Medicinal Chemistry2||Midterm

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Medicinal Chemistry2||Midterm

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For the following compounds

1 point

Which compound(s) has/have neuromuscular blocking activity?

A&C

A&B

Only A

A&D

Only B

According to the following formula:

1 point

Choose the incorrect statement about its structure-activity relationship :

A. R1 & R2 are hydrophilic groups important for the antagonist activity

B. If x is absent, R3 should be H-bond participating group

C. If the nitrogen is tertiary this means it can penetrate the BBB

D. Two carbons as a chain length (CH2)n is acceptable for good activity

Having the following Figure:

1 point

the binding interaction (a) is called:

A.Hydrogen bond

B. Hydrophobic interaction

C. Ionic bond

D. Dipole-dipole bond

For the following molecules:

1 point

A. Compound A is a toxic gas acts as an irreversible AChEI

B. Compound C is a highly toxic and selective AChEl to human

C. Compound B is a reversible AChEl and the esterase enzyme is slowly reactivated

D. Compound D is anti-dot used after the aging to recover the inhibited AChE

For the following AChEls

1 point

An analogue that inhibits AChE through carbamylation mechanism and can cross BBB is

The part of atropine structure that participates in ionic bond with the receptor is the ester group

1 point

True

False

For the following agents (Procyclidine & Trospium):

1 point

Which of the following is a correct comparison between both drugs?

Trospium can penetrate the BBB while Procyclidine cannot.

R1 & R2 are identical in Procyclidine but different in Trospium

X is ester in Trospium while it is absent in Procyclidine

Procyclidine has a longer intermediate chain (CH2)n than Trospium

Having the following scheme showing how Acetylcholine esterase enzyme hydrolyzes acetylcholine:

1 point

which stage shows that the enzyme is acylated and considered as "deactivated"?

According to the following formula:

1 point

Choose the correct statement that describe its structure-activity relationship.

Three carbons chain length (CH2)n is acceptable for its activity

If X is absent, R3 should be H.

R1 & R2 are hydrophobic groups important for the agonist activity

the nitrogen is tertiary this gives the best binding with the receptor

For Acetylcholine (structure below), choose the correct SAR statement.

1 point

Select one:

Adding aromatic ring at the terminal carbon of the acyloxy group increases its agonist activity

If ethylene bridge is extended (three carbons instead of two) this eliminates or decreases activity

If both oxygen atoms removed this increases activity

If nitrogen replaced by carbon this increases activity

The following are different intermediates for AChE enzyme:

1 point

The intermediate that shows a phosphorylated enzyme before aging is:

Removing the aromatic group in Atropine will increase its cholinergic antagonist activity

1 point

True

False

Choose the best matching with each of the following descriptions
*

1 point

An analogue that is selective on muscarinic receptors and stabilized against esterase by only steric sheilding

An analogue that is non- selective but is stabilized against esterases by electronic factors

An analogue that is selective on muscarinic receptors and stabilized against esterases by both electronic and steric sheilding

An analogue that is non-selective and readily hydrolyzed by esterases

Choose the best matching with each of the following descriptions

1 point

An analogue that is non- selective but is stabilized against esterases by electronic factors

An analogue that is selective on muscarinic receptors and stabilized against esterases by both electronic and steric sheilding

An analogue that is non- selective and readily hydrolyzed by esterases

An analogue that is selective on muscarinic receptors and stabilized against esterase by only steric sheilding

Clear selection

Choose the best matching with each of the following descriptions

1 point

An analogue that is selective on muscarinic receptors and stabilized against esterase by only steric sheilding

An analogue that is non- selective but is stabilized against esterases by electronic factors

An analogue that is selective on muscarinic receptors and stabilized against esterases by both electronic and steric sheilding

An analogue that is non- selective and readily hydrolyzed by esterases

Clear selection

Choose the best matching with each of the following descriptions

1 point

An analogue that is selective on muscarinic receptors and stabilized against esterase by only steric sheilding

An analogue that is non- selective but is stabilized against esterases by electronic factors

An analogue that is selective on muscarinic receptors and stabilized against esterases by both electronic and steric sheilding

An analogue that is non- selective and readily hydrolyzed by esterases

Clear selection

Having the following Figure:

1 point

the binding interaction (a) is called

Dipole-dipole bond

Hydrophobic interaction

Hydrogen bond

Ionic bond

Clear selection

For the following compounds:

1 point

Which compound(s) has/have neuromuscular blocking activity?

