Theories of drug receptor interaction
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An important topics of pharmacology. These theories are necessary to understand the basic knowledge of drug-receptor interaction.
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THEORIES OF DRUG RECEPTOR INTERACTION
1. The document discusses drug receptor interaction theories including occupation theory, rate theory, induced fit theory, macromolecular perturbation theory, activation-aggregation theory, and two-state receptor model.
2. It classifies ligands that bind to receptors as full agonists, partial agonists, or antagonists and describes different types of agonists and antagonists.
3. The key forces involved in drug-receptor binding are described as well as interactions that stabilize drug-receptor complexes such as ionic interactions, hydrogen bonding, and hydrophobic interactions.
Theories of drug interaction
Theories of drug interaction Tathagata Pradhan, Indo Soviet Friendship College of Pharmacy, Moga, Punjab
This document discusses theories of drug receptor interaction. It describes the occupation theory which states that pharmacological effect is proportional to the number of occupied receptors. It also discusses the rate theory, induced fit theory, macromolecular perturbation theory, activation-aggregation theory, and two-state model of receptor activation. Each theory provides a different perspective on how drugs interact with receptors and elicit biological responses.Drug receptor intraction
The document discusses theories of drug receptor interaction, including:
1. The occupancy theory states that drug effect is proportional to the number of occupied receptors. Maximal response occurs when all receptors are occupied.
2. The rate theory suggests pharmacological activity depends on the rate of drug association and dissociation from receptors, not just occupancy.
3. The induced-fit theory proposes that drug binding induces conformational changes in the receptor, allowing agonists to elicit a response while antagonists do not.
4. The two-state model postulates receptors exist in two states (active and inactive) and drugs bind preferentially to one state, determining if they act as agonists, inverse agonists, or antagonists
Agonists and antagonists
Agonists and antagonists Ligands Types of agonist-
Endogenous agonist
Super agonist
Full agonist
Partial agonist
Inverse agonist
Irreversible agonist
Properties of Antagonist :
Spare receptors
Addiction
Drug tolerance
Dependence
Tachyphylaxis
Idiosyncrasy
Allergy
Drug receptor interaction
This document discusses drug receptor interactions, including definitions of key terms like drug, receptor, antagonist, and pA2 value. It describes how drugs bind to receptors and can act as agonists or antagonists. Quantitative aspects of drug-receptor interactions are covered, including dose-response curves, potency, and therapeutic indices. Factors that contribute to variability in individual responses are also summarized. Binding studies and docking simulations are introduced as methods to study these interactions.
NEUROHUMORAL TRANSMISSION
STEPS INVOLVED IN NEURO-HUMORAL TRANSMISSION,
IMPULSE CONDUCTION , TRANSMITTER RELEASE,TRANSMITTER ACTION ON POST-JUNCTIONAL ACTIVITY , POST-JUNCTIONAL ACTION ,TERMINATION OF ACTION.
Drug receptors
The Topic DRUG RECEPTORS tells you about everything you want to know it's classification, Regulation, Introduction etc.
Heterocyclic compounds _ Organic Chemistry _ B. Pharm.
This document discusses the properties, synthesis, reactions, and medicinal uses of several aromatic heterocyclic compounds including pyrrole, furan, thiophene, pyrazole, imidazole, oxazole, thiazole, pyridine, azepines, quinoline, and isoquinoline. For each compound, the key topics covered are their aromatic properties, common methods of synthesis such as the Paal-Knorr reaction and Hantzsch synthesis, typical reactions like electrophilic substitution and reduction, and some medicinal applications.
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THEORIES OF DRUG RECEPTOR INTERACTION
1. The document discusses drug receptor interaction theories including occupation theory, rate theory, induced fit theory, macromolecular perturbation theory, activation-aggregation theory, and two-state receptor model.
2. It classifies ligands that bind to receptors as full agonists, partial agonists, or antagonists and describes different types of agonists and antagonists.
3. The key forces involved in drug-receptor binding are described as well as interactions that stabilize drug-receptor complexes such as ionic interactions, hydrogen bonding, and hydrophobic interactions.
