BOUWER, J

PAANS, AM

VAALBURG, W

VANWAARDE, A

Visser, Gerben

Visser, Thomas

The biodistribution of [H-3]4-DAMP (a M(3)-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 M(3) cholinoceptors. 4-DAMP did not bind to blood cells and it was rapidly cleared from the circulation (&gt;90% with a half-life of 0.2 min, the remainder with a half-life of 9.4 min). Labelled metabolites appeared within 5min in plasma, but metabolite uptake by the target organs was low (</p

RODENT BIODISTRIBUTION AND METABOLISM OF TRITIATED 4-DAMP, A M(3) SUBTYPE-SELECTIVE CHOLINOCEPTOR LIGAND

Abstract

Similar works

Full text

Available Versions

Dissertations of the University of Groningen