Product overview

Name AF-DX 116
Alternative names Otenzepad
Purity >98%
Description Selective, competitive M2 receptor antagonist
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Biological Data

Biological description Selective and competitive M2 muscarinic receptor antagonist. Selective for M2 over M3 (Ki values are 64 and 786 nM respectively). Shows selectivity for cardiac muscarinic receptors. Shows hypertensive actions and increases heart rate in cold-stressed rats.

Solubility & Handling

Storage instructions Room temperature
Solubility overview Soluble in DMSO (25mM, gentle warming)
Important This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.

Calculators

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Chemical Data

Purity >98%
Chemical name 11-[[2-[(Diethylamino)methyl]-1-pip eridinyl]acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4 ]benzodiazepin-6-one
Molecular Weight 421.54
Chemical structure AF-DX 116  [102394-31-0] Chemical Structure
Molecular Formula C24H31N5O2
CAS Number 102394-31-0
PubChem identifier 107867
SMILES CCN(CC)CC1CCCCN1CC(=O)N1C2=C(C=CC=C2)C(=O)NC2=CC=CN=C12
InChiKey UBRKDAVQCKZSPO-UHFFFAOYSA-N

References for AF-DX 116

References are publications that support the biological activity of the product
  • BK channel β1 subunits regulate airway contraction secondary to M2 muscarinic acetylcholine receptor mediated depolarization.

    Semenov I et al (2011) J Physiol 589(Pt 7) : 1803-17.
  • Blood pressure and heart rate are increased by AF-DX 116, a selective M2 antagonist, in autonomic imbalanced and hypotensive rats caused by repeated cold stress.

    Hata T et al (2001) Jpn J Pharmacol 85(3) : 313-21.
  • Binding profile of a novel cardioselective muscarine receptor antagonist, AF-DX 116, to membranes of peripheral tissues and brain in the rat.

    Hammer R et al (1986) Life Sci 38(18) : 1653-62.

3 Item(s)

Publications
These publications cite the use of AF-DX 116 purchased from Hello Bio:
  • Targeting muscarinic receptor subtypes as a therapeutic approach in dystonia and Parkinson’s disease

    Klisko DM (2017) Dissertation : 1:2627

1 Item