l2 SAQ Inverse Agonists

The dose of a drug that produces a given effect in a population.

Sleep/no sleep, pain/no pain.

Effective Dose 50.

<p>Measures of potency and efficacy.</p> Signup and view all the answers

<p>By analyzing measures of potency and efficacy.</p> Signup and view all the answers

<p>As the drug concentration increases, the contraction traces also increase.</p> Signup and view all the answers

<p>As the drug concentration increases, the response in mm also increases.</p> Signup and view all the answers

<p>As the drug concentration increases, the % maximal response also increases.</p> Signup and view all the answers

<p>The EC50 value is 2.88 x 10-8 M.</p> Signup and view all the answers

<p>Potency refers to the concentration or dose required to produce a certain response, while efficacy refers to the maximum response that can be achieved.</p> Signup and view all the answers

<p>Agonists and Antagonists</p> Signup and view all the answers

<p>Receptor occupancy, Names, Receptors, Ion channels, Enzymes, Transporters, Full, Partial, Inverse, Biased, Competitive, Noncompetitive, Kd and Bmax, Potency, Dose response, EC50 and Emax, Efficacy, Agonists and antagonists</p> Signup and view all the answers

<p>Agonists: Drugs that bind to a receptor and cause an effect. Antagonists: Drugs that prevent the agonist-induced activation of the receptor.</p> Signup and view all the answers

<p>Partial agonists are drugs that do not fully activate a receptor, even at high doses.</p> Signup and view all the answers

<p>Inverse agonists: Drugs that bind to a receptor and cause the opposite effect of an agonist. Biased agonists: Drugs that selectively activate specific signaling pathways of a receptor.</p> Signup and view all the answers

<p>Competitive antagonists and non-competitive antagonists.</p> Signup and view all the answers

<p>Antagonist competes with agonist for receptor binding sites.</p> Signup and view all the answers

<p>Reversible competitive antagonism can be out-competed by adding extra agonist, while irreversible competitive antagonism stays bound and cannot be displaced.</p> Signup and view all the answers

<p>Non-competitive antagonism blocks at some point other than the receptor binding site, while competitive antagonism occurs at the same binding site as the endogenous ligand.</p> Signup and view all the answers

<ol> <li>The partial agonist is a good fit for the receptor binding site, but less able to promote the receptor conformational change leading to transduction. 2. The receptor may be in an active and inactive state, and that partial agonists form complexes with both states, whereas full agonists preferentially bind the active form.</li> </ol> Signup and view all the answers

<p>An inverse agonist is a ligand that binds to receptors and reduces the fraction of them in an active conformation, producing biological effects opposite to those produced by an agonist.</p> Signup and view all the answers

<p>An inverse agonist reduces the activation of a constitutively active receptor, while a competitive antagonist simply blocks the receptor without further inactivating receptor activity beyond its baseline value.</p> Signup and view all the answers

<p>The classical idea of an agonist is that it activates the whole repertoire of signals following activation.</p> Signup and view all the answers

<p>The revised theory suggests that receptor coupling results in myriad configurations (states), and that a certain configuration may elicit a specific subset of signaling response.</p> Signup and view all the answers

<p>The key concepts include: 1. Receptor activation can be described with mathematical models. 2. Receptor activation is not linear with ligand binding. 3. Usually relatively low receptor occupancy is required to elicit relatively high response. 4. Receptor-mediated activity is affected by the inherent properties of the ligand, the number of receptors present, and the characteristics of the signal transduction machinery.</p> Signup and view all the answers