Vesicular acetylcholine transporter
Encyclopedia
The Vesicular acetylcholine transporter (VAChT) is a neurotransmitter transporter
which is responsible for loading acetylcholine
(ACh) into secretory organelles
in neurons making acetylcholine available for secretion.
imaging of the VAChT may provide insights into early diagnosis of Alzheimer's disease
.
Neurotransmitter transporter
Neurotransmitter transporters are a class of membrane transport proteins that span the cellular membranes of neurons. Their primary function is to carry neurotransmitters across these membranes and to direct their further transport to specific intracellular locations...
which is responsible for loading acetylcholine
Acetylcholine
The chemical compound acetylcholine is a neurotransmitter in both the peripheral nervous system and central nervous system in many organisms including humans...
(ACh) into secretory organelles
Synaptic vesicle
In a neuron, synaptic vesicles store various neurotransmitters that are released at the synapse. The release is regulated by a voltage-dependent calcium channel. Vesicles are essential for propagating nerve impulses between neurons and are constantly recreated by the cell...
in neurons making acetylcholine available for secretion.
Radiolabeled compounds
PETPositron emission tomography
Positron emission tomography is nuclear medicine imaging technique that produces a three-dimensional image or picture of functional processes in the body. The system detects pairs of gamma rays emitted indirectly by a positron-emitting radionuclide , which is introduced into the body on a...
imaging of the VAChT may provide insights into early diagnosis of Alzheimer's disease
Alzheimer's disease
Alzheimer's disease also known in medical literature as Alzheimer disease is the most common form of dementia. There is no cure for the disease, which worsens as it progresses, and eventually leads to death...
.
- (−)-trans-2-Hydroxy-3-(4-(4-
[ 18FFluorine-18Fluorine-18 is a fluorine radioisotope which is an important source of positrons. It has a mass of 18.0009380 u and its half-life is 109.771 minutes....] fluorobenzoyl)piperidino)tetralin; racemate: Ki = 2.70 nM for VAChT, 191 nM for σ1Sigma-1 receptorThe sigma-1 receptor is a chaperone protein at the endoplasmatic reticulum that modulates calcium signaling through the IP3 receptor. In humans, the sigma-1 receptor is encoded by the SIGMAR1 gene....
, and 251 nM for σ2