨基丁酸的衍生物，具有神经调节活性。它可穿透大鼠的血脑屏障，拮抗足部休克对大鼠脑中 GABAA 受体功能和促肾上腺皮质激素释放因子 (CRF) 浓度的影响。

Isoguvacine hydrochloride (1,2,3,6-tetrahydro-4-pyridinecarboxylic acid hydrochloride) 是 GABA 受体激动剂。它与大鼠突触皮质膜结合并激活 α1β2γ2S、α2β2γ2S、α3β2γ2S、α5β2γ2S 和 ρ1 亚基 GABAA 受体。

MK0343 is an orally bioavailable GABAA receptor subtype-selective partial agonist and is a non-sedating anxiolytic.

(+)-Bicuculline methiodide 是一种可穿过大鼠血脑屏障（BBB）的 γ-氨基丁酸 A 型 （GABAA) 受体阻断剂，可阻断阻断癫痫原，可用于研究癫痫等神经系统疾病。(+)-Bicuculline methiodide 可降低脓毒症大鼠的肝损伤。

KRM-II-81 is a γ-Aminobutyric Acid Type A (GABAA) Receptor Ligand. KRM-II-81 exhibits improved anxiolytic-like effects in a mouse marble burying assay and a rat Vogel conflict test.

Lesogaberan (AZD-3355) napadisylate is a potent and selective agonist of GABA B receptors, with an EC 50 of 8.6 nM for human recombinant GABA B receptors. It demonstrates an affinity (Ki) of 5.1 nM for rat GABA B receptors and 1.4 μM for GABA A receptors, as determined by its displacement of [3H]GABA binding in brain membranes. Notably, Lesogaberan napadisylate exerts a peripheral mode of action, inhibiting transient lower esophageal sphincter relaxation.

GABAA receptor agent 2 TFA 是一种有效的、高亲和力的 GABAA 受体拮抗剂，IC50为 24 nM (表达人 α1β2γ2GABAA 的 tsA201 细胞)，Ki 为 28 nM (大鼠GABAA 受体)。GABAA receptor agent 2 TFA 对四种人类 GABA 转运蛋白 (hGAT-1，hBGT-1，hGAT-2 和 hGAT-3) 没有作用。

Lesogaberan (AZD-3355) hydrochloride 是一种有效的选择性 GABAB 受体激动剂，对人重组 GABAB 受体的 EC50为 8.6 nM。通过脑膜中 [3H]GABA 结合位移测量，Lesogaberan hydrochloride 对大鼠 GABAB 和 GABAA 受体的亲和力 (Kis)：分别为 5.1 nM 和 1.4 μM。Lesogaberan hydrochloride 通过外周作用模式抑制短暂的食管下括约肌松弛。

(R)-4-Amino-3-hydroxybutyric acid, also known as (R)-GABOB, acts as a modulator of GABA receptors, specifically binding to both GABAA and GABAB receptors and blocking GABA reuptake in rat brain synaptosomes. Additionally, it serves as a GABAC receptor agonist, triggering currents in patch-clamp assays with Xenopus oocytes that express the human receptor. In vivo studies reveal its capability to suppress electrical discharges in the amygdala in cats undergoing N-amidinobenzamide-triggered seizures, indicating its potential therapeutic application in managing seizure disorders.