ABCC8 p.Tyr179Ala
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PMID: 20660086
[PubMed]
Jacobson MA et al: "The M1 muscarinic receptor allosteric agonists AC-42 and 1-[1'-(2-methylbenzyl)-1,4'-bipiperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one bind to a unique site distinct from the acetylcholine orthosteric site."
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Sentence
Comment
167
In comparison, the affinity of N-desmethylclozapine was only slightly changed on W101A and W101F, where a 2-fold decrease and 1.25-fold increase in potency were measured, respectively. Substitution of Tyr179 with either alanine or phenylalanine resulted in only minor changes in functional potencies -10 -9 -8 -7 -6 -5 -4 -3 0 20 40 60 80 100 Ile Phe Log [Agonist] (M) %Max -10 -9 -8 -7 -6 -5 -4 -3 0 20 40 60 80 100 Asn Gly Log [Agonist] (M) %Max -10 -9 -8 -7 -6 -5 -4 -3 0 20 40 60 80 100 Asn Thr Log [Agonist] (M) %Max Ach AC42 TBPB Fig. 4.
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ABCC8 p.Tyr179Ala 20660086:167:201
status: NEW173 The affinity of acetylcholine was decreased by only 2.5and 2-fold on Y179A and Y179F, respectively.
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ABCC8 p.Tyr179Ala 20660086:173:69
status: NEW175 The affinity for AC-42 and TBPB were increased on Y179A by 1.25and 2.9-fold, respectively.
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ABCC8 p.Tyr179Ala 20660086:175:50
status: NEW