An AMPA receptor positive allosteric modulator
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CX-546

Item No. 45130

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2,3-dihydro-1,4-benzodioxin-6-yl)-1-piperidinyl-methanone
CAS Number
215923-54-9
Molecular Formula
C14H17NO3
Formula Weight
247.3
Purity
≥98%
Formulation (Request formulation change)
A solid
SMILES
O=C(N1CCCCC1)C2=CC=C3OCCOC3=C2
InChi Code
InChI=1S/C14H17NO3/c16-14(15-6-2-1-3-7-15)11-4-5-12-13(10-11)18-9-8-17-12/h4-5,10H,1-3,6-9H2
InChi Key
LJUNPHMOGNFFOS-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $69

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    10 mg

    $110

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    25 mg

    $207

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    50 mg

    $345

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    Product Description

    CX-546 is an AMPA receptor positive allosteric modulator.1,2 CX-546 (300 µM) attenuates desensitization and slows deactivation of glutamate-stimulated GluA1 and GluA2 subunit-containing AMPA receptors. It increases AMPA-stimulated glucose utilization in cortical astrocytes (EC50 = 93.2 µM).3 In vivo, CX-546 (10 mg/kg) reduces mechanical and cold allodynia and immobility time in the forced swim test in a rat model of neuropathic pain induced by spared nerve injury (SNI).4 It reverses fentanyl- and phenobarbital-mediated respiratory depression in rats when administered at a dose of 16 mg/kg.5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Nagarajan, N., Quast, C., Boxall, A.R., et al. Mechanism and impact of allosteric AMPA receptor modulation by the ampakine™ CX546. Neuropharmacology 41(6), 650-663 (2001).

    2. Arai, A.C., Xia, Y.-F., Rogers, G., et al. Benzamide-type AMPA receptor modulators form two subfamilies with distinct modes of action. J. Pharmacol. Exp. Ther. 303(3), 1075-1085 (2002).

    3. Pellerin, L., and Magistretti, P.J. Ampakine™ CX546 bolsters energetic response of astrocytes: A novel target for cognitive-enhancing drugs acting as α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor modulators. J. Neurochem. 92(3), 668-677 (2005).

    4. Le, A.M., Lee, M., Su, C., et al. AMPAkines have novel analgesic properties in rat models of persistent neuropathic and inflammatory pain. Anesthesiology 121(5), 1080-1090 (2014).

    5. Ren, J., Poon, B.Y., Tang, Y., et al. Ampakines alleviate respiratory depression in rats. Am. J. Respir. Crit. Care Med. 174(12), 1384-1391 (2006).