Theories of drug interaction
Theories of drug interaction Tathagata Pradhan, Indo Soviet Friendship College of Pharmacy, Moga, Punjab
This document discusses theories of drug receptor interaction. It describes the occupation theory which states that pharmacological effect is proportional to the number of occupied receptors. It also discusses the rate theory, induced fit theory, macromolecular perturbation theory, activation-aggregation theory, and two-state model of receptor activation. Each theory provides a different perspective on how drugs interact with receptors and elicit biological responses.Drug receptor intraction
The document discusses theories of drug receptor interaction, including:
1. The occupancy theory states that drug effect is proportional to the number of occupied receptors. Maximal response occurs when all receptors are occupied.
2. The rate theory suggests pharmacological activity depends on the rate of drug association and dissociation from receptors, not just occupancy.
3. The induced-fit theory proposes that drug binding induces conformational changes in the receptor, allowing agonists to elicit a response while antagonists do not.
4. The two-state model postulates receptors exist in two states (active and inactive) and drugs bind preferentially to one state, determining if they act as agonists, inverse agonists, or antagonists
Agonists and antagonists
Agonists and antagonists Ligands Types of agonist-
Endogenous agonist
Super agonist
Full agonist
Partial agonist
Inverse agonist
Irreversible agonist
Properties of Antagonist :
Spare receptors
Addiction
Drug tolerance
Dependence
Tachyphylaxis
Idiosyncrasy
Allergy
Drug receptor interaction
This document discusses drug receptor interactions, including definitions of key terms like drug, receptor, antagonist, and pA2 value. It describes how drugs bind to receptors and can act as agonists or antagonists. Quantitative aspects of drug-receptor interactions are covered, including dose-response curves, potency, and therapeutic indices. Factors that contribute to variability in individual responses are also summarized. Binding studies and docking simulations are introduced as methods to study these interactions.
NEUROHUMORAL TRANSMISSION
STEPS INVOLVED IN NEURO-HUMORAL TRANSMISSION,
IMPULSE CONDUCTION , TRANSMITTER RELEASE,TRANSMITTER ACTION ON POST-JUNCTIONAL ACTIVITY , POST-JUNCTIONAL ACTION ,TERMINATION OF ACTION.
Drug receptors
The Topic DRUG RECEPTORS tells you about everything you want to know it's classification, Regulation, Introduction etc.
Heterocyclic compounds _ Organic Chemistry _ B. Pharm.
This document discusses the properties, synthesis, reactions, and medicinal uses of several aromatic heterocyclic compounds including pyrrole, furan, thiophene, pyrazole, imidazole, oxazole, thiazole, pyridine, azepines, quinoline, and isoquinoline. For each compound, the key topics covered are their aromatic properties, common methods of synthesis such as the Paal-Knorr reaction and Hantzsch synthesis, typical reactions like electrophilic substitution and reduction, and some medicinal applications.
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The document discusses chiral molecules and their reactions. Chiral molecules have non-superimposable mirror images due to having four different groups attached to a carbon atom without symmetry. There are three major reactions for chiral molecules: retention, where the configuration of substrate and product remain the same; inversion, where the isomer converts to the other form through an SN2 mechanism; and racemization, where a second chiral center forms diastereomers.
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"Chemistry of Prostaglandins & Leukotrienes" , Tathagata Pradhan , Department...
"Chemistry of Prostaglandins & Leukotrienes" , Tathagata Pradhan , Department...Tathagata Pradhan, Indo Soviet Friendship College of Pharmacy, Moga, Punjab
Prostaglandins and leukotrienes are eicosanoids derived from arachidonic acid. They were first discovered in seminal fluid in the 1930s. Prostaglandins are synthesized via the cyclooxygenase pathway while leukotrienes are synthesized via the lipoxygenase pathway. These lipid mediators act on specific G-protein coupled receptors and are involved in various physiological processes like contraction and relaxation of smooth muscles, inflammation, and platelet aggregation. Due to their role in inflammation and bronchoconstriction, leukotriene receptor antagonists are used to treat asthma.Receptors
Introduction - receptor
Drug – receptor interactions
Ligand gated ion channel receptors
G – protein coupled receptors
Kinase liked receptors
Nuclear receptors
Comparison of receptor types
Conclusion
References
Enzyme induction and inhibition
This document discusses enzyme induction and inhibition. It defines enzymes as biological catalysts that speed up reactions without being permanently altered. Enzyme activity can be altered by small molecules binding to the active site or other sites. Inhibitors reduce enzymatic reaction rates by blocking the active site without destroying enzymes, and can be reversible or irreversible. Inhibitors are classified as competitive, non-competitive, uncompetitive, or mixed based on whether they bind to the active site or other sites and how they impact substrate binding and catalysis. Enzyme induction increases enzyme production and activity through a homeostatic regulatory mechanism, often by combining with a regulatory protein to increase gene expression.
