U2L08 Responses to antagonists
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38 terms
Terms | Definitions |
|---|---|
 competitive (reversible), competitive (irreversible) and non-competitive | What are the three types of antagonist? |
| affinity | Occupation is governed by what property of the receptor-drug interaction? |
| efficacy | Activation is governed by what property of the receptor-drug interaction? |
| atropa belladonna | What plant is atropine derived from? |
| selective muscarinic antagonist | What is atropine? |
| 10^-8 mol/L | At approximately what concentration is atropine active? |
| pupils dilate, dry mouth, hallucinations | What are the effects of atropine? |
| dose ratio | What does DR stand for in the antagonist calculations? |
| how much more is needed in presence of antagonist to get same response | What does DR represent? |
| log(DR - 1) = log XB - log KB | What is the equation for the Schild plot? |
| 1 | If competitive antagonism, slope of the Schild plot will be... |
| KB | If competitive antagonism, what will the x-intercept of the Schild plot be? |
| log xB | What is on the x-axis of the Schild plot? |
| log(DR - 1) | What is on the y-axis of the Schild plot? |
| -log xB when DR = 2, or x intercept on Schild plot | What equation is used to calculate pA2? |
| shifts to right | How does a competitive antagonist change the dose-response curve for an agonist? |
| it doesn't | How does a competitive antagonist change the maximum response? |
| define antagonist drug, receptor classification | What purposes is the pA2 widely used for? |
| independent of it | What relationship does the pA2 have to the agonist? |
| antagonist and receptor | What does the pA2 depend on? |
| pA2 | The negative logarithm to base 10 of the molar concentration to reduce the effect of a dose of agonist to that of half the dose |
| agonists and antagonists | Partial agonists have properties of both... |
| atropine | An antagonist of muscarinic cholinergic receptors |
| hexamethonium, decamethonium, tubocurarine | 3 antagonists of nicotinic cholinergic receptors |
| ganglionic | Which nicotinic cholinergic receptors does hexamethonium act on? |
| neuromuscular junction | Which nicotinic cholinergic receptors do decamethonium and tubocurarine act on? |
| depolarising block | What is unusual about the action of decamethonium? |
| mepyramine | An antagonist of histamine H1 receptors |
| propranolol | An antagonist of β-adrenoceptors |
| receptor reserve | The concept that the pool of receptors is larger than needed for full response |
| Scatchard plot | What plot is used to calculate the total number of binding sites? |
| Bmax | The total number of binding sites is known as... |
| [bound] | What is on the x-axis of the Scatchard plot? |
| [bound]/[free] | What is on the y-axis of the Scatchard plot? |
| -1/KD | What does the slope of the Scatchard plot represent? |
| Bmax (total binding sites) | What does the x-intercept of the Scatchard plot represent? |
| radioactive labelling | How do you measure extremely low concentrations as seen in the Scatchard plot? |
| elicit a response | Antagonists, by themselves, do not... |
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