Back to Search
Start Over
THE ACTIONS OF SOME ESTERS OF 4-HYDROXYQUINUCLIDINE ON GUINEA-PIG ILEUM, ATRIA AND RAT FUNDUS STRIP
- Source :
- British Journal of Pharmacology. 77:549-557
- Publication Year :
- 1982
- Publisher :
- Wiley, 1982.
-
Abstract
- 1 The acetyl, phenylacetyl, and diphenylacetyl esters of 4-hydroxyquinuclidine and their methiodides have been prepared. 2 4-Diphenylacetoxyquinuclidine methiodide has higher affinity for muscarinic receptors than 4-diphenylacetoxy-N-methylpiperidine methiodide (4-DAMP methiodide) but it is less selective. At 30°C its affinity for receptors in ileum is about 5 times that for receptors in atria, a difference similar to that found with diphenylacetoxytrophine methiodide. With 4-DAMP methiodide affinity for receptors in the ileum is over 10 times that for receptors in atria. 3 4-Diphenylacetoxyquinuclidine methiodide has higher affinity for muscarinic receptors than 3-diphenylacetoxyquinuclidine hydrochloride or its methiodide. 4 4-Acetoxyquinuclidine hydrochloride has less than one-hundredth of the activity of 3-acetoxyquinuclidine hydrochloride (acecyclidine) on guinea-pig ileum, atria, and rat fundus: however, 4-acetoxyquinuclidine methiodide is consistently more active than its 3-isomer, though it is only about 1/25 times as active as acecyclidine. 5 4-Acetoxyquinuclidine hydrochloride is only a poor substrate for electric eel acetylcholinesterase: its affinity is similar to that of acecyclidine but it is greatly reduced by methylation. 6 The relations between the structure and activity of the agonists are very different from the relations between the structure and affinity of the antagonists, which supports the view that agonists and antagonists bind to different conformations of the muscarinic receptor.
- Subjects :
- Quinuclidines
Hydrochloride
Stereochemistry
Guinea Pigs
Ileum
Parasympathomimetics
In Vitro Techniques
Structure-Activity Relationship
chemistry.chemical_compound
Muscarinic acetylcholine receptor
medicine
Animals
Structure–activity relationship
Receptors, Cholinergic
Gastric Fundus
Methiodide
Receptor
Pharmacology
Parasympatholytics
Heart
Receptors, Muscarinic
Acetylcholinesterase
Rats
Kinetics
medicine.anatomical_structure
chemistry
Papers
Subjects
Details
- ISSN :
- 00071188
- Volume :
- 77
- Database :
- OpenAIRE
- Journal :
- British Journal of Pharmacology
- Accession number :
- edsair.doi.dedup.....623376a40de56790ba028afe28721c8c