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.
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Types of Antagonism

What defines an antagonist?

An antagonist binds to a receptor and prevents a natural compound or drug from having an effect on the receptor.

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Signal Transduction and Second Messengers

What is Inositol triphosphate (IP3) classified as?

A second messenger.

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Pharmacodynamics Overview

What does pharmacodynamics study?

The biochemical and physiological effects of drugs and their mechanisms of action.

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Drug-Receptor Interactions

What happens when a drug binds to a receptor?

It leads to a response.

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Types of Antagonism

What is pharmacological antagonism?

It involves substances that bind to receptors without activating them, preventing agonist binding.

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Affinity and Efficacy in Pharmacology

What does the log [Dose] represent?

It represents the logarithmic scale of drug concentration in relation to response.

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Types of Antagonism

What characterizes non-competitive antagonism?

It binds to a different site on the receptor, exerting its effect through that site.

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Affinity and Efficacy in Pharmacology

Are drugs completely specific in their actions?

No, no drugs are completely specific; their actions are dose dependent.

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Signal Transduction and Second Messengers

What aspect of signal-transduction pathways ensures that signals are directed to the correct target?

Signal specificity.

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Signal Transduction and Second Messengers

How do second messengers spread throughout the cell?

By diffusion.

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Drug Receptors and Their Functions

What are drug receptors?

Protein molecules that recognize and respond to endogenous chemical signals.

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Drug-Receptor Interactions

What are the two types of drugs based on their interaction with receptors?

Agonists and antagonists.

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Drug-Receptor Interactions

What are the two functional domains of a receptor?

Ligand binding domain and message propagation domain (effector domain).

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Specificity in Drug-Receptor Interactions

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.

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Drug-Receptor Interactions

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.

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Signal Transduction and Second Messengers

What is a key benefit of a signal-transduction pathway related to signal strength?

Signal amplification.

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Types of Antagonism

What is chemical antagonism?

Inactivating the agonist, such as an antacid reacting with acidic drugs.

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Types of Antagonism

What effect do antagonists produce?

Antagonists produce effects opposite to those of an agonist (negative efficacy).

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Types of Antagonism

How does competitive antagonism work?

It competes for the same binding site as the agonist.

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Affinity and Efficacy in Pharmacology

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.

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Protein Targets for Drug Binding

What are the four main types of protein targets for drug binding?

Receptors, enzymes, carrier molecules (transporters), and ion channels.

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Signal Transduction and Second Messengers

What is the most widely used second messenger that is a nucleotide?

Cyclic AMP (cAMP).

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Types of Antagonism

What is the efficacy of antagonists?

Antagonists have zero efficacy (intrinsic activity = 0), meaning no response is achieved by their binding.

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Efficacy and Efficacy in Pharmacology

What is E max?

The maximal effect a drug can produce.

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Types of Antagonism

Can competitive antagonism be reversible?

Yes, it can be either reversible or irreversible.

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Protein Targets for Drug Binding

What type of receptors are intracellular and nuclear receptors?

They are protein targets for drug binding that act within the cell.

p.5
Efficacy and Efficacy in Pharmacology

What is efficacy in pharmacology?

The maximal response a drug produces at full receptor occupation.

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Signal Transduction and Second Messengers

Which ion is commonly used as a second messenger?

Calcium ions (Ca2+).

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Agonists and Antagonists

What happens to a receptor in the presence of an agonist?

The receptor is functionally activated.

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Protein Targets for Drug Binding

What are G protein-linked receptors?

A type of protein target for drug binding.

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Physiological Receptors

What are intracellular receptors?

Receptors located inside the cell that bind to ligands.

p.5
Affinity and Efficacy in Pharmacology

What does potency refer to in pharmacology?

The dose required to produce a certain response.

p.2
Drug Receptors and Their Functions

Where are drug receptors located?

On cell surfaces, within the cell membrane, and inside the cells.

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Drug-Receptor Interactions

What are the two types of binding to receptors?

Irreversible and reversible.

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Physiological Receptors

What type of receptors are linked to enzymes like tyrosine kinase?

Receptors linked to enzymes.

p.2
Affinity and Efficacy in Pharmacology

What theory explains the specificity of drug binding?

Key and Lock theory.

p.9
Signal Transduction and Second Messengers

Name a second messenger that is a nucleotide and is involved in signal transduction.

Cyclic GMP (cGMP).

p.5
Efficacy and Efficacy in Pharmacology

What is ED50?

The dose at which 50% of the maximal effect is observed.

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Physiological Receptors

What are ionotropic receptors?

Ligand-gated ion channel receptors.

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Drug-Receptor Interactions

What is the function of the ligand binding domain?

It is where the drug binds selectively via chemical bonds.

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Protein Targets for Drug Binding

What are tyrosine kinase linked receptors?

A type of receptor that is a protein target for drug binding, involved in cellular signaling.

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Types of Agonists

What is a full agonist?

A full agonist has affinity and efficacy, binds to a receptor, and elicits a maximal response (100%).

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Affinity and Efficacy in Pharmacology

How is potency related to dose?

Potency is inversely related to the dose (drug concentration).

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Types of Antagonism

What is physiological antagonism?

When two substances act to oppose each other's effects.

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Physiological Receptors

What are G-protein coupled receptors?

A type of physiological receptor that interacts with G-proteins.

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Drug-Receptor Interactions

What does the message propagation domain do?

It transduces and propagates extracellular signals into an intracellular amplified response.

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Types of Antagonism

What is the outcome when an antagonist binds to a receptor?

It results in no response but prevents the response of the agonist.

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Signal Transduction and Second Messengers

What are second messengers?

Small, non-protein, water-soluble molecules or ions involved in signal transduction.

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Types of Agonists

What characterizes a partial agonist?

A partial agonist has affinity and some efficacy, binds to a receptor, but never produces a maximal effect (< 100%).

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Drug-Receptor Interactions

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.

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Drug-Receptor Interactions

How is the response to a drug characterized?

It is graded or dose-dependent.

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Types of Antagonism

What does pharmacokinetic antagonism involve?

Altering the way the body handles another drug, affecting absorption, metabolism, or excretion.

p.9
Signal Transduction and Second Messengers

What role does Diacylglycerol (DAG) play in cellular signaling?

It acts as a second messenger.

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Types of Antagonism

What are the two main types of pharmacological antagonism?

Competitive and non-competitive antagonism.

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Types of 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.

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Agonists and Antagonists

What is the state of a receptor in the absence of an agonist?

The receptor is functionally silent.

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Types of Antagonism

What is an example of a non-competitive antagonist?

Channel blockers.

p.4
Affinity and Efficacy in Pharmacology

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.

p.1
Protein Targets for Drug Binding

What are ligand-gated channels?

Channels that open in response to the binding of a ligand, serving as a protein target for drugs.

p.4
Affinity and Efficacy in Pharmacology

How does efficacy change with concentration?

Efficacy increases as a function of concentration.

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