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37 Cards in this Set
- Front
- Back
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Agonist |
A drug or naturally occurring substance in the body that directly causes a measurable response |
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Affinity |
How well an agonist binds to its receptor |
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Efficacy |
Drugs ability to effectively activate the receptor once bound to it |
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How can an agonist response be shown? |
Sigmoidal curve/ s shaped curve |
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What is an EC 50 |
Mid-point of s shaped curve, the effective concentration for 50% of the response |
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Antagonist |
A substance which interferes with or inhibits the physiological action of an agonist |
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What are the three types of antagonist? |
Pharmacological, chemical and physiological |
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Difference between competitive and non-competitive antagonism? |
Competitive - agonist and antagonists are competing for the same receptor Non-competitive - antagonists which act at sites other than the agonist binding site |
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What are the two forms of drug toxicity? |
Latrogenicity - capacity to produce disease from the side effects Teratogenicity - the capacity to produce abnormalities of an unborn child |
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How are drugs studied? |
In Vivo, in vitro and high throughput screening |
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The six steps in chemical signalling? |
Agonist synthesis Agonist release Transport Detection by target cell Physiological response Signal inactivation |
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How many transmembrane domains does a GPCR have? |
7 |
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What is the function of a G protein? |
To act as a molecular switch |
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Subunits with G proteins |
Alpha, beta and gamma |
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What enzyme does Gs regulate ? |
Adenylyl cyclase is stimulated |
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What enzyme does Gi regulate? |
Inhibits adenylyl cyclase |
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What enzyme does GQ regulate? |
Activates phospholipase C |
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What second messenger does adenylyl cyclase produce? |
Cyclic AMP |
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What second messenger does phospholipase C produce? |
IP3 and DAG from PIP 2 |
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What does cAMP do? |
It activates a target enzyme called cAMP-dependant protein kinase A |
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IP3 function |
IP3 binds to receptors on endoplasmic reticulum which releases intracellular stored calcium |
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DAG function |
Activates protein kinase C |
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What is salbutamol? |
It is a selective agonist at the beta 2 receptor that can be used to treat asthma |
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What has a similar structure to salbutamol? |
Adrenaline |
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Salbutamol mechanism of action |
Interacts with the Gs protein in order to activate adenylyl cyclase |
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What is hayfevers proper name? |
Allergic rhinitis |
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How is histamine released? |
It is released from IgE primed mast cells |
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Drug used for heart arrhythmia |
Beta blockers (beta 1 antagonists) |
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Drug used for stomach ulcers |
Histamine H2 receptor antagonist |
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What is Aspirin? |
Cyclo-oxygenase inhibitor (COX) also known as acetyl salicylic acid |
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What is PGE |
It is a prostaglandin which is involved in inflammation and is mediated by COX 2 |
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What is TXA2? |
It is a prostaglandin like product that is involved in platelet aggregation during clotting, mediated by COX 1 |
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What is serotonin's proper name? |
5- hydroxy tryptamine |
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What are the three neurotransmitters that regulate positive mood? |
Dopamine, norepinephrine and serotonin |
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Two types of drugs used to treat depression |
Selective serotonin reuptake inhibitors and norepinephrine-dopamine reuptake inhibitors |
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What is lidocaine? |
Lidocaine is a local anesthetics that selectively blocks sodium ion channels in depolarised or rapidly firing cells (axons) |
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Penicillin mechanism of action |
Kills bacteria through binding of the beta lactam ring which inhibits new cell wall formation |
