The binding of [3H]telenzepine to muscarinic acetylcholine receptors in calf forebrain.
Telenzepine binds to calf brain muscarinic receptors with a selectivity for M1 receptors that is comparable to that exhibited by pirenzepine. Telenzepine has a 10-fold higher affinity than pirenzepine at these receptors and is equipotent with atropine. Because of its potency, selectivity and hydrophilicity, [3H]telenzepine is an excellent radioligand for binding to and monitoring M1 receptor binding sites. The kinetics of [3H]telenzepine binding are extremely slow, even at 37 degrees C.
Schudt
C
C
Department of Biochemistry, Byk Gulden Lomberg Chemische Fabrik GmbH, Konstanz, F.R.G.
Auriga
C
C
Kinder
B
B
Birdsall
N J
NJ
D000818:Animals; D001921:Brain / Q000378:metabolism*; D002417:Cattle; D002540:Cerebral Cortex / Q000187:drug effects / Q000378:metabolism; D066298:In Vitro Techniques; D010276:Parasympatholytics / Q000494:pharmacology*; D010890:Pirenzepine / Q000031:analogs & derivatives* / Q000378:metabolism; D011976:Receptors, Muscarinic / Q000187:drug effects / Q000378:metabolism*
D010276:Parasympatholytics; D011976:Receptors, Muscarinic; C046338:telenzepine; D010890:Pirenzepine