A&C

A&D

Only B

Only A

A&B

Clear selection

For the following agents (Procyclidine & Trospium):

1 point

Which of the following is a correct comparison between both drugs?

R1 & R2 are identical in Trospium but different in Procyclidine

Procyclidine has a longer intermediate chain (CH2)n than Trospium

Procyclidine can participate in ionic bond while Trospium cannot

X is ester in Trospium while it is hydroxyl group in Procyclidine

For the following AChEls

1 point

An aryl carbamate that inhibits AChE through carbamylation mechanism and lack CNS side effects is

The correct statement of comparison between compound 1 and compound 2 is:

1 point

Compound 1 is active as nuromuscular blocking agent while compound 2 is inactive

The binding affinity of compound 1 is stronger than compound 2 for nicotinic receptors.

Compound 1 is more lipophilic than compound 2

Compound 2 has longer duration of action than compound 1

For the following AChEls

1 point

An alkyl carbamate that inhibits AChE through carbamylation mechanism and can't cross BBB is

Having the following scheme showing how Acetylcholine esterase enzyme hydrolyzes acetylcholine:

1 point

which stage shows that the enzyme is deacylated and considered as "reactivated"?

Clear selection

For the following two nicotinic antagonists:

1 point

The correct statement of comparison between compound 1 and compound 2 is:

Compound 2 is active as nuromuscular blocking agent while compound 1 is inactive

Compound 1 is more hydrophilic than compound 2

The binding affinity of compound 2 is stronger than compound 1 for nicotinic receptors

Compound 2 has longer duration of action than compound 1

Clear selection

Choose the correct statement:

1 point

Compound A is a safe gas and can be used as insecticidal agent

Compound D is anti-dot used before the aging to recover the irreversibly inhibited AChE

Compound B is an irreversible AChEI after it is bio-activated and converted to compound C in insects

Compound C is a reversible AChEI and the esterase enzyme is slowly reactivated

For the following AChEls

1 point

An inhibitor for AChE that inhibits the enzyme through non-carbamylation mechanism is

Clear selection

CH2OH group in atropine can participate in H-bond with the receptor active site

1 point

True

False

Which compound(s) has/have neuromuscular blocking activity?

1 point

A&C

Only B

Only A

A&D

A&B

Clear selection

Which of the following is a correct comparison between both drugs?

1 point

X is ester in Trospium while it is hydroxyl group in Procyclidine

Procyclidine can penetrate BBB better than Trospium

Trospium has a shorter intermediate chain (CH2)n than Procyclidine

R1 & R2 are identical in Procyclidine but different in Trospium

Clear selection

The following are different intermediates for AChE enzyme:

1 point

The intermediate that shows an acylated enzyme is:

For the following molecules:

1 point

Choose the incorrect statement:

Compound C is an irreversible AChEI and its activity is dependent on its oxidative delsulfurization

Compound A is toxic gas and can lead to a permanently inhibited AChE enzyme

Compound B is an irreversible ACHEI used as insecticidal agent but it needs a bio-activation in insects

Compound D is anti-dot used before the aging to recover the inhibited AChE

According to the following formula:

1 point

Choose the correct statement that describe its structure-activity relationship.

R1 & R2 are hydrophobic groups important for the antagonist activity

If the nitrogen is quaternary this gives the best penetration to reach the CNS

If X is absent, R3 should be H.

Removing the intermediate chain (CH2)n provides the best activity

Clear selection

The part of atropine structure that participates in ionic bond with the receptor is the amine group

1 point

True

False

Having the following Figure:

1 point

the binding interaction (d) is called:

Hydrogen bond

Dipole-dipole bond

Hydrophobic interaction

Ionic bond

Clear selection

According to the following formula:

1 point

Choose the correct statement that describe its structure-activity relationship.

If the nitrogen is quaternary this enhance the drug penetration through BBB

R1 & R2 are hydrophilic groups important for the antagonist activity

The chain length (CH2)n is not important so can be removed from the structure

If X is absent, R3 should be a group that participates in H-bonding with the receptor

The following are different intermediates for AChE enzyme:

1 point

The intermediate that shows a phosphorylated enzyme after aging is

For the following two nicotinic antagonists:

1 point

The incorrect statement of comparison between compound 1 and compound 2 is:

Compound 2 is active as nuromuscular blocking agent while compound 1 is inactive

The binding affinity of compound 1 is stronger than compound 2 for nicotinic receptors

Compound 1 is more hydrophilic than compound 2

Compound 1 has longer duration of action than compound 2

Clear selection

For the following agents (Procyclidine & Trospium):

1 point

Which of the following is a incorrect comparison between both drugs?

