2- Flashcards

1
Q

what is the drug action ?

A

molecular changes produced by a drug when t bind its target

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2
Q

what are the two aspects of drug action ?

A

Potency and efficacy

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3
Q

site the six mechanism of drug action

A

receptor, enzyme, ion chnnel, transport system trans factor, nucleid acid

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4
Q

what are receptors

A

proteins prticipate in intracellular comm via chemical signal

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5
Q

can receptors be found in cytoplasm ?

A

yep

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6
Q

which properties of receptors ?

A

saturability , reversibilityy (weak intermolar forces, vnderwalls)
stereoselectivity (recpgnize only one isomers)
agonist specificity related drug brind well and dissimilar compounds should bind poorly

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7
Q

tw0 phases of receptor propeties ?

A

Recognition, tranduction (functionnal response).

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8
Q

subpart of receptor

A

ligand binding domain, effector domain ssecond messenger

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9
Q

how is called receptor PLUS CELLULAR TARGET PLUS INTERMEDIARY MOLECULE ?

A

RECEPTOR EFFECTRS SYSTEM OR SIGNAL TRANSDUCTION PATHWAY

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10
Q

What are cell surfae receptor ?

A

ion gated or metabotropic (g coupled or tyrosine kinase linked receptor)

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11
Q

what are nuclar receptor ?

A

hormone

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12
Q

what trigers ions channel ?

A

change in membrane potential or ionic concentration

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13
Q

what triggers protein phosphorilation ?

A

cellular effect

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14
Q

What triggrs g protein ?

A

2nd messenger CAMP and cellular effect

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15
Q

what type are nAchR, NMDA r, GABAA ?

A

ionotropoc

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16
Q

what are ownstream effect of tirosine kinase linked receptor ?

A

for receptor dimer and activate tyrosine linase that results in phosporilation of downstream target.

17
Q

WHat receptors are NGF, PDGF, insulin ?

A

tyrsine linked receptrs

18
Q

what is transcripton facotr ?

A

lingand binding domainDNA binding domain that mediates binding to specific sites on the genome for activate or inhibit transcritpion of the nearby gene.

19
Q

hw to measure basic radioligand binding/affinity ?

A

{L} plus {R} egal LR plus LFREE(ligand qui accroche pas au recepteur)

20
Q

how is measured LR

A

radioligand binding

21
Q

how to discriminate bewteen specific and nonspecific binding ?

A

using radilabelled ligands: radiolabelled ligand has nochance to compete with the unlabelled ligand added in excess : bound activity = non specific + specific binding

or bound radioactivity 1st set of tubes - br 2d set of tubes = bound activity due to specific binding

22
Q

whats pccupancy theory ?

A

effect of a drug is proportionnal to nbr of receptor that is occupied by th edrug and has its basis in the law of mass action. Max response occurs whrn all receptors anre bound.

23
Q

diff type of agonist ?

A

full agonist, partial, inverse agonist, super agonist, endogenous agonist

24
Q

what is intrinsic activity ?

A

drug ability to bind a receptor and elicit a functional responde ?

25
Q

types of antagonism ?

A

competitive vs non competitive

26
Q

competitive abtagonism ?

A

bibds t same receptor as aonist

27
Q

no competitiva antagonism ?

A

binds to distinc site than agonist

28
Q

therapeutic index ?

A

therapeutic vs toxic effect