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AF-DX 116 (CAS 102394-31-0)

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Alternate Names:
11-[[2-[(Diethylamino)methyl]-1-piperidinyl]acetyl]-5,1 1-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one; Otenzepad
Application:
AF-DX 116 is a selective mAChR M2 antagonist
CAS Number:
102394-31-0
Molecular Weight:
421.54
Molecular Formula:
C24H31N5O2
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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AF-DX 116 is a selective muscarinic acetylcholine receptor (mAChR) M2 antagonist. It′s Ki values for human recombinant M2, M1, M3, M4 and M5 muscarinic receptors are 64, 417, 786, 211 and 5130 nM, respectively. AF-DX 116 is a fluorescent probe that can bind to muscarinic receptors


AF-DX 116 (CAS 102394-31-0) References

  1. Comparison of anti-M2-muscarinic effect of AF-DX 116 on atrioventricular nodal conduction with those of pirenzepine and atropine as antibradyarrhythmic drugs.  |  Sasaki, S. and Motomura, S. 1999. J Cardiovasc Pharmacol. 33: 912-21. PMID: 10367595
  2. An AF-DX 116 sensitive inhibitory mechanism modulates nicotinic and muscarinic transmission in cat superior cervical ganglion in the presence of anticholinesterase.  |  Bachoo, M. and Polosa, C. 1992. Can J Physiol Pharmacol. 70: 1535-41. PMID: 1338712
  3. Effects of pirenzepine and AF-DX 116 on ganglionic transmission in the cardiac sympathetic nerves of the dog: interaction of M1 and M2 receptors with nicotinic receptors.  |  Mukaiyama, O., et al. 1991. J Pharmacol Exp Ther. 256: 525-9. PMID: 1704433
  4. AF-DX 116, a cardioselective muscarinic antagonist in humans: pharmacodynamic and pharmacokinetic properties.  |  Schulte, B., et al. 1991. Clin Pharmacol Ther. 50: 372-8. PMID: 1914372
  5. AF-DX 116 differentiates between prejunctional muscarine receptors located on noradrenergic and cholinergic nerves.  |  Dammann, F., et al. 1989. Naunyn Schmiedebergs Arch Pharmacol. 339: 268-71. PMID: 2725704
  6. AF-DX 116 discriminates heart from gland M2-cholinoceptors in man.  |  Pitschner, HF., et al. 1989. Life Sci. 45: 493-8. PMID: 2770414
  7. Binding sites for [3H]AF-DX 116 and effect of AF-DX 116 on endogenous acetylcholine release from rat brain slices.  |  Lapchak, PA., et al. 1989. Brain Res. 496: 285-94. PMID: 2804636
  8. AF-DX 116, a cardioselective muscarinic antagonist.  |  Micheletti, R., et al. 1987. J Pharmacol Exp Ther. 241: 628-34. PMID: 2883303
  9. Muscarinic receptor heterogeneity in smooth muscle: binding and functional studies with AF-DX 116.  |  Ladinsky, H., et al. 1988. Trends Pharmacol Sci. Suppl: 44-8. PMID: 3074536
  10. AF-DX 116: a selective antagonist of the slow inhibitory postsynaptic potential and methacholine-induced hyperpolarization in superior cervical ganglion of the rabbit.  |  Yarosh, CA., et al. 1988. J Pharmacol Exp Ther. 245: 419-25. PMID: 3284995
  11. [3H]AF-DX 116 labels subsets of muscarinic cholinergic receptors in rat brain and heart.  |  Wang, JX., et al. 1987. Life Sci. 41: 1751-60. PMID: 3657382
  12. Cardioselective profile of AF-DX 116, a muscarine M2 receptor antagonist.  |  Giachetti, A., et al. 1986. Life Sci. 38: 1663-72. PMID: 3754611
  13. Facilitation of memory storage by the acetylcholine M2 muscarinic receptor antagonist AF-DX 116.  |  Baratti, CM., et al. 1993. Behav Neural Biol. 60: 69-74. PMID: 8216161
  14. AF-DX 116, a presynaptic muscarinic receptor antagonist, potentiates the effects of glucose and reverses the effects of insulin on memory.  |  Kopf, SR., et al. 1998. Neurobiol Learn Mem. 70: 305-13. PMID: 9774523
  15. Effects of a cardioselective M2 receptor antagonist, AF-DX 116, on ventricular arrhythmias in dogs.  |  Naito, H., et al. 1997. Heart Vessels. 12: 229-33. PMID: 9846808

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

AF-DX 116, 5 mg

sc-223772
5 mg
$107.00