Metabotropic glutamate receptors (mGluR)
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mGlu2 receptor modulator
CBiPES HCl是mGluR-2的选择性正变构调节剂,IC50值为98.2 nM。
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mGluR1 拮抗剂
DL-AP3是D-AP3和L-AP3的外消旋制剂,是磷酸丝氨酸磷酸酶的抑制剂和代谢型谷氨酸受体(mGluR)的拮抗剂,阻断了由mGluR介导的磷酸肌醇转换。
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mGlu5 拮抗剂
MTEP hydrochloride是一种有效的,选择性和非竞争性的mGlu5拮抗剂,IC50和Ki分别为5 nM和16 nM。
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mGluR1 modulator
CPPHA是mGluR5受体的选择性正变构调节剂。
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mGlu3 receptor agonist
LY2794193 is a highly potent and selective mGlu3 receptor agonist (hmGlu3 Ki=0.927 nM??EC50=0.47 nM; hmGlu2 Ki=412 nM??EC50=47.5 nM).
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mGluR5 positive allosteric modulator
BMT-145027 is an mGluR5 positive allosteric modulator without inherent agonist activity, exhibits an EC50 of 47 nM.
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mGlu4 receptor modulator
Lu AF21934 is a selective and brain-penetrant mGlu4 receptor positive allosteric modulator with an IC50 of 500 nM for human mGlu4.
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mGluR5 antagonists
Dipraglurant (ADX 48621) is a mGluR5 antagonists with IC50 of 0.021 μM.
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mGluR4 PAM
ADX88178 is a potent metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) with an EC50 of 4 nM for human mGluR4.
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mGlu2 receptor agonist
LY2812223 is a highly potent, functionally selective mGlu2 receptor agonist with mGlu2 binding affinity for mGlu2 and mGlu3 (Ki=144 nM and 156 nM, respectively).
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group III mGluR receptors agonist
O-Phospho-L-serine is the immediate precursor to L-serine in the serine synthesis pathway, and an agonist at the group III mGluR receptors (mGluR4, mGluR6, mGluR7, and mGluR8); O-Phospho-L-serine also acts as a weak antagonist for mGluR1 and a potent antagonist for mGluR2.
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mGlu4 receptor modulator
TCN238 is a positive allosteric mGlu4 receptor modulator with an EC50 of 1 μM.
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mGlu5 receptor antagonist
Mavoglurant is a structurally novel, non-competitive mGlu5 receptor antagonist, has an IC50 of 30 nM in a functional assay with human mGluR5.
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mGlu5 negative allosteric modulator
Basimglurant (RG7090) is a potent, selective and orally available mGlu5 negative allosteric modulator with a Kd of 1.1 nM.
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mGlu2 agonist/mGlu3 antagonist
LY541850 is a selective orthosteric mGlu2 agonist and mGlu3 antagonist with IC50 values of 0.161 μM and 0.038 μM, respectively.
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mGlu5 receptor antagonist
Mavoglurant (racemate) is the racemate of mavoglurant. Mavoglurant is a novel, non-competitive mGlu5 receptor antagonist.
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mGluRs M3 agonist
L-APB is a potent and specific agonist for the group III mGluRs, with EC50s of 0.13, 0.29, 1.0, 249 μM for mGlu4, mGlu8, mGlu6 and mGlu7 receptors, respectively.
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mGluR5 positive allosteric modulator
(R)-ADX-47273 is a potent mGluR5 positive allosteric modulator, with an EC50 of 168 nM for potentiation .
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mGlu5 receptor antagonist
Methoxy-PEPy is a potent and highly selective mGlu5 receptor antagonist with IC50 of 1 nM.
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partial mGluR4 agonist
(1R,2S)-VU0155041, Cis regioisomer of VU0155041, is a partial mGluR4 agonist with an EC50 of 2.35 μM.
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mGluR5 agonist
CHPG sodium salt is a selective mGluR5 agonist, and attenuates SO2-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells.
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mGlu5 antagonist
Auglurant (VU0424238) is a novel and selective mGlu5 antagonist with an IC50 value of 11 nM (rat) and an IC50 value of 14 nM (human). Auglurant (VU0424238) has an acceptable CNS penetration.
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group II (mGlu2/3) receptor agonist
Eglumegad (LY354740) is a highly potent and selective group II (mGlu2/3) receptor agonist with IC50s of 5 and 24 nM on transfected human mGlu2 and mGlu3 receptors, respectively.
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mGlu5 modulator
VU0652835 is a metabotropic glutamate receptor subtype 5 (mGlu5) negative allosteric modulator with an IC50 of 81 nM.
