What defines an antagonist?
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An antagonist binds to a receptor and prevents a natural compound or drug from having an effect on the receptor.
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What defines an antagonist?
An antagonist binds to a receptor and prevents a natural compound or drug from having an effect on the receptor.
What is Inositol triphosphate (IP3) classified as?
A second messenger.
What does pharmacodynamics study?
The biochemical and physiological effects of drugs and their mechanisms of action.
What happens when a drug binds to a receptor?
It leads to a response.
What is pharmacological antagonism?
It involves substances that bind to receptors without activating them, preventing agonist binding.
What does the log [Dose] represent?
It represents the logarithmic scale of drug concentration in relation to response.
What characterizes non-competitive antagonism?
It binds to a different site on the receptor, exerting its effect through that site.
Are drugs completely specific in their actions?
No, no drugs are completely specific; their actions are dose dependent.
What aspect of signal-transduction pathways ensures that signals are directed to the correct target?
Signal specificity.
How do second messengers spread throughout the cell?
By diffusion.
What are drug receptors?
Protein molecules that recognize and respond to endogenous chemical signals.
What are the two types of drugs based on their interaction with receptors?
Agonists and antagonists.
What are the two functional domains of a receptor?
Ligand binding domain and message propagation domain (effector domain).
What does specificity in drug receptors refer to?
Individual classes of drugs bind only to certain targets, and individual targets recognize only certain classes of drugs.
What happens when a drug binds to a receptor?
It forms a drug-receptor (DR) complex, which can lead to a response if the drug is an agonist.
What is a key benefit of a signal-transduction pathway related to signal strength?
Signal amplification.
What is chemical antagonism?
Inactivating the agonist, such as an antacid reacting with acidic drugs.
What effect do antagonists produce?
Antagonists produce effects opposite to those of an agonist (negative efficacy).
How does competitive antagonism work?
It competes for the same binding site as the agonist.
What does the term 'affinity' refer to in pharmacology?
Affinity describes the ability or tendency of a drug to bind to its receptor to form a complex.
What are the four main types of protein targets for drug binding?
Receptors, enzymes, carrier molecules (transporters), and ion channels.
What is the most widely used second messenger that is a nucleotide?
Cyclic AMP (cAMP).
What is the efficacy of antagonists?
Antagonists have zero efficacy (intrinsic activity = 0), meaning no response is achieved by their binding.
What is E max?
The maximal effect a drug can produce.
Can competitive antagonism be reversible?
Yes, it can be either reversible or irreversible.
What type of receptors are intracellular and nuclear receptors?
They are protein targets for drug binding that act within the cell.
What is efficacy in pharmacology?
The maximal response a drug produces at full receptor occupation.
Which ion is commonly used as a second messenger?
Calcium ions (Ca2+).
What happens to a receptor in the presence of an agonist?
The receptor is functionally activated.
What are G protein-linked receptors?
A type of protein target for drug binding.
What are intracellular receptors?
Receptors located inside the cell that bind to ligands.
What does potency refer to in pharmacology?
The dose required to produce a certain response.
Where are drug receptors located?
On cell surfaces, within the cell membrane, and inside the cells.
What are the two types of binding to receptors?
Irreversible and reversible.
What type of receptors are linked to enzymes like tyrosine kinase?
Receptors linked to enzymes.
What theory explains the specificity of drug binding?
Key and Lock theory.
Name a second messenger that is a nucleotide and is involved in signal transduction.
Cyclic GMP (cGMP).
What is ED50?
The dose at which 50% of the maximal effect is observed.
What are ionotropic receptors?
Ligand-gated ion channel receptors.
What is the function of the ligand binding domain?
It is where the drug binds selectively via chemical bonds.
What are tyrosine kinase linked receptors?
A type of receptor that is a protein target for drug binding, involved in cellular signaling.
What is a full agonist?
A full agonist has affinity and efficacy, binds to a receptor, and elicits a maximal response (100%).
How is potency related to dose?
Potency is inversely related to the dose (drug concentration).
What is physiological antagonism?
When two substances act to oppose each other's effects.
What are G-protein coupled receptors?
A type of physiological receptor that interacts with G-proteins.
What does the message propagation domain do?
It transduces and propagates extracellular signals into an intracellular amplified response.
What is the outcome when an antagonist binds to a receptor?
It results in no response but prevents the response of the agonist.
What are second messengers?
Small, non-protein, water-soluble molecules or ions involved in signal transduction.
What characterizes a partial agonist?
A partial agonist has affinity and some efficacy, binds to a receptor, but never produces a maximal effect (< 100%).
What is the relationship between the number of receptors occupied and the magnitude of the response?
The magnitude of the response is proportional to the number (fraction) of receptors occupied by drug molecules.
How is the response to a drug characterized?
It is graded or dose-dependent.
What does pharmacokinetic antagonism involve?
Altering the way the body handles another drug, affecting absorption, metabolism, or excretion.
What role does Diacylglycerol (DAG) play in cellular signaling?
It acts as a second messenger.
What are the two main types of pharmacological antagonism?
Competitive and non-competitive antagonism.
What is the role of an antagonist in relation to cell surface receptors?
An antagonist binds to a receptor but does not activate it, preventing the response of an agonist.
What is the state of a receptor in the absence of an agonist?
The receptor is functionally silent.
What is an example of a non-competitive antagonist?
Channel blockers.
What is 'efficacy' in the context of drug-receptor interactions?
Efficacy (or intrinsic activity) is the ability of a bound drug to change the receptor in a way that produces an effect.
What are ligand-gated channels?
Channels that open in response to the binding of a ligand, serving as a protein target for drugs.
How does efficacy change with concentration?
Efficacy increases as a function of concentration.