DARIFENACIN REVEALS A FUNCTIONAL ROLE FOR M4 MUSCARINIC ACETYLCHOLINE RECEPTORS IN GUINEA PIG GALLBLADDER

Ahmet Akıcı; Muradiye Nacak; Arthur Christopoulos; Şule Oktay

Article Details

DARIFENACIN REVEALS A FUNCTIONAL ROLE FOR M4 MUSCARINIC ACETYLCHOLINE RECEPTORS IN GUINEA PIG GALLBLADDER

Authors:

Ahmet Akıcı | Muradiye Nacak | Arthur Christopoulos | Şule Oktay

Publisher:

Marmara University

Journal:

Marmara Medical Journal 2002 Vol.15 Issue 4, pp.248-252

Document Type:

Article

Publication Date:

12/2016

Document Language:

Turkish

Document ID (Org No.):

2000546372

Frequency:

Monthly

eISSN:

1309-9469

pISSN:

1019-1941

Abstract:

 


Objective: Previous studies have revealed the presence of M1 to M4 muscarinic receptors in guinea pig gallbladder, with M3 and M4 receptors being claimed to mediate contractions.Methods: In the present study, cumulative concentration-response curves to carbachol were constructed in the absence and presence of darifenacin, which has greater selectivity for M3 over M4 receptors, in guinea-pig gallbladder.Results: Darifenacin caused concentration- dependent dextral shifts of the carbachol curve, however, at 1 pM, it also caused a degree of insurmountable antagonism. Using a novel analytical approach, we obtained a pKB estimate for darifenacin (7.51 ± 0.14) that is in excellent agreement with its affinity for M2/M4, but not M3 receptors.Conclusion: Given our previous demonstration that M2 receptors are unlikely to contribute to muscarinic contractions in this tissue, our currentfindings provide pharmacological evidence for a predominant role of M4 muscarinic receptors in guinea pig gallbladder contractions.Key Words: Muscarinic receptor, Guinea-pig, Gallbladder, Contraction, Darifenacin.

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Article Details

DARIFENACIN REVEALS A FUNCTIONAL ROLE FOR M4 MUSCARINIC ACETYLCHOLINE RECEPTORS IN GUINEA PIG GALLBLADDER

Authors: Ahmet Akıcı | Muradiye Nacak | Arthur Christopoulos | Şule Oktay

Publisher: Marmara University

Journal: Marmara Medical Journal 2002 Vol.15 Issue 4, pp.248-252

Document Type: Article

Publication Date: 12/2016

Document Language: Turkish

Document ID (Org No.): 2000546372

Frequency: Monthly

eISSN: 1309-9469

pISSN: 1019-1941

Issues

Authors:

Ahmet Akıcı | Muradiye Nacak | Arthur Christopoulos | Şule Oktay

Publisher:

Marmara University

Journal:

Marmara Medical Journal 2002 Vol.15 Issue 4, pp.248-252

Document Type:

Article

Publication Date:

12/2016

Document Language:

Turkish

Document ID (Org No.):

2000546372

Frequency:

Monthly

eISSN:

1309-9469

pISSN:

1019-1941