Enzyme inhibition for M.Pharm
ENZYME INHIBITION THE MOST IMPORTANT TOPIC FOR BIOLOGY AS WELL AS CHEMISTRY PEOPLES. WE HAVE HERE COVERED FOR THE PHARMA STUDENTS THIS WILL MAKE THEM EASY AS WE ARE COLLECTED ALL THE DATA A SINGLE PLACE WICH COVERS ALL THE COTENTS.
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Resolution of racemic mixture
The document discusses various methods for resolving a racemic mixture into its pure enantiomers, including:
1) Mechanical separation, which separates crystal forms of enantiomers
2) Preferential crystallization, which seeds a solution with a pure enantiomer to induce crystallization
3) Biochemical separation using microorganisms that metabolize one enantiomer more quickly
4) Chromatographic separation exploiting differences in how enantiomers adsorb to a chiral support
5) Kinetic methods using reactions that proceed at different rates for each enantiomer
6) Precipitation of one enantiomer through reaction with a reagent
7) Formation of diastereomers with an opt
Concepts of agonist and antagonist receptors
This document summarizes the concepts of agonists and antagonists in receptor activation and inhibition. It defines agonists as ligands that enhance receptor activity and antagonists as those that oppose agonist action and block receptor activation. The document compares the properties and types of agonists, including full, partial, and inverse agonists, and antagonists, including competitive, non-competitive, and irreversible antagonists. It discusses how agonists and antagonists regulate signaling pathways through their effects on receptor activation and inhibition.
Anti inflammatory drugs
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SAR of Morphine
This document discusses structure-activity relationships in drug design and formulation. It introduces Hammett and Hansch plots, which relate reaction rates and biological activity to electronic and physicochemical properties. Modification of lead compounds is explored through changing functional groups, stereochemistry and lipophilicity. Morphine is used as a case study to illustrate how properties like log P, binding groups and stereochemistry impact opioid activity. The conclusion emphasizes the role of medicinal chemistry in understanding disease and developing safer, more effective pharmaceuticals.
History of Medicinal Chemistry
Medicinal chemistry involves the design and synthesis of pharmaceutical agents to benefit humanity. It includes synthesis, structure-activity relationship studies, receptor interactions, and analysis of absorption, distribution, metabolism, and excretion. The field has its roots in the isolation of alkaloids like morphine in the early 19th century. In the late 19th century, semi-synthetic and synthetic derivatives of plant-derived compounds were developed. Modern medicinal chemistry emerged in the late 19th/early 20th century with advances like the receptor theory and development of antibiotics and sulfonamides. The 1940s-1960s were a "golden era" with the invention of many modern drug classes such as corticosteroids, antipsychotics
Drug receptor-interactions
1. There are several types of drug receptors that mediate the effects of drugs, including ion channel-linked receptors, G-protein-linked receptors, enzyme-linked receptors, and intracellular receptors.
2. Drugs interact with specific receptors through precise physiochemical and spatial interactions, and this binding can lead to responses by activating ion channels, enzymes, or other intracellular signaling pathways.
3. The interaction between a drug and its receptor is described using principles from enzyme kinetics, with terms like efficacy, potency, affinity, agonists, partial agonists, and antagonists. Competitive and non-competitive antagonism can alter the response to receptor activation.
Types of receptors
This document discusses the different types of receptors:
1) Ligand-gated ion channels directly open ion channels in response to neurotransmitters.
2) G-protein coupled receptors activate intracellular second messenger systems through G-proteins.
3) Kinase-linked receptors activate intracellular protein kinases.
4) Nuclear receptors regulate gene transcription by binding to DNA response elements as dimers.
Sythesis of heterocyclic drugs ketoconazole and metronidazole
A Heterocyclic compounds are those which has atoms of at least two different elements as members of its ring.
Heterocyclic chemistry is a branch of organic chemistry dealing with the synthesis, properties, and applications of these heterocycles.
Synthesis of benzimidazole
1) The document describes the procedure for synthesizing benzimidazole from o-phenylenediamine and formic acid.