Procyclidine has a shorter intermediate chain (CH2)n than Trospium

R1 & R2 are identical in Trospium but different in Procyclidine

X is ester in Trospium while it is absent in Procyclidine

Trospium can penetrate the BBB while Procyclidine cannot

Clear selection

For the following molecules:

1 point

Choose the incorrect statement:

Compound C is an irreversible AChEI after it is bio-activated and converted to compound B in insects

Compound B is an irreversible AChEI used as insecticidal agent

Compound D is anti-dot used before the aging to recover the inhibited AChE

Compound A is a safe gas and can be used as insecticidal agent

Clear selection

The following are different intermediates for AChE enzyme:

1 point

The intermediate that shows a carbamylated enzyme is:

Clear selection

For Acetylcholine (structure below), choose the correct SAR statement

1 point

If ethylene bridge is extended (three carbons instead of two) this increases activity

If both oxygen atoms removed this increases activity

If nitrogen replaced by carbon this increases activity

Adding aromatic ring at the terminal carbon of the acyloxy group makes it antagonist

Clear selection

For Acetylcholine (structure below), choose the correct SAR statement.

1 point

If both oxygen atoms removed this eliminates or decreases activity

Adding aromatic ring at the terminal carbon of the acyloxy group increases its agonist activity

If nitrogen replaced by carbon this increases activity

If ethylene bridge is extended (three carbons instead of two) this increases activity

Clear selection

For the following molecules:

1 point

Compound B is an irreversible AChEI and used as insecticidal agent

Compound D is anti-dot used after the aging to recover the inhibited AChE

Compound B is an irreversible AChEI after it is bio-activated and converted to compound C in insects

Clear selection

Removing the aromatic group in Atropine will increase its cholinergic antagonist activity

1 point

True

False

For the following molecules:

1 point

Choose the correct statement:

Compound A is a safe gas and can be used as insecticidal agent

Compound C is an irreversible AChEl after it is bio-activated and converted to compound B in insects

Compound B is a reversible AChEI and the esterase enzyme is slowly reactivated

Compound D is anti-dot used after the aging to recover the inhibited AChE

Regarding the structure of acetylcholine The following derivative is:

1 point

a. Less active than the Ach

b. Active

C.inactive

D.not stable

e. Selective

Clear selection

Regarding the structure of acetylcholine The following derivative is:

1 point

active

not stable

stable

inactive

Regarding the structure of acetylcholine The following derivative is:

1 point

inactive

selective

active

not selective

Clear selection

Regarding the mechanism of Acetylcholinesterase-Catalyzed Hydrolysis of Ach:

1 point

a. At the end of acylation step the enzyme render inactive

b. At the end of deacylation step the enzyme render inactive

c. At the end of acylation step the enzyme render active

d. During both of them the enzyme keep its activity

Clear selection

The following is the structure of bethanecol, from the chemical structure you can say:

1 point

a. bethanecol is stable by resonance

b. all of the above

c. bethanecol is muscarinic selective

d. bethanecol is stable to hydrolysis

Clear selection

Procyclidine is:

1 point

Can cross blood brain barrier

It is nicotinic and muscarinic antagonist

Is an aminoether anticholinergic agent

It is nicotinic receptor

Clear selection

1 point

Compound B has a longer duration of action than that of compound C

Compound D is a tetrahydroisoquinoline-based analog which has a long duration of action

In compound A, converting amines from quaternary to tertiary increases the activity and duration of action

Compound B has a weaker binding affinity to the nicotinic receptors than that of compound C

Clear selection

Alkyl carbamates are superior to aryl carbamates as AChEls due to the formation of alkoxide anions. Is this statement True or False?

1 point

True

False

Clear selection

The following figure shows the binding of ACh to the enzyme AChE. The binding interaction (c) is called

1 point

Hydrogen bonding

Dipole-dipole bonding

Ionic bonding

Hydrophobic interaction

Clear selection

Acetylcholine cannot be therapeutically used as a cholinergic agonist due to lack of selectivity and low bioavailability. Is this statement True or False?

