Kwon Quiz 9

the same

Epinephrine has ___ binding affinity for α1 compared to norpinephrine.

the same

Epinephrine has ___ binding affinity for α2 compared to norpinephrine.

True

T/F All adrenergic receptors are activated by the sympathetic nervous system, and NO adrenergic receptors are actived by the parasympathetic nervous system.

G coupled protein receptor

What type of receptor is α1?

G coupled protein receptor

What type of receptor is α2?

False

T/F Drugs tend to have the same binding affinity for both α1 and α2 receptors.

Both

___ receptors exist postsynaptically.

α2

___ receptors exist presynaptically.

Phenylephrine

What drug is a selective AGONIST for α1?

Clonidine

What drug is a selective AGONIST for α2?

Prazosin

What drug is a selective ANTAGONIST for α1?

Yohimbine

What drug is a selective ANTAGONIST for α2?

Dobutamine

What drug is an agonist for ß1?

Albuterol / Terbutaline

Which drug is an agonist for ß2?

α1

Select the correct receptor. Stimulation causes activation of PLC increasing Ca2+

α1

Select the correct receptor. Causes smooth muscle contraction.

α2

Select the correct receptor. Causes inhibition of transmitter release.

α2

Select the correct receptor. Uses the Gi signaling cascade.

α1

Select the correct receptor. Uses the Gq signaling cascade.

α2

Select the correct receptor. Stimulation causes decreases in cAMP.

calmodulin, MLCK

After the Gq signaling cascade and activation of PKC to release Ca2+, the calcium binds to ___ creating a complex. This complex binds to ___ and phosphorylates it to stimulate smooth muscle contraction.

Norepinephrine

___ binds to presynaptic α2 receptors and inhibits norepinphrine release.

Decrease

Decrease in cAMP leads to ____ in Ca2+.

ß2, α1, α2

Which receptor subtype is found on vascular smooth muscle tissue?

ß1

Which receptor subtype is found on heart tissue?

ß3

Which receptor subtype is found on adipose tissue?

ß2

Which receptor subtype is found on airway smooth muscle tissue?

increase, increase

ß1 receptor activation on the heart causes a(n) ___ of contractile force and a(n) ___ of heart rate.

All of them

Which of the following receptors works on the Gs signaling cascade?

increase, increase, decrease

Stimulation of ß2 adrenergic receptor causes a(n) ___ of potassium channels, ___ of sodium and calcium exchange, and a(n) ___ of MLCK activity.

Troponin

In the ß1 signaling cascade, activation of adenylyl cyclase causes an increase of Ca2+ that binds to ___ and activates cardiac muscle contraction

True

T/F Epinephrine, albuterol or isoproterenol are NOT good substrates for uptake 1 or MAO.

Increasing

____ bulkiness of substituents on the N-atom make the molecule better ß-agonists.

Reduces interaction of α receptors & ß receptors

What does removal of the OH sidechain on dopamine cause?

False

T/F The OH group on a dopamine is considered generally insignificant for its role in ligand-adrenergic receptor binding.

Reduces

Removal of one or both OH groups from the benzene ring off of drug molecules generally ___ affinity for ADRENERGIC receptors.

sympathomimetic drugs

They mimic the effects of norepinephrine and epinephrine

SNS

What nervous system do sympathomimetic drugs primarily effect?

True

T/F Sympathomimetic drugs typically produce undesirable side effects.

Adrenergic receptor agonists

Sympathomimetic drugs are an example of what kind of drug?

Direct

___-acting agonists directly bind to adrenergic receptors by mimicing the neurotransmitters.

Indirect

___-acting agonists facilitate release of norepinephrine to stimulate receptors.

Direct adrenergic receptor agonists

Phenylephrine is an example of a...

Indirect adrenergic receptor agonists

Amphetamines are an example of a...

Indirect adrenergic receptor agonists

Cocaine is an example of a...

True

T/F Cocaine has a different indirect mechanism of action, for it targets and blocks the neuronal reuptake of NE, rather than facilitating the release of more NE.

Direct adrenergic receptor agonists

Epinephrine is an example of a...

a1

What receptor is phenylephrine a substrate for?

