Lecture 3 Flashcards
What are agonist
dungs interacted with receptor to generate a responses
dung that interact with receptor are known as agonist efficacy
+ receptor activity increases
- receptor activity decreases
this forums a drug complex generating a response
What isa full agonist
binds and have affinity for and actuates a receptor displaying full efficacy of the receptor
EG: Isoprofernol which mimics the Action of aderline at beta
What is a partial agonist
have only partial efficacy at the receptor relative to a full agonist
eg:busprisone
What is occupancy
proportion of the receptor occupied by the drug
size of the respon se varies with the proportion of the recepto r Occupied
what increases if the Occupancy increases
agonist
whatis Occupancy formula
Occupancy= no. of receptors1/ Total no. of receptors
easy occupant cy?
free receptor + agonist →← agonist R Complex + actuation of transduction → response cycle
What does k1 + K2 Stand for?
K1 → forward rate of reaction
K1 → backward rate of reaction
What is the formula of occupancy using K
occupancy= Na /N To T=E A/ K2/ KI A
What isthe max response
tissues invowed no. of receptor and no. of Coupling Complex= big response
What is the Concentration response Curve is?
To measure how occupancy Varies [AJ we measure bio response varies [A)
- instead
What is a potency?
measures the cons of a drug this Is Whre it is effective
↳ helps with the Oose
↳ E50/ A50]
Less 150= higher potency
what is affinity
it is a measure of how Strong a bug bird to its recept s ka= Occupancy affinity decreases
whatis a slope
some drugs might have a steckper dope
what is efficacy
efficacy is the relationship Between receptor occupancy and the ability to Initiate a response
Drug binding with a receptor
increase ‘ value = strong response
total no. of receptor for that drug
Coupling exsist
