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Neurotransmitters Notes

Pharmacology Notes > BIOL10832 Excitable Cells Notes

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Excitable Cells - Lecture 9 (27/02/2018)

Neurotransmitters

Receptors

Receptors are membrane-spanning proteins comprised of a number of subunits.

When ligand binding occurs, this induces a conformational change in the receptor, as shown in the Lock-and-Key Hypothesis.

Agonists and Antagonists

Agonists and Antagonists are used as tools for understanding synaptic functions and candidates for drug discovery.
An Allosteric modulator binds to the receptor at a different site to alter how the receptor binds to the ligand. Nicotinic Acetylcholine Receptor - Ligand-gated ion channel.

The Nicotonic Acetylcholine receptor is a membranespanning protein made up of five subunits (2, , , , ),
which are arranged to form a pore.


2x ACh's bind to 2 subunits to open then channel.
Na+ (and K+) flow down their electrochemical gradient causing the membrane to depolarise (epsp).

Neurotransmitters
Classical








Neuropeptides
Acetylcholine.
Dopamine.
Serotonin (5-hydroxytryptamine).
Adrenaline (epinephrine).
Noradrenaline (norepinephrine).
Histamine.
L-Glutamic acid.
γ-amino-butyric acid (GABA).





Substance P.
Endorphins.
Enkephalins.
Vasopressin.
Oxytocin.

Others



NO (Nitric Oxide).
Adenosine.
ATP.

Identification of Neurotransmitter
A Neurotransmitter candidate:




Must be synthesised by the neuron.
Must be present in the synaptic terminal at sufficient concentrations.
Must be released on presynaptic stimulation.
Exogenous application to postsynaptic cell must evoke a response.
A Mechanism must exist for its removal from the synaptic cleft.

Diversity of Neurotransmitters
There are 3 main classes of Neurotransmitter:

Amino acids: (eg: glutamate; glycine; -aminobutyric acid
(GABA), synaptic vesicles, 50 nm)

Amines: (eg: acetylcholine (ACh); dopamine; noradrenaline;
serotonin (5-HT), synaptic vesicles)

Peptides: (eg: enkephalin; substance P; neuropeptide Y)
(dense-core secretory granules, 100 nm)

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