Acetylcholine
Acetylcholine is an organic cation that acts as a neurotransmitter in many organisms, including humans. Acetylcholine is also the principal neurotransmitter in all autonomic ganglia. In cardiac tissue acetylcholine neurotransmission has an inhibitory effect, which lowers heart rate. However, acetylcholine also behaves as an excitatory neurotransmitter at neuromuscular junctions in skeletal muscle.
Chemistry
It is an ester of acetic acid and choline. The molecule is a polyatomic cation, meaning that it is a positive ion comprising of more than one atom.
The Cholinergic System
Acetylcholine acts as a neurotransmitter in both the peripheral nervous system (PNS) and central nervous system (CNS). Acetylcholine is also one of many neurotransmitters in the autonomic nervous system (ANS) and is the only neurotransmitter used in the motor division of the somatic nervous system (sensory neurons use glutamate and various peptides at their synapses).
Drugs targeting the cholinergic system
- Agonists
An acetylcholine receptor agonist works by increasing the level of receptor activation, either directly or indirectly. Direct agonists work by imitating the neurotransmitter; an example of this is the stimulant drug nicotine. Indirect agonists most often work by inhibiting the enzyme acetylcholinesterase; this enzyme breaks down acetylcholine, and therefore inhibition of it increases activation of cholinergic receptors. The stimulant drug caffeine is an indirect agonist, as is THC. These work by blocking Acetylcholine esterate, which is an enzyme that breaks down acetylcholine, leading to an increased build up over time.
- Antagonists
An acetylcholine receptor antagonist works by attaching to acetylcholine receptors to prevent agonists binding. The deliriant drugs atropine, scopolamine and DPH all act as antagonists upon muscarinic receptors, as does the deadly neurotoxin BZ.