The effect of calmodulin antagonists on amylase release from the rat parotid gland in vitro

1983 ◽  
Vol 397 (3) ◽  
pp. 220-224 ◽  
Author(s):  
Terry N. Spearman ◽  
Fred R. Butcher
1993 ◽  
Vol 264 (3) ◽  
pp. G541-G552
Author(s):  
Y. Hiramatsu ◽  
R. Kawai ◽  
R. C. Reba ◽  
T. R. Simon ◽  
B. J. Baum ◽  
...  

(RR)- and (SS)-quinuclidinyl iodobenzilate enantiomers [(RR)- and (SS)-IQNB, active and inert, respectively] have been synthesized for quantitative evaluation of muscarinic acetylcholine receptor (mAChR) binding. Pharmacokinetic approaches have not been used previously to assess in vivo IQNB binding in nonexcitable tissues. We have applied this method to examine mAChRs in rat parotid gland in comparison to those in brain and heart. Short-term infusion studies in vivo showed that the "instantaneous" reversible binding of (RR)- and (SS)-IQNB was high in the parotid (greater nonspecific binding potential), intermediate in the heart, and lowest in cortex and cerebellum. Long-term bolus injection experiments showed that the parotid gland mAChRs possessed a binding potential for receptor specific sites (380), which was intermediate between that of parietal cortex (930) and cerebellum (10) and greater than that of heart (165). In vitro binding to plasma membranes was generally consistent with the in vivo findings. In aggregate, these studies show that mAChRs can be evaluated in vivo in a nonexcitable tissue with the use of stereospecific ligands and a pharmacokinetic approach. The data suggest that IQNB, a mAChR antagonist, can identify characteristics of specific binding sites, which may reflect tissue differences.


1980 ◽  
Vol 25 (8-9) ◽  
pp. 597-600 ◽  
Author(s):  
Akifumi Togari ◽  
Takeshi Kato ◽  
Toshiharu Nagatsu

1989 ◽  
Vol 49 ◽  
pp. 174
Author(s):  
Kazuhiro Yamada ◽  
Akifumi Togari ◽  
Shosei Matsumoto

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