1. Membrane Transporter/Ion Channel Neuronal Signaling
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  3. AMPA receptor modulator-9

AMPA receptor modulator-9 is an orally active, selective positive allosteric modulator (PAM) of AMPARs with blood-brain barrier penetration. AMPA receptor modulator-9 selectively potentiates AMPAR activity in human and rat models, with an EC2x value of 0.96 μM in rat embryonic cortex primary neurons. AMPA receptor modulator-9 upregulates BDNF protein expression in rat primary cortical neuronal cultures. AMPA receptor modulator-9 enhances AMPA-mediated excitatory postsynaptic responses in rat and mice. AMPA receptor modulator-9 can be used for the study of cognitive disorders.

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AMPA receptor modulator-9

AMPA receptor modulator-9 Chemical Structure

CAS No. : 1204572-46-2

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Description

AMPA receptor modulator-9 is an orally active, selective positive allosteric modulator (PAM) of AMPARs with blood-brain barrier penetration. AMPA receptor modulator-9 selectively potentiates AMPAR activity in human and rat models, with an EC2x value of 0.96 μM in rat embryonic cortex primary neurons. AMPA receptor modulator-9 upregulates BDNF protein expression in rat primary cortical neuronal cultures. AMPA receptor modulator-9 enhances AMPA-mediated excitatory postsynaptic responses in rat and mice. AMPA receptor modulator-9 can be used for the study of cognitive disorders[1].

IC50 & Target[1]

AMPA Receptor

 

In Vitro

AMPA receptor modulator-9 (Compound 14o) exerts AMPA receptor-potentiating activity in primary cultures of neurons from rat embryonic cortex, with an EC2x value of 0.96 μM[1].
AMPA receptor modulator-9 enhances AMPA-evoked inward current in Xenopus laevis oocytes injected with rat cortex or human hippocampus poly(AM+) mRNA (rat cortex mRNA: EC50 = 9.9 μM; human hippocampus mRNA: EC50 = 18 μM)[1].
AMPA receptor modulator-9 (3-30 μM) modulates AMPA-mediated excitatory postsynaptic responses in the CA1 area of rat hippocampal slices through enhancing the response area[1].
AMPA receptor modulator-9 (0.3-10 μM, 24 h) upregulates BDNF protein expression in rat primary cortical neuronal cultures in a dose-dependent manner[1].

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

In Vivo

AMPA receptor modulator-9 (Compound 14o) (0.01-30 mg/kg, i.p., single dose) significantly enhances the induction and maintenance of long-term potentiation (LTP) in the dentate gyrus of anesthetized rats[1].

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

Animal Model: Adult Wistar rats, Adult CD1 mice and Adult C57BI/6 mice[1]
Dosage: 0.01, 0.03, 1, 3, 10, 30 mg/kg
Administration: i.p., single dose
Result: Enhanced the induction and maintenance of long-term potentiation (LTP) in the dentate gyrus (10, 30 mg/kg).
Improved episodic memory in CD1 mice (1, 3 mg/kg).
Enhanced spatial working memory in C57BI/6 mice (0.01, 0.03 mg/kg).
Exertd neuroprotective effects in Wistar rats with transient global cerebral ischemia (10mg/kg).
Molecular Weight

293.17

Formula

C10H10Cl2N2O2S

CAS No.
SMILES

O=S1(NCN(C2=CC(Cl)=C(C=C21)Cl)C3CC3)=O

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    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.

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Product Name:
AMPA receptor modulator-9
Cat. No.:
HY-178153
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