An M2 and M4 muscarinic acetylcholine receptor antagonist
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AF-DX 384

Item No. 25638

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2-[2-[(dipropylamino)methyl]-1-piperidinyl]ethyl]-5,6-dihydro-6-oxo-11H-pyrido[2,3-b][1,4]benzodiazepine-11-carboxamide
CAS Number
118290-26-9
Molecular Formula
C27H38N6O2
Formula Weight
478.6
Purity
≥95%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 50 mMEthanol: 10 mM
SMILES
O=C1NC(C=CC=N2)=C2N(C(NCCN3C(CN(CCC)CCC)CCCC3)=O)C4=C1C=CC=C4
InChi Code
InChI=1S/C27H38N6O2/c1-3-16-31(17-4-2)20-21-10-7-8-18-32(21)19-15-29-27(35)33-24-13-6-5-11-22(24)26(34)30-23-12-9-14-28-25(23)33/h5-6,9,11-14,21H,3-4,7-8,10,15-20H2,1-2H3,(H,29,35)(H,30,34)
InChi Key
MZDYABXXPZNUCT-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $37

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    5 mg

    $98

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    10 mg

    $142

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    25 mg

    $306

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    Product Description

    AF-DX 384 is an antagonist of M2 and M4 muscarinic acetylcholine receptors (Kis = 6.03 and 10 nM, respectively).1 It is selective for M2 and M4 over M1, M3, and M5 receptors (Kis = 30.9, 66.07, and 537.03 nM, respectively). AF-DX 384 increases acetylcholine release in the hippocampus and cortex of young and aged rats in vivo when infused locally at a concentration of 1 µM and in the cortex when administered intraperitoneally at a dose of 5 mg/kg.2 It reverses deficits in novel object recognition and passive avoidance in aged rats, as well as in young rats with impairments induced by scopolamine (Item No. 14108).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Dörje, F., Wess, J., Lambrecht, G., et al. Antagonist binding profiles of five cloned human muscarinic receptor subtypes. J. Pharmacol. Exp. Ther. 256(2), 727-733 (1991).

    2. Vannucchi, M.G., Scali, C., Kopf, S.R., et al. Selective muscarinic antagonists differentially affect in vivo acetylcholine release and memory performances of young and aged rats. Neuroscience 79(3), 837-846 (1997).