1 point

True

False

Clear selection

For the following neuromuscular blocking agents, choose the CORRECT statement from the choices below:

1 point

Compound C has a longer duration of action than that of compound B

In compound A, converting amines from quaternary to tertiary increases the activity and duration of action

Compound D is a tetrahydroisoquinoline-based analog with a self-destruction elimination mechanism

Compound B has a weaker binding affinity to the nicotinic receptors than that of compound C

Clear selection

From the following ACh analogs, compound B has a lower cholinergic activity than ACh due to the following fact:

1 point

The amine part is not permanently charged, so will not make the desired ionic bond

The triethyl groups connected to the amine bind with the receptor but induce different conformation from the active one

The ethylene bridge has longer carbon chain than the desired length

The acyloxy-alkyl group doesn't fit in the hydrophobic pocket of the muscarinic receptor

Clear selection

Acetylcholine has high bioavailability due to its stability for hydrolysis and its good penetration to cellular membranes. Is this statement True or False?

1 point

True

False

Clear selection

This figure shows the chemical groups required for the activity of acetylcholine (ACh) on muscarinic receptors. Please choose the correct SAR statement from the choices below:

1 point

Adding an aromatic ring at the terminal carbon of the acyloxy group converts the compound to an antagonist

Activity increases if the ethylene bridge is extended (using a three- carbon bridge instead of two-carbon bridge)

Activity increases if the nitrogen atom is replaced by a carbon atom

Activity increases if both oxygen atoms in the acyloxy group are removed

Clear selection

Which of the following is a natural chemical messenger for the adrenergic receptor?

1 point

Acetylcholine

Noradrenaline

Serotonin

Dopamine

Clear selection

The aromatic group in Atropine is the main group responsible for the cholinergic antagonist activity

1 point

True

False

The following structure (carbachol) is a cholinergic agonist

1 point

What is the purpose of the amino group in red?

It protects the neighboring ester group by means of an electronic effect.

It acts as a steric shield to protect the ester group

It interacts with a hydrophilic pocket in the binding site

It acts as a metabolically susceptible group

Which feature of acetylcholine interacts with the binding site of cholinergic receptors by hydrogen bonding?

1 point

The quaternary nitrogen

The acyl methyl group

All three N-methyl groups

The ester

Clear selection

Atropine has been used to decrease gastrointestinal motility and to counteract anticholinesterase poisoning.

1 point

What function does this molecule have

Nicotinic agonist

Nicotinic antagonist

Muscarinic agonist

Muscarinic antagonist

The mechanism by which acetylcholine is inactivated by acetylcholinesterase involved:

1 point

Acylation and deacylation of the serin residue.

Acylation and deacylation of the acetylcholine.

Clear selection

Atracurium is used intravenously as a neuromuscular blocker

1 point

The molecule undergoes a chemical degradation at slightly alkaline pH. What is the name of this reaction?

Hofmann rearrangement

McLafferty rearrangement

Cope rearrangement

Hofmann elimination

To which class of compounds do adrenaline, noradrenaline and dopamine belong?

1 point

Catecholamines

Diphenolethylamines

Phenethylamines

Adrenergics

Having the following Figure:

1 point

the binding interaction (b) is called

lonic bond

Hydrophobic interaction

Dipole-dipole bond

Hydrogen bond

Clear selection

Which of the following modifications of Norepinephrine increases the selectivity for beta receptors?

1 point

Removing both catechol hydroxyl groups

Changing the position of both catechol hydroxyl groups to be at 2 and 5

Replacing the OH group at position 3 by H atom

Replacing the OH group at position 4 by H atom

Clear selection

The following figure shows the binding interactions of Epinephrine with adrenergic receptors:

1 point

The binding interaction (b) is:

Covalent bond

lonic bond

Hydrogen bonding

Hydrophobic (pi pi stacking) interaction

Choose the correct description for the following modification on Norepinephrine:

1 point

It becomes non-selective adrenergic antagonist

It becomes more selective as alpha receptors agonists

It becomes non-selective adrenergic agonist

It becomes more selective as beta receptor agonist

Clear selection

Choose the best matching with each of the following descriptions:

1 point

Non-Selective beta receptor antagonist with oxymethylene group

Non-selective beta receptor antagonist that doesn't have oxymethylene group

Selective beta-1 receptor antagonist with oxymethylene group

Clear selection

Choose the best matching with each of the following descriptions:

