GTS-21 (DMXBA or DMBX-anabaseine) is a drug has been ability to potentially enhance memory and cognitive function. It has been studied for its potential therapeutic uses, particularly in the treatment of neurodegenerative diseases and psychiatric disorders.

2007年11月18日 · GTS-21 (also known as DMBX-A), is a novel, small-molecule, orally active and selective alpha-7 nicotinic acetylcholine (nACh) receptor agonist that has demonstrated memory and cognition enhancement activity in human clinical trials.

GTS-21 dihydrochloride is a selective alpha7 nicotinic acetylcholine receptor (α7-nAChR) agonist with anti‑inflammatory and cognition‑enhancing activities. GTS-21 dihydrochloride is also a α4β2 (K i. =20 nM for humanα4β2) and 5-HT3A receptor (IC50 =3.1 μM) antagonist.

GTS-21 dihydrochloride is a selective alpha7 nicotinic acetylcholine receptor (α7-nAChR) agonist with anti‑inflammatory and cognition‑enhancing activities. GTS-21 dihydrochloride is also a α4β2 (K i =20 nM for humanα4β2) and 5-HT3A receptor (IC 50 =3.1 μM) antagonist.

We labeled GTS-21 in two different positions with carbon-11 ([2-methoxy-(11)C]GTS-21 and [4-(11)C]GTS-21) along with two corresponding demethylated metabolites ([2-methoxy-(11)C]4-OH-GTS-21 and [4-methoxy-(11)C]2-OH-GTS-21) for pharmacokinetic studies in baboons and mice with positron emission tomography (PET).

GTS-21 dihydrochloride (DMBX-A)是一种α7nACh受体的 部分激动剂，选择性地与 α7 亚基结合，在 α2、α3 和 α4 没有明显的活性（EC50 = 10 μM 体外（纹状体 切片））。 GTS-21 dihydrochloride显示出引发促智、神经保护和抗炎的作用。 结构式：COC1=CC=C (/C=C2C (C3=CC=CN=C3)=NCCC/2)C (OC)=C1. [H]Cl. 储藏条件：干燥、避光，短期（数天至数周）或 -20°C 长期储存（正确储存 2-3 年）。

GTS-21 is a selective agonist at α-7 nicotinic receptors with anti-inflammatory and cognition enhancing activities. GTS-21 has also been investigated for the treatment of schizophrenia.

GTS-21（也称为 DMBX-anabaseine）是一种选择性 α7 烟碱乙酰胆碱受体 (α7nAChR) 激动剂，之前已被发现可抑制与类风湿性关节炎 (RA) 相关的炎症。 RA是一种自身免疫性疾病，其中异常的免疫系统在滑膜炎症和骨损伤的发生和发展中起关键作用。

GTS-21 (also known as DMBX-anabaseine), a selective α7 nicotinic acetylcholine receptor (α7nAChR) agonist, has previously been found to inhibit the inflammation associated with rheumatoid arthritis (RA). RA is an autoimmune disease, where an abnormal immune system plays a critical role in the occurr …

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