2) Key steps include heating a mixture of o-phenylenediamine and excess formic acid at 100°C for 2 hours, then making the reaction mixture alkaline with sodium hydroxide to precipitate crude benzimidazole.
3) Benzimidazole has biological applications as an active component in anthelmintic and antiulcer drugs, and its derivatives also show antimicrobial and anticancer properties.
Bioassay
Bioassay is defined as measuring the biological response of living tissues to determine the potency or concentration of an active principle in a preparation. There are various types of bioassays including quantal assays, graded assays, and multiple point assays. Bioassays can be performed on intact animals, isolated tissues, specific cells, or organisms and are useful for standardizing drugs obtained from natural sources and for measuring the activity of new or undefined substances. While powerful, bioassays can be time-consuming and expensive compared to physico-chemical methods.
Drug metabolism
Metabolic Changes of Drugs and Related Organic Compounds describes the human metabolic processes of various functional groups found in therapeutic agents.
The importance of a chapter on metabolism lies in the fact that drug interactions are based on these processes.
For pharmacists, it is necessary for them to understand why certain drugs are contraindicated with other drugs.
This chapter attempts to describe the various phases of drug metabolism, the sites where these biotransformation will occur, the role of specific enzymes, metabolism of specific functional groups, and several examples of the metabolism of currently used therapeutic agents.
Interaction between drugs and receptors.pptx
The document discusses several theories of drug-receptor interaction:
1) Occupation theory states response is proportional to receptor occupancy
2) Rate theory states effect depends on rate of drug binding to receptors
3) Allosteric theory proposes drugs can bind distinct allosteric sites to enhance or inhibit receptor activity
4) Lock and key theory analogizes drug-receptor binding as a key fitting into a lock
5) Induced fit theory states binding induces conformational changes in the receptor and ligand in a dynamic process.
Drug receptor interaction theory and spare receptors.pptx
1) The document discusses several theories of drug-receptor interaction including occupation theory, rate theory, allosteric theory, lock-and-key theory, and induced-fit theory.
2) It defines spare receptors as receptors that remain unbound despite a drug producing its maximum effect. The presence of spare receptors allows cells to use endogenous ligands economically.
3) Spare receptors have implications for drug development by suggesting drugs can still be fully effective even without occupying all receptors. This highlights the complexity of drug-receptor interactions.
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Neurohumoral transmission in CNS-
The term neurohumoral transmission designates the transfer of a nerve impulse from a presynaptic to a postsynaptic neuron by means of a humoral agent e.g. a biogenic amine, an amino acid or a peptide.
Hansch and Free-Wilson QSAR Models
In this slide I covered the detailed about hansch analysis, Free-Wilson analysis, and Mixed approach. I also gave a detailed application for each points.
Reactions of chiral molecules
The document discusses chiral molecules and their reactions. Chiral molecules have non-superimposable mirror images due to having four different groups attached to a carbon atom without symmetry. There are three major reactions for chiral molecules: retention, where the configuration of substrate and product remain the same; inversion, where the isomer converts to the other form through an SN2 mechanism; and racemization, where a second chiral center forms diastereomers.
Receptor - Pharmacology
This powerpoint basically used for better understanding of different types of receptors and various terminology in pharmacology.
"Chemistry of Prostaglandins & Leukotrienes" , Tathagata Pradhan , Department...
"Chemistry of Prostaglandins & Leukotrienes" , Tathagata Pradhan , Department...Tathagata Pradhan, Indo Soviet Friendship College of Pharmacy, Moga, Punjab
Prostaglandins and leukotrienes are eicosanoids derived from arachidonic acid. They were first discovered in seminal fluid in the 1930s. Prostaglandins are synthesized via the cyclooxygenase pathway while leukotrienes are synthesized via the lipoxygenase pathway. These lipid mediators act on specific G-protein coupled receptors and are involved in various physiological processes like contraction and relaxation of smooth muscles, inflammation, and platelet aggregation. Due to their role in inflammation and bronchoconstriction, leukotriene receptor antagonists are used to treat asthma.Receptors
Introduction - receptor
Drug – receptor interactions
Ligand gated ion channel receptors
G – protein coupled receptors
Kinase liked receptors
Nuclear receptors
Comparison of receptor types
Conclusion
References
Enzyme induction and inhibition
This document discusses enzyme induction and inhibition. It defines enzymes as biological catalysts that speed up reactions without being permanently altered. Enzyme activity can be altered by small molecules binding to the active site or other sites. Inhibitors reduce enzymatic reaction rates by blocking the active site without destroying enzymes, and can be reversible or irreversible. Inhibitors are classified as competitive, non-competitive, uncompetitive, or mixed based on whether they bind to the active site or other sites and how they impact substrate binding and catalysis. Enzyme induction increases enzyme production and activity through a homeostatic regulatory mechanism, often by combining with a regulatory protein to increase gene expression.
