2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. iGluR
  4. BPAM363

BPAM363 is an orally active, selective positive allosteric modulator (PAM) of AMPARs with blood-brain barrier penetration. BPAM363 selectively potentiates AMPAR activity in human and rat models, with an EC2x value of 0.96 μM in rat embryonic cortex primary neurons. BPAM363 upregulates BDNF protein expression in rat primary cortical neuronal cultures. BPAM363 enhances AMPA-mediated excitatory postsynaptic responses in rat and mice. BPAM363 can be used for the study of cognitive disorders.

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BPAM363

BPAM363 Chemical Structure

CAS No. : 1204572-46-2

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BPAM363 Related Antibodies

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Description

BPAM363 is an orally active, selective positive allosteric modulator (PAM) of AMPARs with blood-brain barrier penetration. BPAM363 selectively potentiates AMPAR activity in human and rat models, with an EC2x value of 0.96 μM in rat embryonic cortex primary neurons. BPAM363 upregulates BDNF protein expression in rat primary cortical neuronal cultures. BPAM363 enhances AMPA-mediated excitatory postsynaptic responses in rat and mice. BPAM363 can be used for the study of cognitive disorders[1].

IC50 & Target[1]

AMPA Receptor

 

In Vitro

BPAM363 (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].
BPAM363 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].
BPAM363 (3-30 μM) modulates AMPA-mediated excitatory postsynaptic responses in the CA1 area of rat hippocampal slices through enhancing the response area[1].
BPAM363 (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.

BPAM363 Related Antibodies
Parmacokinetics
Species Dose Route Vss T1/2 AUC Cmax F Tmax
Rat[1] 1.5 mg/kg i.v. 3.89 L/kg 2.9 h 1363 ng·h/mL 1038 ng/mL / /
Rat[1] 3 mg/kg p.o. / / 1887 ng·h/mL 189 ng/mL 69.2 % 6 h
In Vivo

BPAM363 (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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Room temperature in continental US; may vary elsewhere.
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Purity & Documentation
References
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BPAM363 Related Classifications

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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:

BPAM3631204572-46-2BPAM 363BPAM-363iGluRIonotropic glutamate receptorscognitive disordersAMPABDNFInhibitorinhibitorinhibit

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