Bupropion binds to two sites in the Torpedo nicotinic acetylcholine receptor transmembrane domain: a photoaffinity labeling study with the bupropion analogue [125I] …
A Pandhare, AK Hamouda, B Staggs, S Aggarwal… - Biochemistry, 2012 - ACS Publications
Bupropion, a clinically used antidepressant and smoking-cessation drug, acts as a
noncompetitive antagonist of nicotinic acetylcholine receptors (nAChRs). To identify its
binding site (s) in nAChRs, we developed a photoreactive bupropion analogue,(±)-2-(N-tert-
butylamino)-3′-[125I]-iodo-4′-azidopropiophenone (SADU-3-72). Based on inhibition of
[125I] SADU-3-72 binding, SADU-3-72 binds with high affinity (IC50= 0.8 μM) to the Torpedo
nAChR in the resting (closed channel) state and in the agonist-induced desensitized state …
noncompetitive antagonist of nicotinic acetylcholine receptors (nAChRs). To identify its
binding site (s) in nAChRs, we developed a photoreactive bupropion analogue,(±)-2-(N-tert-
butylamino)-3′-[125I]-iodo-4′-azidopropiophenone (SADU-3-72). Based on inhibition of
[125I] SADU-3-72 binding, SADU-3-72 binds with high affinity (IC50= 0.8 μM) to the Torpedo
nAChR in the resting (closed channel) state and in the agonist-induced desensitized state …
[引用][C] Bupropion Binds to Two Sites in the Torpedo Nicotinic Acetylcholine Receptor Transmembrane Domain: A Photoaffinity Labeling Study with the Bupropion …
P Akash, S Brandon, A Shaili, J Michaela - 2012
以上显示的是最相近的搜索结果。 查看全部搜索结果