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Evidence for the presence of muscarinic M-2 and M-4 receptors in guinea-pig gallbladder smooth muscle

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dc.contributor.authorKARAALP, ATİLA
dc.contributor.authorsOktay, S; Cabadak, H; Iskender, E; Goren, Z; Caliskan, E; Orun, O; Aslan, N; Karaalp, A; Tolun, A; Ulusoy, NB; Levey, AI; El-Fakahany, EE; Kan, B
dc.date.accessioned2022-03-12T16:57:47Z
dc.date.available2022-03-12T16:57:47Z
dc.date.issued1998
dc.description.abstract1 The affinities of 10 selective muscarinic receptor antagonists against [H-3]-quinuclidinyl benzilate (QNB) binding were determined to characterize the muscarinic receptors present in guinea-pig gallbladder smooth muscle. The highest correlation was obtained for the comparison between the pK(i) values for the gallbladder smooth muscle and M-2 sites. Pirenzepine revealed two binding sites with affinities indicating the presence of muscarinic M-2 receptors in abundance and a minor population of an additional site(s). 2 Carbachol produced gallbladder contractions, stimulated phosphoinositide (PI) hydrolysis and inhibited cAMP formation concentration-dependently with pD(2) values of 6.12 +/- 0.11, 5.18 +/- 0.33 and 7.19 +/- 0.15, respectively. 3 Pirenzepine, 4-DAMP, HHSiD, pF-HHSiD, AF-DX 116, methoctramine, AQ-RA 741, guanylpirenzepine and AF-DX 384 showed competitive antagonism against carbachol-induced gallbladder contractions. There was no correlation between the pA(2) values for the gallbladder and pK(i) values for the M-2 sites, whereas significant correlations were found for the M-1, M-3 and M-4 sites, the best correlation being between the pA(2) values for the gallbladder and M-4 subtypes. 4 Finally, the presence of both m(2) and m(4) receptor proteins were demonstrated by Western blot analysis. It is concluded that guinea-pig gallbladder smooth muscle has both muscarinic M-2 and M-4 receptors, which are coupled to adenylate cyclase inhibition and PI hydrolysis. 5 Although it seems likely that Mt receptors do not play a primary role in carbachol-induced guinea-pig gallbladder contraction, the characterization of the muscarinic subtypes which mediate these contractile responses needs further evidence.
dc.identifier.doi10.1046/j.1365-2680.1998.18474.x
dc.identifier.issn0144-1795
dc.identifier.pubmed9788289
dc.identifier.urihttps://hdl.handle.net/11424/226974
dc.identifier.wosWOS:000076300900001
dc.language.isoeng
dc.publisherWILEY
dc.relation.ispartofJOURNAL OF AUTONOMIC PHARMACOLOGY
dc.rightsinfo:eu-repo/semantics/closedAccess
dc.subjectSIGNAL-TRANSDUCTION PATHWAYS
dc.subjectSUBTYPE-SPECIFIC ANTIBODIES
dc.subjectADENYLATE-CYCLASE
dc.subjectBINDING-PROPERTIES
dc.subjectPHOSPHOINOSITIDE TURNOVER
dc.subjectACETYLCHOLINE-RECEPTORS
dc.subjectANTAGONIST
dc.subjectINHIBITION
dc.subjectM2
dc.subjectHETEROGENEITY
dc.titleEvidence for the presence of muscarinic M-2 and M-4 receptors in guinea-pig gallbladder smooth muscle
dc.typearticle
dspace.entity.typePublication
local.avesis.id339627e1-87ae-4e93-be03-e80a2c9aad4e
local.import.packageSS17
local.indexed.atWOS
local.indexed.atSCOPUS
local.indexed.atPUBMED
local.journal.numberofpages10
oaire.citation.endPage204
oaire.citation.issue4
oaire.citation.startPage195
oaire.citation.titleJOURNAL OF AUTONOMIC PHARMACOLOGY
oaire.citation.volume18
relation.isAuthorOfPublicationf69f1d1c-df19-4b9c-9d29-a8d3882bae38
relation.isAuthorOfPublication.latestForDiscoveryf69f1d1c-df19-4b9c-9d29-a8d3882bae38

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