Pharmacology SAR

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Pharmacological effect on the subject
Activity

Quantitative measure
Potency

Gold standard for all opioids
Morphine

Investigation of the mutual complementarity between a drug structure and the binding site
SAR

What does QSAR stand for?
Quantitative Structure-Activity Relationship

What is used to determine drug-receptor interactions in a subset of structure-property correlations in which a variety of chemical and physical molecular properties is employed to define the association between structure and property?
QSAR

Is it more efficient to determine an EC50 value in vivo or in vitro?
In vivo

The definition of QSARs is defined by which 3 properties?
Physical, Biological, Intrinsic

By swapping out an amino acid you can determine?
If that amino acid is directly responsible for activity

What type of inhibitor is effective against HIV infection
Protease inhibitor

A critical component of the HIV genome codes for which protease?
Aspartate protease

Structural studies of the inhibitor-enzyme complex showed that what type of molecule serves to mediate contact between the enzyme and inhibitor
Water molecule

Which functional group can you add in order to increase the ability to form Hydrogen bonds
Hydroxyl groups

Inhibitors of HIV-1 protease
Saquinavir, Indinavir, Ritonavir, Nefinavir, Amprenavir, Lopinavir

What is an example in which both enantiomers of a drug are equally active?
General anesthetics

Can enantiomers of a drug differ at all and if so how?
They can differ quantitatively and qualitatively or not at all

What is the benefit of single enantiomer drugs?
Reduced side effects

NSAIDs cause gastric irritation due to?
Ion trapping

What groups are known as vector groups to alter physiochemical properties
Carrier and vulnerable groups

Which group is used to control ADE properties
Carrier groups

What else controls ADE with carrier groups
Ionization

What group affects metabolism
Vulnerable groups

What part of the benzodiazepine is a basic pharmacophore
Nucleus

What is the gold standard drug for benzos?
Diazepam

A privileged structure capable of being directed with appropriate molecular modification against a number of discrete and nonrelated receptors
Pharmacophore

One of the most challenging issues in both drug-receptor recognition and drug development is the translation of the receptor recognition properties of a protein and peptides to small molecules, this is called
Peptide mimetics or peptidomimetics

Opioid receptors are examples of what type of receptor?
GPCR

What are the specific receptor types of opioids
Mu, kappa, delta

This mu opioid agonist continues to be the drug of choice for treatment of severe chronic pain
mORPHINE

2 major side effects of mu opioid analgesics
Tolerance and constipation

Does central tolerance or peripheral tolerance occur rapidly?
Central tolerance, increased dose required to maintain analgesia

How are Ki and Kd proportional?
Directly proportional

What does Ki stand for?
Inhibition constant

What is peripheral tolerance
How a drug affects the rest of the body

What protein regulates the distribution and bioavailability of drugs along with the removal of toxic metabolites and xenobiotics
P-glycoprotein

P-gp (efflux transporter) contributes to the development of central tolerance of morphine by?
Actively pumping morphine out of the CNS

Where is P-gp expressed in?
BBB and GI tract

Elimination of the P-gp substrate activity of opioids would?
Diminish tolerance and reduce severity of constipation

What is the cutoff time in seconds for animal testing of opioids?
10 seconds

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