scholarly journals An Activity-Dependent Retrograde Signal Induces the Expression of the High-Affinity Choline Transporter in Cholinergic Neurons

Neuron ◽  
2009 ◽  
Vol 61 (2) ◽  
pp. 272-286 ◽  
Author(s):  
Arjun Krishnaswamy ◽  
Ellis Cooper
Keyword(s):  
Cholinergic Neurons ◽  
Choline Transporter ◽  
High Affinity ◽  
Retrograde Signal ◽  
Activity Dependent ◽  
High Affinity Choline Transporter

scholarly journals Syntheses and In-vitro Evaluation of Tetrahydroaminoacridine (THA) Based Analogues as High Affinity Choline Transporter (HAChT) Imaging Probe

2016 ◽  
Vol 17 (2) ◽  
pp. 97-102
Author(s):  
Mohammad Anwar Ul Azim ◽  
Takashi Kozaka ◽  
Izumi Uno ◽  
Daisuke Miwa ◽  
Yoji Kitamura ◽  
...  
Keyword(s):  
Binding Assay ◽  
Research Work ◽  
Cholinergic Neurons ◽  
Choline Uptake ◽  
Choline Transporter ◽  
High Affinity ◽  
20 Nm ◽  
High Affinity Choline Transporter

Introduction: In cholinergic neurons, high affinity choline uptake (HACU) by the high affinity choline transporter (HAChT) is a rate-limiting and regulatory step for the synthesis of Acetylcholine (Ach).Thus, HAChT appear to be a relatively specific presynaptic marker for cholinergic neurons in Alzheimer’s disease.Objectives: The principle objective of the study is to check the affinity of tetrahydroaminoacridine (THA) derivatives for HAChT. Another objective of the research work is to clarify whether the hemicholinium-3 (ChT inhibitor) and HACU enhancer molecules share the same binding sites or not.Materials and Methods: The inhibition activities of tacrine, the 2,3-dimethylfuran derivative of tacrine (DMTA) and their corresponding 2-oxo-1-pyrrolidineacetyl derivatives, namely PTAA and MKC-231 were measured by displacement of a typical HAChT antagonist [3H]HC-3 in rat cerebral membrane. The percentage of inhibition against the binding of [3H]HC-3 to HAChT were calculated using GraphPad Prism v4 software.Results: Hemicholinium-3 showed affinity for HAChT (IC50 = 20 nM) in the in vitro binding assay. A very insignificant inhibition activity (IC50 = 1000 nM) of Tacrine was revealed. The newly synthesized tacrine derivatives, DMTA and PTAA did not show any affinity for HAChT. Although MKC-231 was reported to enhance cholinergic activity at synaptic terminals, it did not show any affinity for the HAChT in [3H]HC-3 binding assay.Conclusion: In vitro [3H]HC-3 binding assay revealed no affinity of MKC-231, tacrine and its corresponding2-oxo-1-pyrrolidineacetate derivative towards HAChT. So, it is worthy to develop radiolabeled HC-3 derivatives with high affinity for HAChT, which can diffuse the BBB, to enable the in vivo investigation of HACU system.Bangladesh J. Nuclear Med. 17(2): 97-102, July 2014

Localisation of the high-affinity choline transporter-1 in the rat skeletal motor unit

2002 ◽  
Vol 307 (3) ◽  
pp. 275-280 ◽  
Author(s):  
Katrin Lips ◽  
Uwe Pfeil ◽  
Rainer Haberberger ◽  
Wolfgang Kummer
Keyword(s):  
Motor Unit ◽  
Choline Transporter ◽  
High Affinity ◽  
High Affinity Choline Transporter

scholarly journals Blockage of High-Affinity Choline Transporter Increases Visceral Hypersensitivity in Rats with Chronic Stress

2018 ◽  
Vol 2018 ◽  
pp. 1-8
Author(s):  
Chen Zhao ◽  
Mengjuan Lin ◽  
Yasi Pan ◽  
Baoping Yu
Keyword(s):  
Normal Saline ◽  
Specific Inhibitor ◽  
Visceral Hypersensitivity ◽  
Choline Uptake ◽  
Uptake System ◽  
Threshold Intensity ◽  
Choline Transporter ◽  
High Affinity ◽  
Acetylcholine Concentration ◽  
High Affinity Choline Transporter

Background. Visceral hypersensitivity is a common feature of irritable bowel syndrome. Cholinergic system involves in the development of visceral hypersensitivity, and high-affinity choline transporter (CHT1) is of crucial importance in choline uptake system. However, involvement of CHT1 in visceral hypersensitivity remains unknown. The research aimed to study the CHT1 expression in dorsal root ganglions (DRGs) and the role of CHT1 in visceral hypersensitivity. Methods. Repetitive water avoidance stress (WAS) was used to induce visceral hypersensitivity in rats. Colorectal distension (CRD) was determined, and the abdominal withdrawal reflex (AWR) and threshold intensity data were recorded to measure the visceral sensitivity. After intraperitoneal injection of hemicholinium-3 (HC-3), the specific inhibitor of CHT1, CRD data were also recorded. The CHT1 expression of DRGs was investigated by Western blotting, immunohistochemistry, and quantitative RT-PCR. Acetylcholine levels in the DRGs were detected by the assay kit. Results. Repetitive WAS increased the AWR score of CRD at high distension pressure and decreased the mean threshold of rats. The CHT1 expression and acetylcholine concentration of DRG were significantly increased in WAS rats. After the administration of HC-3, the AWR score in WAS group was significantly increased at higher distension pressure while the threshold intensity was significantly reduced compared to the normal saline group. Acetylcholine concentration was significantly lower than the normal saline rats. Conclusion. Our research firstly reports that CHT1 is overexpressed in noninflammatory visceral hypersensitivity, and blockage of CHT1 can enhance the visceral hypersensitivity. CHT1 may play an inhibitory role in visceral hypersensitivity.

scholarly journals Constitutive high-affinity choline transporter endocytosis is determined by a carboxyl-terminal tail dileucine motif

2005 ◽  
Vol 94 (1) ◽  
pp. 86-96 ◽  
Author(s):  
Fabiola M. Ribeiro ◽  
Stefanie A. G. Black ◽  
Sean P. Cregan ◽  
Vania F. Prado ◽  
Marco A. M. Prado ◽  
...  
Keyword(s):  
Choline Transporter ◽  
High Affinity ◽  
Dileucine Motif ◽  
Carboxyl Terminal ◽  
High Affinity Choline Transporter
Sign in / Sign up

Export Citation Format

Share Document