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CNS penetrant mGlu7/8 receptor 激动剂
VU6005649是一种CNS渗透性mGlu7/8受体激动剂,对mGlu7受体和mGlu8受体的EC50分别为0.65 μM和2.6 μM。
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mGlu4 receptors modulator
VU 0364770是mGlu4受体的正变构调节剂,在表达mGlu4的HEK 293细胞中EC50值为290 nM。
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GluR 抑制剂
(-)-Huperzine A是一种天然存在的倍半萜生物碱化合物,存在于石楠石杉中。
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- Takuya Ohba, .et al. Protective effects of Huperzia serrata and its components against oxidative damage and cognitive dysfunction, PharmaNutrition, 2020, 13:100203
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mGluR5 modulator
ADX-47273是一种有效的,特异性的mGlu5正变构调节剂(PAM)EC50为0.17 μM,对其他亚型没有作用活性。
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mGluR2 modulator
BINA是mGlu2的选择性正构构调节剂(在表达人mGlu2的CHO细胞中EC50 = 33.2 nM)。
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mGluR 激动剂
LY-404039是一种用于科学研究的药物,用作代谢型谷氨酸受体II亚型mGluR2和mGluR3的选择性激动剂。它在动物研究中具有抗焦虑和抗精神病作用,但不会引起镇静作用。早期的人体试验使用LY-404,039前药形式LY-214,0023,也取得了令人鼓舞的结果。
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mGluR5 PAM
VU 0357121是代谢型谷氨酸受体5(mGlu5)的正变构调节剂(PAM),EC50 = 33 nM,Glumax为92%。
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CTEP是mGlu5受体的高效,选择性和口服生物利用性变构拮抗剂,IC50为2.2 nM。
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mGlu5 receptor 拮抗剂
MPEP是mGlu5受体亚型(IC50 = 36 nM)的有效且高度选择性的非竞争性拮抗剂,并且是mGlu4受体的正构构调节剂。
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GluR modulator
VU 0364439是mGlu4受体的正变构调节剂(PAM)(对于人mGlu4,体外EC50 = 19.8 nM)。
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mGluR 拮抗剂
PHCCC是I组代谢型谷氨酸受体拮抗剂(IC50?3μM)。
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mGlu2 receptor 激动剂
LY 379268是高选择性的II类mGlu受体激动剂(对于hmGlu2和hmGlu3而言,EC50值分别为2.69和4.48 nM),其选择性是I类和III类受体的80倍以上。
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mGluR2 PAM
JNJ-40411813是新颖的mGluR2 PAM。
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mGluR 拮抗剂
SIB 1893是代谢型谷氨酸mGlu5受体亚型的高度选择性非竞争性拮抗剂。
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mGluR 拮抗剂
SIB 1757是mGlu5代谢型谷氨酸受体亚型的高度选择性拮抗剂。
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mGlu4 receptors modulator
VU 0361737是mGluR-4的选择性正变构调节剂(人和大鼠受体的EC50值分别为240和110 nM)。
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mGlu5 receptor 拮抗剂
MPEP HCl是对mGlu5a受体亚型(IC50 = 36 nM)的有效,高度选择性的非竞争性拮抗剂,但在浓度高达30 uM的mGlu1b受体上无激动剂或拮抗剂活性。
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mGluR-2 modulator
JNJ-42153605是亲代谢型谷氨酸2受体的正变构调节剂。
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mGluR-2 拮抗剂
LY 341495已被证明是一种高效的选择性II类代谢型谷氨酸受体(mGluR-2)拮抗剂,对于人类mGluR-2,mGluR,Ki/IC50值分别为2.3、1.3、173、990、6800、8200和22000 nM。mGluR-3,mGluR-8,mGluR-7a,mGluR-1a,mGluR-5a和mGluR-4a。
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mGluR-1 拮抗剂
841720是一种有效的非竞争性mGluR-1拮抗剂,相对于mGluR-5具有34倍的选择性(IC50值分别为10和342 nM)。
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NMDA& mGlu receptor 激动剂
Ibotenic Acid是最初从鹅膏菌属物种中分离出来的一种神经兴奋性氨基酸,它起着NMDA和代谢型谷氨酸受体激动剂的作用。
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Kainate receptor 激动剂
Kainic acid monohydrate是海藻酸酯类离子型谷氨酸受体激动剂。可在体内诱发癫痫发作和神经退行性变,也已用于在啮齿动物中诱发实验性癫痫和检查兴奋性诱发的神经元凋亡机制。
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Noopept是在俄罗斯和周边国家/地区推广并指定为促智剂的药物。
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mGluR5 Modulator
VU0364289是新型N-芳基哌嗪mGlu5阳性变构调节剂。
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mGluR 激动剂
(S)-3,5-DHPG是I类代谢型谷氨酸受体(mGluRs)的激动剂,与mGluR1a和mGluR5a(分别为Ki = 0.9和3.9 uM)结合,但不与离子型谷氨酸受体结合。
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