Abstract:
:The potency of six antimuscarinic oxotremorine analogs at sympathetic ganglionic M1 and brainstem M2 muscarinic receptors was compared in the rat. Inhibition of the pressor effects of McNA343 or physostigmine was used as functional indicators of M1 and M2 blockade, respectively. 50% inhibitory doses (ID50) were calculated against both cholinomimetics. Of the analogs, PCA-10 was the most potent, with ID50 values of 0.16 and 0.11 mumol/kg versus McNA343 and physostigmine, respectively. A correlation analysis indicated that these analogs did not functionally discriminate between responses mediated by neuronal M1 or M2 muscarinic receptors in vivo. In contrast, these analogs antagonized M1 ganglionic responses at doses which produced negligible antagonism at cardiac and vascular M2 receptors.
journal_name
Life Scijournal_title
Life sciencesauthors
Vargas HM,Ringdahl Bdoi
10.1016/0024-3205(90)90442-tsubject
Has Abstractpub_date
1990-01-01 00:00:00pages
2065-73issue
22eissn
0024-3205issn
1879-0631pii
0024-3205(90)90442-Tjournal_volume
47pub_type
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