Abstract：
:The identity of the muscarinic receptor subtype in the chick ileum was investigated in functional and binding studies. Preliminary studies [Choo, L.-K., Mitchelson, F., Napier, P. 1988. J. Auton. Pharmacol. 8, 259-266] suggested apparent avian and mammalian family differences in the muscarinic receptor profile of ileal smooth muscle. In the current study, further characterisation was undertaken using a greater range of antagonists exhibiting high affinity for specific muscarinic receptor subtypes. Dissociation constants from functional and binding experiments were compared with published values for antagonists at each of the five muscarinic receptor subtypes. Linear regression and correlation analyses revealed the receptor initiating the contractile response was most likely of the muscarinic M(3) receptor subtype as the slope of the linear regression was 1.01+/-0.14 and the corresponding correlation coefficient (r) was 0.95. The mammalian muscarinic M(5) receptor subtype also showed a high correlation with the data giving a slope of 0.89+/-0.27 and r value of 0.76. These findings were in direct contrast to those from binding experiments in which the single binding site detected was of the muscarinic M(2) receptor subtype. The slope of the linear regression was 1.14+/-0.24 with an r value of 0.87. Thus, these results suggest that there exists a high proportion of the muscarinic M(2) receptor subtype within the tissue that does not contribute to the functional response.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Darroch S,Irving HR,Mitchelson FJdoi
10.1016/s0014-2999(00)00489-1keywords:
subject
Has Abstractpub_date
2000-08-18 00:00:00pages
161-9issue
1-2eissn
0014-2999issn
1879-0712pii
S0014-2999(00)00489-1journal_volume
402pub_type
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