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N-[ 11 C]Methyl-3-[[(dimethylamino)carbonyl]oxy]-2-(2',2'-diphenylpropionoxymethyl)pyridinium

N-[ 11 C]Methyl-3-[[(dimethylamino)carbonyl]oxy]-2-(2',2'-diphenylpropionoxymethyl)pyridinium

The MICAD Research Team

PMID: 20641552

Abstract:

Acetylcholinerase (AChE) is an enzyme involved in terminating nerve impulses by hydrolyzing the neurotransmitter acetylcholine (ACh). It plays an important role in heart rate and cardiac contractions, for example, by decreasing the ACh levels associated with cardiac parasympathetic responses (1).
AChE, and more exactly the inhibition of its enzymatic function, also seems to play an important role in poisoning from organophosphorus (OP) agents (2). Current treatments consisting of a reversible covalent AChE inhibitor (pyridostigmine (3)), a receptor antagonist atropine (ATR), and a AChE reactivator (pralidoxime chloride) have shown good protection against OP intoxication in animals. Research efforts are being made to find drugs with multiple protective functions. For example, Leader et al. (4) synthesized and evaluated a group of pyridophen analogues, binary pyridogstigmine-aprophen prodrugs with differential inhibition of AChE, butyrylcholinesterase (BChE), and muscarinic receptors (5).
Most of the AChE heart tracers developed for cardiac neurotransmission using positron emission tomography (PET) have shown low selectivity of AChE over BChE, and non-specific binding in AChE enzyme overexpressed regions (6). [11C]Nedrophonium and [11C]Neostigmine, originally developed as potential PET heart imaging agents, have shown either high nonspecific binding or poor myocardial uptake and were therefore unsuitable for PET imaging of the heart vagal system.
[11C]pyridostigmine and its para- and ortho-analogs, as well as N-[11C]methyl-3-[[(dimethylamino)carbonyl]oxy]-2-(2',2'-diphenylpropionoxymethyl)pyridinium ([11C]MDDP), were synthesized by Wang et al. (7) as potential PET agents for imaging heart AChE in vivo. Leader et al. (4) showed that MDDP iodide selectively inhibited AChE more than BChE. However, the first rodent studies performed by Wang et al. (7) using PET- [11C]MDDP did show the presence of nonspecific binding (see the Rodents section for details).

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP56512493	4-(Dimethylamino)azobenzene-4′-sulfonyl chloride		56512-49-3	Price

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