AMPA receptor modulator-4

CAS: 2917551-59-6 F: C11H12ClFN2O2S W: 290.74

AMPA receptor modulator-4, a 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide (BTD), is an orally active positive allos

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Bioactivity	AMPA receptor modulator-4, a 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide (BTD), is an orally active positive allosteric modulators of the AMPA receptors (AMPAR PAMs). AMPA receptor modulator-4 can cross the blood-brain barrier. AMPA receptor modulator-4 increases the cognition performance and improves working memory performance in mice[1].
Invitro	AMPA receptor modulator-4 (化合物 15e) 对稳定表达 GluA2(Q) 亚基的 HEK293 细胞上 1 mM 谷氨酸诱导的钙内流的 pEC50 为 5.66[1]。 AMPA receptor modulator-4 的 EC2x 为 2.1 μM (FlipR)-1.5 μM (FDSS)[1]。
In Vivo	AMPA receptor modulator-4 (10 和 30 mg/kg; 腹腔给药; 一次) 以 10 mg/kg 的剂量增加大鼠 LTP 的持续时间[1]。 AMPA receptor modulator-4 (1 和 3 mg/kg; 口服灌胃) 在三个疗程前 1 小时给药，可以显着提高 CD1 小鼠的认知能力[1]。 AMPA receptor modulator-4 (0.03、0.1 和 0.3 mg/kg; 腹腔注射) 改善 C57BI/6 小鼠的自发交替性能和工作记忆性能[1]。 AMPA receptor modulator-4 (30, 100 mg/kg; 口服灌胃; 一次) 在 NMRI 小鼠中具有非促惊厥作用[1]。 Animal Model:
Name	AMPA receptor modulator-4
CAS	2917551-59-6
Formula	C11H12ClFN2O2S
Molar Mass	290.74
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Eric Goffin, et al. New insights in the development of positive allosteric modulators of α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors belonging to 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides: Introduction of (mono/difluoro)methyl groups at the 2-position of the thiadiazine ring. Eur J Med Chem. 2023 Mar 15;250:115221.

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