Neurotransmitter receptors & pharmacology Flashcards
Name 2 cholinergic receptors
Nicotinic
Muscarinic
Where do M2 receptors appear?
Parasympathetic postganglionic
What are some effects of M2 activation?
Vasodilation (flush) DIlation of pupil Decrease salivation Decreased perspiration Hallucinations
Acetylcholine is a physiological agonist. Is it selective or non-selective?
Non-selective
Name a nicotinic ganglionic antagonist (Ng)?
Hexamethonium
Name a nicotinic neuromuscular depolarizing blocker (Nm)
Decamethonium
Succinylcholine
What is the lock and key model of neurotransmitters?
Agonist binding to receptor causes conformational shift of receptor
How do antagonists bind to inhibit receptors?
Antagonists have similar structure to agonist but do not induce necessary conformation changes
What receptor is Gs/cAMP linked to?
B-adrenergic
What receptor is Gi/cAMP linked to?
M2 Muscarinic
What receptor is Gq/IP3/DAG linked to?
alpha1-adrenergic
What receptor is Gq/NO/cGMP linked to?
H1 histaminergic
Which receptors are linked to tyorsine kinase receptors?
Dopamine, NMDA
What occurs when there are multiple receptor sites at a single synpase during polarized conditions?
Presynaptic M2 receptors have a high affinity for Ach and occupied receptors are linked to synaptic vesicles to reduce exocytosis. Postaynaptic nicotinic receptors are unoccupied and closed
What occurs when there are multiple receptor sites at a single synapse during depolarized conditions?
Presynaptic M2 receptors have a low affinity for Ach. Ach dissociates from vesicles. VOltage-gated Ca2+ channels open and allow vesicle fusion & exocytosis
What occurs when there are multiple receptor sites at a single synapse during repolariztion?
Presynaptic M2 receptors and postsynaptic nicotinic receptors have high affinity for Ach. Occupied presynaptic receptors are linked to vesicles to reduce exocyotsis
What is the effect of Beta1 on heart rate?
Increase
What is the effect of Beta1 on heart contractility?
Increase
What is the effect of Beta2 on bronchi?
Dilate
What receptor does Atenolol act on?
Beta1 blocker
What receptor does Propanolol act on?
Beta1 agonist, Beta2 blocker
What receptor does prazosin act on?
Alpha1 blocker
What receptor does phenylephrine act on?
Alpha1 agonist
What receptor does Dobutamine act on?
Beta1 agonist
What receptor does Albuterol act on?
beta2 agonist
What receptor does norepinephrine act on?
Alpha1, Alpha2, Beta1 agonist
How to association constant?
Kd = Koff / Kon
How to calclate affinity?
affinity = association rate (Kon) * [ligand]
What is the neurotransmitter for the cholinergic receptor? Where is it found?
Acetylcholine
Neromuscular junctions
What is the neurotransmitter for biogenic amines? Where is it found?
Norepinephrine
sympathetic postganglion
What is the neurotransmitter for amino acid receptors? WHere is it found?
Glutamate, GABA
CNS
What is the neurotransmitter for peptide receptors? where is it found?
Substance P
CNS
What is the neurotransmitter for purine receptors? where is it found?
ATP
CNS
What are metabotropic receptors?
G-protein linked & tyrosine kinase linked receptors