2022-10-13T03:31:55+03:00[Europe/Moscow] en true <p>drug and receptor</p>, <p>receptor</p>, <p>low</p>, <p>Kd</p>, <p>larger concentration of drug-receptor complex; greater affinity for the drug</p>, <p>Ionic (electrostatic) interaction</p>, <p>histamine, lysine, arginine </p>, <p>aspartic acid, glutamine </p>, <p>ionic</p>, <p>ion-dipole</p>, <p>dipole-dipole</p>, <p>hydrogen bonding</p>, <p>intermolecular</p>, <p>intramolecular</p>, <p>decreases free energy; stabilizing </p>, <p>pi stacking</p>, <p>Van der Waals forces</p>, <p>full agonist</p>, <p>partial agonist</p>, <p>agonist</p>, <p>antagonist</p>, <p>inverse agonist</p>, <p>agonist</p>, <p>agonist</p>, <p>antagonist</p>, <p>enantiomer </p>, <p>equilibrium; basal activity</p>, <p>Full agonist</p>, <p>Partial agonist</p>, <p>Full inverse agonist</p>, <p>Antagonist </p>, <p>eutomer</p>, <p>distomer</p>, <p>eudismic ratio</p>, <p>d</p>, <p>chiral</p>, <p>3</p> flashcards
Ligand Stereochemistry

Ligand Stereochemistry

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  • drug and receptor

    the interaction between what two things is ultimately responsible for pharmaceutical effect- pharmacodynamics ?

  • receptor

    -protein-molecule that recognizes and responds to endogenous chemical signals

  • low

    The driving force or drug-receptor complex is at what energy state?

  • Kd

    -measures the affinity of a receptor to a drug

    -represents concentration of the drug that gives 50% drug-receptor complex

  • larger concentration of drug-receptor complex; greater affinity for the drug

    A smaller Kd tells us what about the receptor?

  • Ionic (electrostatic) interaction

    -when a full charge interacts with another full charge

  • histamine, lysine, arginine

    Basic groups involves with ionic interactions? (gives us a positive charge)

  • aspartic acid, glutamine

    Acidic groups that give us a negative charge?

  • ionic

    What type of interaction is occuring?

    What type of interaction is occuring?

  • ion-dipole

    What type of reaction is this?

    What type of reaction is this?

  • dipole-dipole

    What type of reaction is this?

    What type of reaction is this?

  • hydrogen bonding

    What type of reaction is this?

    What type of reaction is this?

  • intermolecular

    hydrogen bonding that occurs between two molecules

  • intramolecular

    hydrogen bonding that occurs within the same molecule

  • decreases free energy; stabilizing

    Increase in entropy of H2O molecules _______. Leads to _________ the complex

  • pi stacking

    What type of hydrophobic interaction is this?

    What type of hydrophobic interaction is this?

  • Van der Waals forces

    -as molecules approach, temporary dipoles in one atom induce opposite dipoles in another; therefore, producing an intermolecular attraction

  • full agonist

    What is this a representation of ?

    What is this a representation of ?

  • partial agonist

    What is this a representation of?

    What is this a representation of?

  • agonist

    To effect a certain response of a receptor, design a(n) ____

  • antagonist

    To block a particular response of a natural ligand of a receptor, design a(n)

  • inverse agonist

    To produce the opposite affect of the natural ligand, design a(n)

  • agonist

    Which shows structural similarity to natural ligand; agonist or antagonist?

  • agonist

    What type of drug is this?

    What type of drug is this?

  • antagonist

    What type of drug is this?

    What type of drug is this?

  • enantiomer

    What type of drug is this?

    What type of drug is this?

  • equilibrium; basal activity

    R and R* are in _______ which defines the _________ of the receptor.

  • Full agonist

    ______ bind only to R*- lead to an increase in basal activity

  • Partial agonist

    ________ bind preferentially to R* (some still bind to R)

  • Full inverse agonist

    __________ bind only to R (decrease in basal activity)

  • Antagonist

    __________ have equal affinities for both R & R* (no effect on basal activity)

  • eutomer

    more potent enantiomer

  • distomer

    less potent enantiomer

  • eudismic ratio

    the ratio of eutomer/distomer potencies of enantiomers

  • d

    Distomers are usually ______

    a. more potent

    b. less potent

    c. equally efficacious

    d. impure

  • chiral

    What is the typical stereochemistry of drugs? Chiral or racemic ?

  • 3

    How many binding sites must the receptor have in order for the drug to bind?