Enzyme inhibition for M.Pharm
ENZYME INHIBITION THE MOST IMPORTANT TOPIC FOR BIOLOGY AS WELL AS CHEMISTRY PEOPLES. WE HAVE HERE COVERED FOR THE PHARMA STUDENTS THIS WILL MAKE THEM EASY AS WE ARE COLLECTED ALL THE DATA A SINGLE PLACE WICH COVERS ALL THE COTENTS.
Factors affecting drug metabolism
Phase I Vs Phase II Drug metabolism and factors affectiing drug metabolism.
Enzyme induction, Enzyme inhibitor, physicochemical properties wthich acan affect the drug metabolism
Resolution of racemic mixture
The document discusses various methods for resolving a racemic mixture into its pure enantiomers, including:
1) Mechanical separation, which separates crystal forms of enantiomers
2) Preferential crystallization, which seeds a solution with a pure enantiomer to induce crystallization
3) Biochemical separation using microorganisms that metabolize one enantiomer more quickly
4) Chromatographic separation exploiting differences in how enantiomers adsorb to a chiral support
5) Kinetic methods using reactions that proceed at different rates for each enantiomer
6) Precipitation of one enantiomer through reaction with a reagent
7) Formation of diastereomers with an opt
Concepts of agonist and antagonist receptors
This document summarizes the concepts of agonists and antagonists in receptor activation and inhibition. It defines agonists as ligands that enhance receptor activity and antagonists as those that oppose agonist action and block receptor activation. The document compares the properties and types of agonists, including full, partial, and inverse agonists, and antagonists, including competitive, non-competitive, and irreversible antagonists. It discusses how agonists and antagonists regulate signaling pathways through their effects on receptor activation and inhibition.
Anti inflammatory drugs
The document discusses anti-inflammatory agents known as non-steroidal anti-inflammatory drugs (NSAIDs). NSAIDs work by inhibiting the cyclooxygenase (COX) enzymes that produce prostaglandins, which are inflammatory mediators. There are two main COX isoforms, and most NSAIDs inhibit both COX-1 and COX-2 to varying degrees. Selective COX-2 inhibitors may reduce side effects associated with COX-1 inhibition like gastric irritation. NSAIDs are classified into different categories based on their chemical structure and properties. The most common NSAIDs inhibit COX through different mechanisms of action and metabolic pathways.
SAR of Morphine
This document discusses structure-activity relationships in drug design and formulation. It introduces Hammett and Hansch plots, which relate reaction rates and biological activity to electronic and physicochemical properties. Modification of lead compounds is explored through changing functional groups, stereochemistry and lipophilicity. Morphine is used as a case study to illustrate how properties like log P, binding groups and stereochemistry impact opioid activity. The conclusion emphasizes the role of medicinal chemistry in understanding disease and developing safer, more effective pharmaceuticals.
History of Medicinal Chemistry
Medicinal chemistry involves the design and synthesis of pharmaceutical agents to benefit humanity. It includes synthesis, structure-activity relationship studies, receptor interactions, and analysis of absorption, distribution, metabolism, and excretion. The field has its roots in the isolation of alkaloids like morphine in the early 19th century. In the late 19th century, semi-synthetic and synthetic derivatives of plant-derived compounds were developed. Modern medicinal chemistry emerged in the late 19th/early 20th century with advances like the receptor theory and development of antibiotics and sulfonamides. The 1940s-1960s were a "golden era" with the invention of many modern drug classes such as corticosteroids, antipsychotics
Drug receptor-interactions
1. There are several types of drug receptors that mediate the effects of drugs, including ion channel-linked receptors, G-protein-linked receptors, enzyme-linked receptors, and intracellular receptors.
2. Drugs interact with specific receptors through precise physiochemical and spatial interactions, and this binding can lead to responses by activating ion channels, enzymes, or other intracellular signaling pathways.
