TY - JOUR
AU1 - Lebbin, Claudia
AU2 - Hofmann, Alfred
AU3 - Waser, Peter
AB - 


1.

The activities of some cholinergic compounds were investigated on the terminal ileum of the guinea-pig and their muscarinic potencies were found to be in the following order: acetylcholine (ACh) > diazoacetylcholine (DACh) > iodoacetylcholine (IACh) > azidoacetylcholine (AACh).



2.

Protection experiments with atropine showed a decreased affinity of the four cholinergic compounds for the muscarinic receptor, demonstrating a direct interaction of the drugs and the receptor.



3.

The maximal contractions (intrinsic activity) caused by DACh were greater than those caused by ACh, IACh and AACh.



4.

Incubation of the ileum with ACh was followed by a reversible loss of its ability to contract (desensitization). The time course of recovery was similiar to that after incubation with AACh.



5.

IACh caused a partial (50%), irreversible paralysis of the muscle.



6.

The furaziridines seem to react partially irreversibly (30%), whereas, paranitrophenyldiazonium fluoborate (p-NDB) caused a complete, irreversible blockade of the muscarinic receptor.




TI - Affinity-labelling of the muscarinic receptor of the guinea-pig ileum
JF - Naunyn-Schmiedeberg's Archives of Pharmacology
DO - 10.1007/BF00499978
DA - 2004-10-05
UR - https://www.deepdyve.com/lp/springer-journals/affinity-labelling-of-the-muscarinic-receptor-of-the-guinea-pig-ileum-sURrj0XUyr
SP - 237
EP - 249
VL - 289
IS - 3
DP - DeepDyve
ER -