Vesamicol: Difference between revisions

Latest revision as of 19:56, 26 April 2025

A drug that inhibits acetylcholine storage in synaptic vesicles

Vesamicol is a pharmacological agent that acts as an inhibitor of the vesicular acetylcholine transporter (VAChT). This compound is primarily used in research settings to study the cholinergic system and its role in various physiological and pathological processes.

Mechanism of Action[edit]

Vesamicol functions by inhibiting the VAChT, which is responsible for transporting acetylcholine into synaptic vesicles within cholinergic neurons. By blocking this transporter, vesamicol effectively reduces the storage of acetylcholine in vesicles, leading to decreased release of this neurotransmitter into the synaptic cleft. This action results in diminished cholinergic transmission, which can be useful for studying the effects of reduced acetylcholine activity in the nervous system.

Pharmacological Effects[edit]

The inhibition of acetylcholine storage by vesamicol can lead to a variety of effects depending on the system being studied. In the central nervous system, reduced cholinergic activity can affect processes such as learning, memory, and motor control. In the peripheral nervous system, vesamicol can influence autonomic functions and neuromuscular transmission.

Research Applications[edit]

Vesamicol is primarily used in experimental research to investigate the role of acetylcholine in various biological systems. It is particularly valuable in studies of neurodegenerative diseases such as Alzheimer's disease, where cholinergic dysfunction is a hallmark. By modulating acetylcholine levels, researchers can better understand the contributions of cholinergic pathways to disease progression and symptomatology.

Chemical Properties[edit]

Vesamicol is a piperidine derivative with the chemical formula C₁₇H₂₅NO. It is characterized by a cyclohexanol group linked to a phenylpiperidine moiety. The compound is typically synthesized in laboratory settings for research purposes.

Safety and Handling[edit]

As with many research chemicals, vesamicol should be handled with care in a controlled laboratory environment. Appropriate safety measures, including the use of personal protective equipment, should be employed to prevent exposure.

Related Pages[edit]

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-[[File:Vesamicol.png|Vesamicol|thumb]]
+{{Short description|A drug that inhibits acetylcholine storage in synaptic vesicles}}
-'''Vesamicol''' is a compound of notable interest in neuropharmacology due to its unique action on [[presynaptic]] terminals, where it modulates the release of the neurotransmitter [[acetylcholine]] (ACh). Its peculiar mechanism offers insights into the regulation of neurotransmitter release and has potential therapeutic implications.<ref name="pmid8619013">{{cite journal |author=Salin-Pascual RJ, Jimenez-Anguiano A |title=Vesamicol, an acetylcholine uptake blocker in presynaptic vesicles, suppresses rapid eye movement (REM) sleep in the rat |journal=Psychopharmacology |volume=121 |issue=4 |pages=485–7 |date=October 1995 |pmid=8619013 |doi= 10.1007/BF02246498|url=}}</ref>
+'''Vesamicol''' is a pharmacological agent that acts as an inhibitor of the vesicular acetylcholine transporter (VAChT). This compound is primarily used in research settings to study the [[cholinergic system]] and its role in various physiological and pathological processes.
-=== Mechanism of Action ===
+==Mechanism of Action==
+Vesamicol functions by inhibiting the VAChT, which is responsible for transporting [[acetylcholine]] into synaptic vesicles within [[cholinergic neurons]]. By blocking this transporter, vesamicol effectively reduces the storage of acetylcholine in vesicles, leading to decreased release of this neurotransmitter into the synaptic cleft. This action results in diminished cholinergic transmission, which can be useful for studying the effects of reduced acetylcholine activity in the [[nervous system]].
-While many drugs target postsynaptic receptors to modulate neurotransmitter signaling, vesamicol is unique in that it acts presynaptically. Its primary mechanism can be elaborated through the following points:
+==Pharmacological Effects==
+The inhibition of acetylcholine storage by vesamicol can lead to a variety of effects depending on the system being studied. In the [[central nervous system]], reduced cholinergic activity can affect processes such as learning, memory, and [[motor control]]. In the [[peripheral nervous system]], vesamicol can influence [[autonomic functions]] and [[neuromuscular transmission]].
-'''Inhibition of VAChT''': Vesamicol is a non-competitive and reversible antagonist of the [[Vesicular acetylcholine transporter|VAChT]], an essential intracellular transporter. VAChT facilitates the transport of newly synthesized ACh from the cytoplasm into secretory vesicles located within the presynaptic nerve terminal.
+==Research Applications==
+Vesamicol is primarily used in experimental research to investigate the role of acetylcholine in various biological systems. It is particularly valuable in studies of [[neurodegenerative diseases]] such as [[Alzheimer's disease]], where cholinergic dysfunction is a hallmark. By modulating acetylcholine levels, researchers can better understand the contributions of cholinergic pathways to disease progression and symptomatology.
-'''Transport and Proton Gradient''': The loading of ACh into secretory vesicles by VAChT is driven by a proton gradient, which is established between cell organelles and the cytoplasm. Vesamicol's action interferes with this gradient, thereby blocking the uptake process.
+==Chemical Properties==
+Vesamicol is a piperidine derivative with the chemical formula C<sub>17</sub>H<sub>25</sub>NO. It is characterized by a cyclohexanol group linked to a phenylpiperidine moiety. The compound is typically synthesized in laboratory settings for research purposes.
-'''Consequence of ACh Loading Blockade''': When vesamicol inhibits the uptake of ACh into the vesicles, these vesicles essentially become "empty". When such vesicles fuse with the neuron membranes in response to a neuronal action potential, the release of ACh into the synaptic cleft is reduced, leading to decreased cholinergic signaling.
+==Safety and Handling==
+As with many research chemicals, vesamicol should be handled with care in a controlled laboratory environment. Appropriate safety measures, including the use of personal protective equipment, should be employed to prevent exposure.
-=== Pharmacological Classification ===
+==Related Pages==
+* [[Acetylcholine]]
-Vesamicol can be characterized as a cholinergic [[physiological antagonist]]. This is because, while it reduces the effective activity of cholinergic [[neuron]]s, it does not directly antagonize or block postsynaptic ACh receptors. Instead, its mode of action is upstream of the receptor interaction, emphasizing its presynaptic site of action.
+* [[Cholinergic system]]
+* [[Neurotransmitter]]
-=== Research and Therapeutic Implications ===
+* [[Synaptic vesicle]]
+* [[Alzheimer's disease]]
-The ability of vesamicol to modulate ACh release can have potential therapeutic applications, especially in disorders characterized by abnormal cholinergic neurotransmission. Furthermore, the compound provides an invaluable tool for neuroscientists to study and dissect the processes of neurotransmitter release and storage at a molecular level.
+[[Category:Pharmacology]]
+[[Category:Neurotransmitter inhibitors]]
-== Conclusion ==
+[[Category:Research chemicals]]
-Vesamicol's unique mechanism of action has piqued the interest of the scientific community, offering profound insights into presynaptic regulation of neurotransmission. Its potential therapeutic applications, though still under investigation, could open new avenues in the treatment of neurological and psychiatric disorders.
+{{nt}}
-== References ==
-<ref name="pmid8619013"></ref>
-{{Cholinergics}}
-{{pharmacology-stub}}
-[[Category:Piperidines]]
-[[Category:Alcohols]]