PMID: 9234262Jan 1, 1994Paper

Rodent biodistribution and metabolism of tritiated 4-DAMP, a M3 subtype-selective cholinoceptor ligand

Nuclear Medicine and Biology
A van WaardeW Vaalburg


The biodistribution of [3H]4-DAMP (a M3-selective cholinoceptor antagonist) was studied in rats which had received either saline or saline containing atropine (to block cholinoceptors). Specific binding of the radioligand was observed in the urinary bladder, ileum, pancreas, stomach, submandibular gland and trachea. Maximal ratios of total-to-non-specific uptake reached values of 1.8 (trachea), 3.2 (bladder), 4.0 (stomach), 4.8 (ileum), 6.6 (pancreas) and 6.9 (submandibular gland) at 5-10 min post-injection; this rank order reflects the tissue densities of M3 cholinoceptors, 4-DAMP did not bind to blood cells and it was rapidly cleared from the circulation (> 90% with a half-life of 0.2 min, the remainder with a half-life of 9.4 min). Labelled metabolites appeared within 5 min in plasma, but metabolite uptake by the target organs was low (< 15% of total radioactivity 40 min post-injection). Although 4-DAMP binds to M3-cholinoceptors in vivo, its potential use as a radiopharmaceutical appears limited since the compound does not cross the blood-brain barrier and it does not show measurable specific binding in airways.


Oct 1, 1992·International Journal of Radiation Applications and Instrumentation. Part B, Nuclear Medicine and Biology·A van WaardeK I Lie
Mar 1, 1992·American Journal of Respiratory Cell and Molecular Biology·V K MaheshJ W Bloom
Apr 15, 1985·International Journal of Cancer. Journal International Du Cancer·G TatonG G Poirier
Apr 1, 1989·Pharmacology & Toxicology·J M GrönroosT J Nevalainen
Jan 1, 1989·Pharmacology & Toxicology·L NilvebrantL Malmberg
Sep 1, 1989·British Journal of Pharmacology·S Lazareno, F F Roberts
Aug 3, 1989·European Journal of Pharmacology·A D MichelR L Whiting
Jan 1, 1985·International Journal of Nuclear Medicine and Biology·R E GibsonR Eng
Nov 1, 1984·Pediatric Research·J A Whitsett, B Hollinger
Oct 1, 1983·Toxicology and Applied Pharmacology·B W SchwabS D Murphy

Related Concepts

4-diphenylacetoxy-1,1-dimethylpiperidinium iodide
Radioligand Assay
Drug or Chemical Tissue Distribution
Rats, Wistar
Muscarinic Antagonists

Trending Feeds


Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Lipidomics & Rhinovirus Infection

Lipidomics can be used to examine the lipid species involved with pathogenic conditions, such as viral associated inflammation. Discovered the latest research on Lipidomics & Rhinovirus Infection.

Alzheimer's Disease: MS4A

Variants within the membrane-spanning 4-domains subfamily A (MS4A) gene cluster have recently been implicated in Alzheimer's disease in genome-wide association studies. Here is the latest research on Alzheimer's disease and MS4A.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Torsion Dystonia

Torsion dystonia is a movement disorder characterized by loss of control of voluntary movements appearing as sustained muscle contractions and/or abnormal postures. Here is the latest research.

Generating Insulin-Secreting Cells

Reprogramming cells or using induced pluripotent stem cells to generate insulin-secreting cells has significant therapeutic implications for diabetics. Here is the latest research on generation of insulin-secreting cells.

Central Pontine Myelinolysis

Central Pontine Myelinolysis is a neurologic disorder caused most frequently by rapid correction of hyponatremia and is characterized by demyelination that affects the central portion of the base of the pons. Here is the latest research on this disease.

Epigenome Editing

Epigenome editing is the directed modification of epigenetic marks on chromatin at specified loci. This tool has many applications in research as well as in the clinic. Find the latest research on epigenome editing here.