3. The interaction between a drug and its receptor is described using principles from enzyme kinetics, with terms like efficacy, potency, affinity, agonists, partial agonists, and antagonists. Competitive and non-competitive antagonism can alter the response to receptor activation.
Types of receptors
This document discusses the different types of receptors:
1) Ligand-gated ion channels directly open ion channels in response to neurotransmitters.
2) G-protein coupled receptors activate intracellular second messenger systems through G-proteins.
3) Kinase-linked receptors activate intracellular protein kinases.
4) Nuclear receptors regulate gene transcription by binding to DNA response elements as dimers.
Sythesis of heterocyclic drugs ketoconazole and metronidazole
A Heterocyclic compounds are those which has atoms of at least two different elements as members of its ring.
Heterocyclic chemistry is a branch of organic chemistry dealing with the synthesis, properties, and applications of these heterocycles.
Synthesis of benzimidazole
1) The document describes the procedure for synthesizing benzimidazole from o-phenylenediamine and formic acid.
2) Key steps include heating a mixture of o-phenylenediamine and excess formic acid at 100°C for 2 hours, then making the reaction mixture alkaline with sodium hydroxide to precipitate crude benzimidazole.
3) Benzimidazole has biological applications as an active component in anthelmintic and antiulcer drugs, and its derivatives also show antimicrobial and anticancer properties.
Bioassay
Bioassay is defined as measuring the biological response of living tissues to determine the potency or concentration of an active principle in a preparation. There are various types of bioassays including quantal assays, graded assays, and multiple point assays. Bioassays can be performed on intact animals, isolated tissues, specific cells, or organisms and are useful for standardizing drugs obtained from natural sources and for measuring the activity of new or undefined substances. While powerful, bioassays can be time-consuming and expensive compared to physico-chemical methods.
Drug metabolism
Metabolic Changes of Drugs and Related Organic Compounds describes the human metabolic processes of various functional groups found in therapeutic agents.
The importance of a chapter on metabolism lies in the fact that drug interactions are based on these processes.
For pharmacists, it is necessary for them to understand why certain drugs are contraindicated with other drugs.
This chapter attempts to describe the various phases of drug metabolism, the sites where these biotransformation will occur, the role of specific enzymes, metabolism of specific functional groups, and several examples of the metabolism of currently used therapeutic agents.
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"Chemistry of Prostaglandins & Leukotrienes" , Tathagata Pradhan , Department...
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Sythesis of heterocyclic drugs ketoconazole and metronidazole
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Similar to Theories of drug receptor interaction
Interaction between drugs and receptors.pptx
The document discusses several theories of drug-receptor interaction:
1) Occupation theory states response is proportional to receptor occupancy
2) Rate theory states effect depends on rate of drug binding to receptors
3) Allosteric theory proposes drugs can bind distinct allosteric sites to enhance or inhibit receptor activity
4) Lock and key theory analogizes drug-receptor binding as a key fitting into a lock
5) Induced fit theory states binding induces conformational changes in the receptor and ligand in a dynamic process.
Drug receptor interaction theory and spare receptors.pptx
1) The document discusses several theories of drug-receptor interaction including occupation theory, rate theory, allosteric theory, lock-and-key theory, and induced-fit theory.
2) It defines spare receptors as receptors that remain unbound despite a drug producing its maximum effect. The presence of spare receptors allows cells to use endogenous ligands economically.
3) Spare receptors have implications for drug development by suggesting drugs can still be fully effective even without occupying all receptors. This highlights the complexity of drug-receptor interactions.
1. theories of d r intersctn presentn
Drugs interact with receptors through various forces like hydrogen bonding, ionic interactions, and hydrophobic interactions. This interaction forms a drug-receptor complex that can dissociate. The affinity and stability of this complex determines the drug's potency and efficacy. Several theories have attempted to explain how drug-receptor binding leads to a biological response, such as occupation theory, induced fit theory, and two-state receptor model. The two-state model proposes that receptors exist in two conformations - active and inactive - and drugs can shift the equilibrium to elicit different responses.
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Receptors are cellular components that drugs bind to in order to produce their pharmacological effects. The ability of a drug to bind is determined by its chemical structure interacting with complementary surfaces on the receptor. When an agonist binds to a receptor, it activates or enhances the cell's activity by triggering biochemical events. Antagonists also bind receptors but do not activate the cell's activity; they prevent agonists from binding. The affinity and intrinsic activity of a drug determine which effects it produces.
