YM-202074

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YM-202074 is a selective, allosteric metabotropic glutamate receptor type 1 (mGluR1) antagonist with high affinity. YM-202074 binds to the allosteric site of rat mGluR1 with a K_i of 4.8 nM. YM-202074 fumarate also inhibits mGluR1-mediated inositol phosphate production in rat cerebellar granule cells with an IC₅₀ of 8.6 nM. YM-202074 has potent neuroprotective effects in transient MCA (tMCA) occlusion rat models.

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YM-202074 Chemical Structure

CAS No. : 299900-83-7

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Other Forms of YM-202074:

YM-202074 fumarate Get quote

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Description

IC₅₀ & Target

rat mGluR1

4.8 nM (Ki)

In Vitro

YM-202074 significantly inhibits the mGluR1-mediated inositol phosphates production in rat cerebellar granule cells with an IC₅₀ of 8.6 nM^[1].
YM-202074 shows specific selectivity over other mGluRs, such as without agonistic nor antagonistic activity on mGluR2, mGluR3, mGluR4a, mGluR6 or mGluR7b (≤ 10 μM), but inverse agonistic activity on mGluR5 (10 μM) in HEK cells and CHO cells^[1].
YM-202074 shows no affinity for ionotropic glutamate receptors (≤ 10 μM) and moderate off-target activity at a few receptors, such as with >60% inhibition of Adrenaline α2C receptor, dopamine transporter, acetylcholine M2/M4 receptor, sigma2 receptor, sodium channel site 2, and ≤ 50% inhibition of other 74 sites^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

YM-202074 (i.v. infusion, 5 mg/kg/h for 8 h or 20 mg/kg/h for 0.5 h followed by 5 mg/kg/h for 7.5 h) rapidly reaches the brain, achieving a free concentration of approximately 0.3 μM within 12 minutes and a steady-state phase within 1.5 hours with the loading infusion of 20 mg/kg/h for 0.5 h^[1].
YM-202074 (i.v. infusion, 10-20 mg/kg/h for 0.5 h followed by 2.5-5 mg/kg/h for 0.5-6 h) provides neuroprotection independent of nonspecific factors such as hypothermia, with no significant Physiological variables in tMCA occlusion rat models^[1].
YM-202074 (i.v. infusion, 10-20 mg/kg/h for 0.5 h followed by 2.5-5 mg/kg/h for 23.5 h) dose-dependently improves neurological deficit and reduces the infarct volume in both the hemisphere and cortex in tMCA occlusion rat models, with potent efficacy in high dose^[1].
YM-202074 (i.v. infusion, 20 mg/kg/h for 0.5 h followed by 5 mg/kg/h from 2 or 3 h to 24 h after tMCA occlusion) significantly maintains neuroprotection even when given 2 h after the onset of ischemia in tMCA occlusion rat models^[1].
YM-202074 (i.v. infusion, 20 mg/kg/h for 0.5 h followed by 5 mg/kg/h from 2h to 24 h week after tMCA occlusion) notably sustains the improvement of neurological deficit and the reduction of infarct volume as well as increase of rat body weight for 1 week following the onset of ischemia in tMCA occlusion rat models^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male SD rats firstly given a left jugular vein cannulation at the dorsal neck with chloral hydrate anesthesia (i.p., 350 mg/kg,), and 24 h later, a 3-0 poly-L-lysine-coated suture was advanced about 17 mm intracranially from the common carotid artery bifurcation via the right and internal external carotid artery with halothane (0.5-1.5%) for 3 h^[1].
Dosage:	10 or 20 mg/kg/h (loading infusion), 2.5 or 5 mg/kg/h (maintenance infusion)
Administration:	i.v. infusion, loading infusion for 0.5 h followed by maintenance infusion for 23.5 h
Result:	Dose-dependently improved neurological deficit and reduces the infarct volume in both the hemisphere and cortex in tMCA occlusion rat models. Significantly reduced infarct volume in the hemisphere and the cortex by 55% and 70%, and improved neurological scores in tMCA occlusion rat models with 20 mg/kg/h for 0.5 h followed by 5 mg/kg/h for 23.5 h.

Animal Model:	Male SD rats firstly given a left jugular vein cannulation at the dorsal neck with chloral hydrate Anesthesia (i.p., 350 mg/kg,), and24 h later, a 3-0 poly-L-lysine-coated suture was advanced about 17 mm intracranially from the common carotid artery bifurcation via the right and internal external carotid artery with halothane (0.5–1.5%) for 3 h^[1].
Dosage:	20 mg/kg/h (loading infusion), 5 mg/kg/h (maintenance infusion)
Administration:	i.v. infusion, loading infusion for 0.5 h followed by maintenance infusion from 2 or 3 h to 24 h after tMCA occlusion, and then measured infarct volume of ischemic damage.
Result:	Significantly maintained neuroprotection even when given 2 h after the onset of ischemia in tMCA occlusion rat models, with the degree of protection against hemisphere and subcortical infarct volume by 34% and 37%, respectively. Notably sustained the improvement of neurological deficit and the reduction of infarct volume (especially cortex by 39%) as well as increase of rat body weight for 1 week following the onset of ischemia in tMCA occlusion rat models.

Molecular Weight

414.56

Formula

C₂₂H₃₀N₄O₂S

CAS No.

299900-83-7

SMILES

O=C(N(C1CCCCC1)C)C2=CN3C4=C(C=CC(CN(CCOC)C)=C4)N=C3S2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Kohara A, et al. Neuroprotective effects of the selective type 1 metabotropic glutamate receptor antagonist YM-202074 in rat stroke models. Brain Res. 2008 Jan 29; 1191:168-79. [Content Brief]

YM-202074 Related Classifications

Neurological Disease

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

YM-202074299900-83-7YM202074YM 202074mGluRMetabotropic glutamate receptorsAntagonistmGluR1NeuroprotectionRat cerebellar granule cellsHEK cellsCHO cellstMCA occlusion rat modelInhibitorinhibitorinhibit

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