Exploring the Relationship between Nicotinic Acetylcholine Receptor Ligand Size, Efficiency, Efficacy, and C-Loop Opening

2017 ◽  
Vol 57 (8) ◽  
pp. 1947-1956 ◽  
Author(s):  
Qianyun Ma ◽  
Han-Shen Tae ◽  
Guanzhao Wu ◽  
Tao Jiang ◽  
Rilei Yu
Keyword(s):  
Acetylcholine Receptor ◽  
Nicotinic Acetylcholine Receptor ◽  
Receptor Ligand ◽  
Nicotinic Acetylcholine ◽  
The Relationship ◽  
Size Efficiency

scholarly journals Firing responses mediated via distinct nicotinic acetylcholine receptor subtypes in rat prepositus hypoglossi nuclei neurons

2018 ◽  
Vol 120 (4) ◽  
pp. 1525-1533
Author(s):  
Yue Zhang ◽  
Yuchio Yanagawa ◽  
Yasuhiko Saito
Keyword(s):  
Acetylcholine Receptor ◽  
Nicotinic Acetylcholine Receptor ◽  
Firing Frequency ◽  
Membrane Properties ◽  
Receptor Subtypes ◽  
Nicotinic Acetylcholine ◽  
Firing Patterns ◽  
Prepositus Hypoglossi ◽  
Specific Antagonist ◽  
The Relationship

We previously reported that cholinergic current responses mediated via nicotinic acetylcholine (ACh) receptors (nAChRs) in the prepositus hypoglossi nucleus (PHN), which participates in gaze control, can be classified into distinct types based on different kinetics and are mainly composed of α7- and/or non-α7-subtypes: fast (F)-, slow (S)-, and fast and slow (FS)-type currents. In this study, to clarify how each current type is related to neuronal activities, we investigated the relationship between the current types and the membrane properties and the firing responses that were induced by each current type. The proportion of the current types differed in neurons that exhibited different afterhyperpolarization (AHP) profiles and firing patterns, suggesting that PHN neurons show a preference for specific current types dependent on the membrane properties. In response to ACh, F-type neurons showed either one action potential (AP) or multiple APs with a short firing duration, and S-type neurons showed multiple APs with a long firing duration. The firing frequency of F-type neurons was significantly higher than that of S-type and FS-type neurons. An α7-subtype-specific antagonist abolished the firing responses of F-type neurons and reduced the responses of FS-type neurons but had little effect on the responses of S-type neurons, which were reduced by a non-α7-subtype-specific antagonist. These results suggest that the different properties of the current types and the distinct expression of the nAChR subtypes in PHN neurons with different membrane properties produce unique firing responses via the activation of nAChRs. NEW & NOTEWORTHY Prepositus hypoglossi nucleus (PHN) neurons show distinct nicotinic acetylcholine receptor (nAChR)-mediated current responses. The proportion of the current types differed in the neurons that exhibited different afterhyperpolarization profiles and firing patterns. The nAChR-mediated currents with different kinetics induced firing responses of the neurons that were distinct in the firing frequency and duration. These results suggest that the different properties of the current types in PHN neurons with different membrane properties produce unique firing responses via the activation of nAChRs.

Influence of acetylcholine levels on the binding of a SPECT nicotinic acetylcholine receptor ligand [123I]5-I-A-85380

Synapse ◽  
2003 ◽  
Vol 48 (3) ◽  
pp. 116-122 ◽  
Author(s):  
Masahiro Fujita ◽  
Mohammed S. Al-Tikriti ◽  
Gilles Tamagnan ◽  
Sami S. Zoghbi ◽  
Ali Bozkurt ◽  
...  
Keyword(s):  
Acetylcholine Receptor ◽  
Nicotinic Acetylcholine Receptor ◽  
Receptor Ligand ◽  
Nicotinic Acetylcholine

Expression of the endogenous, nicotinic acetylcholine receptor ligand, SLURP-1, in human colon cancer

2008 ◽  
Vol 28 (4) ◽  
pp. 109-116 ◽  
Author(s):  
A. Pettersson ◽  
S. Nordlander ◽  
G. Nylund ◽  
A. Khorram-Manesh ◽  
S. Nordgren ◽  
...  
Keyword(s):  
Colon Cancer ◽  
Acetylcholine Receptor ◽  
Nicotinic Acetylcholine Receptor ◽  
Human Colon ◽  
Human Colon Cancer ◽  
Receptor Ligand ◽  
Nicotinic Acetylcholine

Primary sensory neuronal expression of SLURP-1, an endogenous nicotinic acetylcholine receptor ligand

2009 ◽  
Vol 64 (4) ◽  
pp. 403-412 ◽  
Author(s):  
Yasuhiro Moriwaki ◽  
Yosuke Watanabe ◽  
Tomoe Shinagawa ◽  
Miho Kai ◽  
Mai Miyazawa ◽  
...  
Keyword(s):  
Acetylcholine Receptor ◽  
Nicotinic Acetylcholine Receptor ◽  
Receptor Ligand ◽  
Nicotinic Acetylcholine ◽  
Neuronal Expression

A-85380 [3-(2(S)-azetidinylmethoxy) pyridine]: In Vitro pharmacological properties of a novel, high affinity α4β2 nicotinic acetylcholine receptor ligand

1996 ◽  
Vol 35 (6) ◽  
pp. 725-734 ◽  
Author(s):  
James P. Sullivan ◽  
Diana Donnelly-Roberts ◽  
Clark A. Briggs ◽  
David J. Anderson ◽  
Murali Gopalakrishnan ◽  
...  
Keyword(s):  
Acetylcholine Receptor ◽  
Nicotinic Acetylcholine Receptor ◽  
Pharmacological Properties ◽  
Receptor Ligand ◽  
Nicotinic Acetylcholine ◽  
High Affinity
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