ABSTRACT
The distribution and kinetics of 14C-vecuronium were studied in rats and mice. 14C-Vecuronium accumulated rapidly in the liver. Both unchanged and metabolized vecuronium were excreted with the bile into the intestines and stomach. Reabsorption in the gut was probably responsible for an enterohepatic increase in radioactivity in the liver after one hour. Excretion through the kidneys increased continuously from low values after the initial peak. Binding in compartments with acid mucopolysaccharides such as cartilage, connective tissue etc., was less important. Blood-brain barrier and placenta were permeable only to a small degree.
Subject(s)
Vecuronium Bromide/pharmacokinetics , Animals , Autoradiography , Carbon Radioisotopes , Female , Male , Mice , Organ Specificity , Pregnancy , Rats , Tissue Distribution , Whole-Body CountingABSTRACT
The alkylating agent [14C]chloroacetylcholine perchlorate [( 14C] ClACh) was synthesized and used for affinity labelling of the nicotinic acetylcholine receptor from Torpedo marmorata. Solubilized and affinity-purified receptor proteins were reduced and alkylated according to the bromoacetylcholine-method. Covalent binding of [14C] ClACh to the cholinergic receptor proved to be specific and saturable, and occurred exclusively to the alpha-subunit. Halogen substitution of acetylcholine by chlorine and insertion of a 14C-isotope instead of the widely used 3H resulted in favourable properties of the affinity label.
