Lecture 3.2 Flashcards
(37 cards)
What is pharmacological subtyping?
Organising the different variations of a receptor type by their pharmacological characteristics.
What are receptor superfamilies?
Grouping receptors according to their specific structures and functional features.
What is a modulatory site?
Additional receptors that modulate the activity of the primary receptor.
What is an agonist?
A chemical that stimulates/activates a receptor, increasing the receptor output beyond baseline levels.
What is an inverse agonist?
A chemical that activates a receptor, reducing receptor output below baseline levels.
What is a partial agonist?
A chemical that exerts a similar, but weaker, effect to an agonist or inverse agonist.
What is an antagonist?
A chemical that reduces the effect of an agonist or inverse agonist (if no agonist or inverse agonist is present, then it has no effect).
What does endogenous mean?
Produced by the body.
What does exogenous mean?
Produced outside of the body.
What is constitutive receptor activity?
Receptors causing a response in the absence of a neurotransmitter.
What is allosteric modulation?
Where a molecule binds to a receptor located away from the orthosteric site, but can still influence the main neurotransmitter receptor function.
What is a primary neurotransmitter receptor site?
Influences the receptor in its usual manner (e.g., open an ion channel).
What is a secondary neurotransmitter receptor site?
Can indirectly influence the receptor only when the primary neurotransmitter has bound with the primary receptor site (it cannot act on the receptor alone).
What is positive allosteric modulation?
Increases the functional outcome of the primary or ‘gatekeeper’ receptor.
What is negative allosteric modulation?
Reduces the functional outcome of the primary or ‘gatekeeper’ receptor.
What is co-transmission?
Where a neuron can package multiple neurotransmitters into different vesicles and release them simultaneously.
What can receptors be categorised based on?
Their location, gene/chromosome location, and stimulatory or inhibitory functions.
Neurotransmitters can act on what receptor types?
Multiple receptor types.
What are examples of pharmacological subtyping?
Serotonergic and dopaminergic receptors.
What are 2 receptor superfamilies? What is the inclusion criteria and what are they associated with?
○ G-Protein Linked Superfamily.
§ Considered the largest superfamily of receptors.
§ Includes receptors that:
□ Have 7 transmembrane regions.
□ Use a G-Protein.
□ Use a second messenger system.
§ Note that different receptors can use different neurotransmitters but still be a member of the superfamily.
§ Associated with slow onset modulatory signaling.
○ Ligand-Gated Ion Channel Superfamily.
§ Includes receptors that have 5 identical subunits, each with (all have):
□ 4 transmembrane regions.
□ The same receptor.
□ Modulatory sites.
□ Cylindrical in shape with ion channel in the centre.
□ Associated with fast onset signaling (excitation / inhibition).
What can agonists be?
Either endogenous or exogenous.
What are the 2 categories of exogenous?
Naturally derived and manufactured.
Are receptors unable to cause a response unless they are occupied by a neurotransmitter? How does this relate to constitutive receptor activity?
No, receptors can cause a baseline response without a neurotransmitter; constitutive receptor activity is this baseline activity that can be altered by neurotransmitters.
What’s first on the agonist spectrum?
Agonist