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The document discusses drug receptors and how drugs act in the body. It provides information on:
- Receptors are molecules that drugs bind to, initiating their effects. The binding is determined by the drug's chemical structure.
- Agonists activate or enhance cellular activity by binding to receptors. Antagonists bind but do not activate the receptor, instead blocking agonists from binding.
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Molecular mechanisms of drugs
1. Drug-receptor interactions involve drugs binding reversibly to receptors via various interactions like ionic bonds or hydrogen bonds.
2. When a drug binds a receptor, it can either activate the receptor like an agonist to produce a biological response, or have no effect like an antagonist.
3. Different theories describe drug-receptor interactions, like occupation theory which says response is proportional to receptor occupancy, or induced fit theory where binding causes conformational changes in the receptor and drug.
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- Agonists, partial agonists, and inverse agonists are drug ligands that interact with receptors to elicit different cellular responses. Agonists mimic the effects of endogenous ligands, partial agonists produce submaximal effects, and inverse agonists stabilize receptors in their inactive state.
- The two-state receptor model describes receptors existing in two conformational states (active and inactive) that ligands differentially stabilize. Biased agonism occurs when ligands preferentially activate different intracellular signaling pathways.
- Key concepts include efficacy, intrinsic activity, and constitutive receptor activity. Partial agonists have efficacy below full agonists and produce submaximal responses even at full receptor occupancy. Inverse agonists suppress constitutive receptor activity.
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Pharmacodynamics covers how drugs act on the body. Drugs can act through receptor-mediated or non-receptor mediated mechanisms. Receptor-mediated actions involve drug binding to receptors, which then trigger signal transduction pathways. The main receptor families are ligand-gated ion channels, G-protein coupled receptors, enzymatic receptors, and nuclear receptors. Drugs can have different effects depending on their affinity and efficacy at receptors. Tolerance can develop with repeated drug use through pharmacokinetic or pharmacodynamic changes. Therapeutic dosing aims to achieve drug concentrations within the therapeutic window for maximum benefit.
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PRINCIPLES OF PHARMOCODYNAMICS 2 [Autosaved].pptx
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Theories of drug receptor interaction
- 1. Theories of Drug- Receptor Interaction BY -: NITESH KUMAR B. PHARM 7TH SEM JAIPUR COLLEGE OF PHARMACY. JAIPUR, RAJASTHAN
- 2. 1. Occupancy theory-: It is proposed by Gaddum and Clark. According to this theory, the intensity of pharmacological effect is directly proportional to the number of receptors occupied by the drug. The number of receptors occupied by the drug depends on the amount of dose of the drug and the total number of receptors available. 2. Rate theory-: This theory suggests that the number of drug- receptor interactions formed per unit time determines the intensity of the response. This means that the intensity of pharmacological activity is directly proportional to the rate of association and dissociation of the drug and the receptor.
- 3. Thus, drugs that associate with and then rapidly dissociate from the receptor, thus allowing other drug molecules to subsequently interact with the receptor, would be expected to produce the most intense response. 3. Induced-fit theory-: It is proposed by Koshland. According to this theory, the receptor does not normally pre-exist in the proper conformation for drug binding. As the drug approaches the receptor, a conformational change occurs in the receptor to allow effective binding.
- 4. Following dissociation of the drug, the receptor can then revert to its original conformation. In this theory, an antagonist can induce a conformational change in the receptor. However, this change is not the proper change required to produce pharmacological activity.
- 5. 4. Macromolecular perturbation theory Combining the rate theory and the induced-fit theory results in macromolecular perturbation theory. This theory suggests that two types of conformational changes exist and the rate of their existence determines the observed biological response. Agonists produce the specific perturbation required for a biological response, whereas antagonists produce a nonspecific perturbation, which fails to yield a biological response perturbation theory.
- 6. So, the intensity of pharmacological response is directly proportional to the rate of formation of specific perturbation. 5. Activation – aggregation theory-: According to this theory, even in the absence of a drug, receptors are always in a state of dynamic equilibrium between active and inactive states. Agonists bind to the active state and thus shift the equilibrium towards the active state, whereas antagonists bind to both the states and thus there is no change in equilibrium.