AF-DX 384 - CAS 118290-26-9
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
AF-DX 384 has been found to be a mAChR M2/M4 selective antagonist.
≥98% by HPLC
Yellow Solid
Canonical SMILES:
1.Involvement of muscarinic M2 and M3, but not of M1 and M4 receptors in vagally stimulated contractions of rabbit bronchus/trachea.
Eltze M;Galvan M Pulm Pharmacol. 1994 Apr;7(2):109-20.
The inhibition of preganglionic and postganglionic contractions of the rabbit isolated bronchus/trachea by antagonists with selectivity for different muscarinic receptor subtypes was compared with their affinities at M1, M2, M3 and M4 receptors. Neither M1/M3 receptor-unselective antagonists (atropine, hexahydro-siladifenidol, thiazinamium, p-fluoro-hexahydro-sila-difenidol) nor antagonists with selectivity for the M1 over M3 subtype ((+)-biperiden, UH-AH 37, telenzepine, o-methoxy-sila-hexocyclium, pirenzepine) consistently showed a preferential inhibition of the response to preganglionic over postganglionic stimulation. Potencies for inhibition of contraction to preganglionic stimulation by antagonists discriminating more than threefold both between M1 and M3, and between M3 and M2 receptors (hexocyclium, (+)-biperiden, UH-AH 37, telenzepine, o-methoxy-silahexocyclium, p-fluoro-hexahydro-sila-difenidol, pirenzepine) are most consistent with affinities at smooth muscle M3 receptors as determined on methacholine-contracted rabbit trachea. Antagonists with a 10-fold higher affinity at M2 over M3 receptors enhanced contractions to field stimulation (AQ-RA 741 = AF-DX 384 = idaverine > himbacine = imperialine = AF-DX 116 = methoctramine >> gallamine), whereas antagonists with a selectivity profile of M4 > or = M3 > M2 (hexahydro-sila-difenidol, pirenzepine, dicyclomine) failed to increase the contractions.
2.Characterization and autoradiographic distribution of [3H]AF-DX 384 binding to putative muscarinic M2 receptors in the rat brain.
Aubert I;Cécyre D;Gauthier S;Quirion R Eur J Pharmacol. 1992 Jul 7;217(2-3):173-84.
The novel radioligand [3H]AF-DX 384 binds specifically and saturably to putative muscarinic M2 receptor sites in homogenates of rat cerebral cortex. In saturation studies, [3H]AF-DX 384 appears to bind to two subpopulations of sites/states, one of high affinity (Kd1 = 0.28 +/- 0.08 nM) and another of low affinity (Kd2 = 28.0 +/- 5.0 nM). The maximal binding capacity (Bmax) of [3H]AF-DX 384 binding sites represented 9.7 +/- 2.3 fmol/mg protein (Bmax1) and 1993 +/- 551 fmol/mg protein (Bmax2) for the high and low affinity sites/states, respectively. The ligand selectivity profile of [3H]AF-DX 384 (at 2 nM) revealed that (-)-quinuclidinyl benzylate = atropine greater than 4-diphenylacetoxy-N-methylpiperidine methobromide greater than AQ-RA 741 greater than AF-DX 384 greater than UH-AH 371 much greater than methoctramine greater than oxotremorine-M greater than hexahydro-sila-defenidol much greater than pirenzepine greater than carbamylcholine much much greater than nicotine. This suggests that under our assay conditions [3H]AF-DX 384 binds mostly to M2-like muscarinic receptors in the rat central nervous system. This is further supported by the clear M2-like pattern of distribution observed using quantitative receptor autoradiography.
3.Comparative ontogenic profile of cholinergic markers, including nicotinic and muscarinic receptors, in the rat brain.
Aubert I;Cécyre D;Gauthier S;Quirion R J Comp Neurol. 1996 May 20;369(1):31-55.
The ontogenic profiles of several cholinergic markers were assessed in the rat brain by using quantitative in vitro receptor autoradiography. Brain sections from animals at different stages of development were processed with [3H]AH5183 (vesamicol; vesicular acetylcholine transport sites), [3H]N-methylcarbamylcholine (alpha(4)beta(2) nicotinic receptor sites), [3H]hemicholinium-3 (high-affinity choline uptake sites), [3H]3-quinuclidinyl benzilate (total population of muscarinic receptor sites), [3H]4-DAMP (muscarinic M1/M3 receptor sites), [3H]pirenzepine (muscarinic M1 receptor sites), and [3H]AF-DX 116 and [3H]AF-DX 384 (muscarinic M2 receptor sites) as radiolabeled probes. The results revealed that, by the end of the prenatal period (embryonic day 20), the densities of nicotinic receptor and vesicular acetylcholine transport sites already represented a considerable proportion of those observed in adulthood (postnatal day 60) in different laminae of the frontal, parietal, and occipital cortices, in the layers of Ammon's horn fields and the dentate gyrus of the hippocampal formation, as well as in the amygdaloid body, the olfactory tubercle, and the striatum. In contrast, at that stage, the densities of total muscarinic, M1/M3, M1, and possibly M2 receptor and high-affinity choline uptake sites represent only a small proportion of levels seen in the adult.
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CAS 118290-26-9 AF-DX 384

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