Metabotropic glutamate receptors (mGluR)
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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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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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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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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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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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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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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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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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mGlu5 receptor antagonist
Methoxy-PEPy is a potent and highly selective mGlu5 receptor antagonist with IC50 of 1 nM.
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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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mGluR5 antagonists
Dipraglurant (ADX 48621) is a mGluR5 antagonists with IC50 of 0.021 μM.
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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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