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Excitable Cells - Lecture 9 (27/02/2018)
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).
γ-amino-butyric acid (GABA).
NO (Nitric Oxide).
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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