ß1

What receptor is dobutamine a substrate for?

ß2

What receptor is albuterol a substrate for?

α2

What receptor is clonidine a substrate for?

α1, α2, ß1, ß2, ß3

What receptor is norepinephrine a substrate for?

α1, α2, ß1, ß2, ß3

What receptor is epinephrine a substrate for?

ß1, ß2

What receptor is isoproterenol a substrate for?

False

T/F Epinephrine is a selective, direct-acting adrenergic agonist.

ß1, increasing

Epinephrine activates ___ receptors on myocardial cells, that ___ contractility, increasing cardiac output.

In the SA node

Where are pacemaker cells located in the heart?

ß1, increasing

Epinephrine activates ___ receptors on pacemaker cells, that ___ heart rate, increasing cardiac output.

ß2

Epinephrine activation of ___ receptors causes vasodilation.

α1, α2

Epinephrine activation of ___ receptors leads to vasoconstriction.

ß2

Epinephrine activation of ___ receptors leads to bronchodilation.

α1

Epinephrine activation of ___ receptors leads to contraction of the spincter muscle of the bladder.

α1

Epinephrine activation of ___ receptors leads to radial dilator muscle of the iris.

ß2

Epinephrine activation of ___ receptors leads to decreased GI contractions.

ß2

Epinephrine activation of ___ receptors leads to relaxation of the detrusor muscle of the urinary bladder.

Increased

Epinephrine causes ___ circulating glucose, lactic acid, and free fatty acids.

ß-cells

What kind of pancreatic cells produce insulin?

α-cells

What kind of pancreatic cells produce glucagon?

Islet of langerhans

What kind of pancreatic cells produce pacreatic juice?

ß2

Activation of ___ receptors causes glucagon secretion from glucagon-secreting α-cells.

α2

Activation of ___ receptors causes inhibition of insulin secretion from insulin-secreting ß-cells

α1, ß2

Activation of ___ receptors causes gluconeogenesis and glycogenolysis in the liver.

ß3

Activation of ___ receptors causes lipolysis in adipocytes.

Treatment hyperkalemia

Which of the following is not a clinical use of epinephrine?

ß2

Low concentrations of epinephrine activate ___ receptors on vascular smooth muscle.

α1

High concentrations of epinephrine activate ___ receptors on vascular smooth muscle.

True

T/F Albuterol has NO stimulation on the heart.

Phenylephrine

Select the drug that is clinically used to treat sinus and nasal congestion.

Albuterol

Select the drug that is clinically used to hyperkalemia.

Clonidine

Which of the following drugs does NOT increase heart rate?

Clonidine

Select the drug that is clinically used to treat opiate agonist withdrawl.

Dobutamine

Select the STANDARD drug used to treat congestive heart failure.

NE

Select the STANDARD drug used to treat upper GI bleeding.

Phenylephrine

Which drug is longer acting?

Terbutaline

Select the drug that is NOT A STANDARD clinically used drug to treat shock.

Epinephrine

Select the STANDARD drug used to treat allergic induced anaphylaxis.

Causes muscle contraction

Stimulation of MLCK does what?

False

T/F Stimulation of ß1 receptors cause a decrease in heart rate.

Kinda true, since epinephrine causes BOTH vasodilation and vasoconstriction

T/F Epinephrine causes vasodilation of vascular smooth muscles, and norepinephrine causes vasoconstriction.

Terbutaline

Select the drug that is clincially used to inhibit uterine contraction in premature labor.

Clonidine

Select the drug that is clincially used to treat ADHD

Structure-activity relationship

What does SAR stand for? (in this PDA class)

decrease

A decrease in the amount of intracellular cAMP leads to a ___ in norepinephrine production

Reduce NE, not affect Epi

Uptake 1 will....

How tyramine affect adrenergic receptor agonists

Tyramine indirectly enhances the effects of adrenergic receptor agonists by causing the release of stored norepinephrine from presynaptic nerve terminals

Epinephrine

Which of the following has significant metabolic response?

True

T/F Although norepinephrine is a non-selective agonist for all 5 adrenergic receptors, it has weak binding affinity for ß2 and ß3 receptors.