Which channel does SUR1 regulate in pancreatic beta cells?
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ATP-dependant K+ channel
How does a competitive receptor antagonist affect the receptor efficacy of the
agonist?
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It does NOT affect receptor efficacy because higher agonist
concentrations can outcompete the antagonist
,How does one obtain drugs classified as NAPRA II?
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From Pharmacist, without the need for prescription
Is the affinity of a drug most influenced by changes in the "off" or "on" rate?
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"off" rate
How does a chemical antagonist inactivate the agonist?
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Modifies or sequesters agonist
- renders agonist inactive
What is the therapeutic index used for? (TD50/ED50)
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Estimating relative safety margin of drug
, Where does NO bind Guanylyl Cyclase? What is the effect of this binding?
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Bind N-terminal domain
- enhances its activation of cGMP (200-400x)
What is a partial agonist?
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Not able to achieve maximal response (compared to full agonist)
- even with increasing agonist concentrations
- may show greater potency at a given receptor
Where are beta 1 receptors found? (3)
What is their action at each of these areas?
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1. SA node - increases HR
2. Cardiac muscle - increases contractility
3. Adipose tissue - increases lipolysis
What effect does a competitive receptor antagonist have on the Kd of the agonist?
Give this one a try later!
Give this one a try later!
ATP-dependant K+ channel
How does a competitive receptor antagonist affect the receptor efficacy of the
agonist?
Give this one a try later!
It does NOT affect receptor efficacy because higher agonist
concentrations can outcompete the antagonist
,How does one obtain drugs classified as NAPRA II?
Give this one a try later!
From Pharmacist, without the need for prescription
Is the affinity of a drug most influenced by changes in the "off" or "on" rate?
Give this one a try later!
"off" rate
How does a chemical antagonist inactivate the agonist?
Give this one a try later!
Modifies or sequesters agonist
- renders agonist inactive
What is the therapeutic index used for? (TD50/ED50)
Give this one a try later!
Estimating relative safety margin of drug
, Where does NO bind Guanylyl Cyclase? What is the effect of this binding?
Give this one a try later!
Bind N-terminal domain
- enhances its activation of cGMP (200-400x)
What is a partial agonist?
Give this one a try later!
Not able to achieve maximal response (compared to full agonist)
- even with increasing agonist concentrations
- may show greater potency at a given receptor
Where are beta 1 receptors found? (3)
What is their action at each of these areas?
Give this one a try later!
1. SA node - increases HR
2. Cardiac muscle - increases contractility
3. Adipose tissue - increases lipolysis
What effect does a competitive receptor antagonist have on the Kd of the agonist?
Give this one a try later!