1 point

Non-Selective beta receptor antagonist with oxymethylene group

Non-selective beta receptor antagonist that doesn't have oxymethylene group

Selective beta-1 receptor antagonist with oxymethylene group

Clear selection

Choose the best matching with each of the following descriptions:

1 point

Non-Selective beta receptor antagonist with oxymethylene group

Non-selective beta receptor antagonist that doesn't have oxymethylene group

Selective beta-1 receptor antagonist with oxymethylene group

Clear selection

The following scheme explains the metabolic pathways for one of the neurotransmitters:
*

1 point

The structure of metabolite D is:

Choose the correct description for the following modification on Norepinephrine:

1 point

It becomes non-selective adrenergic agonist

It becomes a substrate for both COMT and MAO enzymes

It becomes more selective for alpha receptors

It becomes more selective for beta receptors

Clear selection

Choose the incorrect SAR statement

1 point

Removing the NH2 group will decrease its activity

The propylenediamine is a linker and can be replaced by other linkers with no effect on activity

If the tetrahydrofuran ring is replaced by furan this is predicted to decrease its duration of actio

It is a Quinazoline-based analogue with a selective agonist activity on alpha receptors

Clear selection

Choose the incorrect statement:

1 point

All of them are imidazoline-based analogues

Compound A can penetrate BBB better than the other compounds

Compound C has the highest ionization at the physiological pH

Only compound D has an adrenergic antagonist activity

Clear selection

All the following modifications on Norepinephrine will increase the selectivity for beta receptors except:

1 point

Replacing the OH group at position 3 by CH2OH group

Changing the position of both catechol hydroxyl groups to be at 2 and 5

Replacing the OH group at position 3 by H atom

Adding a tert-butyl group to the amine group

Clear selection

All the following modifications on Norepinephrine will increase the selectivity for beta receptors except:

1 point

Adding a tert-butyl group to the amine group

Replacing the OH group at position 4 by H atom

Replacing the OH group at position 3 by H atom

Changing the position of both catechol hydroxyl groups to be at 3 and 5

Clear selection

Choose the correct statement

1 point

Compound B has the imidazoline ring part of a guanidino group

All of them are selective alpha receptor agonists

Compound C has the least ionization at the physiological pH

Only compound D has an adrenergic antagonist activity

Clear selection

Choose the correct description for the following modification on Norepinephrine:

1 point

It becomes adrenergic antagonist

It becomes more selective for beta receptors

It becomes more selective for alpha receptors

It becomes non-selective adrenergic agonist

Clear selection

Choose the correct description for the following modification on Norepinephrine

1 point

It becomes resistant to both COMT and MAO enzymes

It becomes non-selective adrenergic agonist

It becomes more selective for beta receptors

It becomes more selective for alpha receptors

Clear selection

Choose the correct SAR statement

1 point

It is a Quinazoline-based analogue with a selective agonist activity on alpha receptors

If the tetrahydrofuran ring is replaced by furan this is predicted to increase its duration of action

Removing the NH2 group will decrease its activity

The propylenediamine is an essential linker and if replaced by other linkers this will decrease its activity

Clear selection

Which of the following modifications of Norepinephrine increases the selectivity for alpha receptors?

1 point

Changing the position of catechol hydroxyl groups to be at 2 and 5

Adding tert-butyl group to the amine group

Removing both catechol hydroxyl groups

Replacing the OH group at position 3 by H atom

Clear selection

The following figure shows the binding interactions of Epinephrine with adrenergic :receptors

1 point

The binding interaction (c) is

Covalent bond

Hydrophobic (pi pi stacking) interaction

lonic bond

Hydrogen bonding

Clear selection

Which of the following modifications of Norepinephrine increases the selectivity for alpha receptors?

1 point

Adding tert-butyl group to the amine group

Replacing the OH group at position 4 by H atom

Replacing the OH group at position 3 by H atom

Changing the 4-OH from position 4 to position 5

Clear selection

Albuterol (Salbutamol) is an important clinical agent

1 point

Why was the hydroxymethylene group introduced?

It was introduced to increase the area of conformational space available to the OH group

It was a chain extension to place the OH group closer to its binding region in the binding site

It was introduced to reposition the phenol OH such that it was not recognized by metabolic enzymes

It was introduced to reduce the electronic influence of the OH group on the aromatic ring

Clear selection

Identify the tactic which is used to obtain B- adrenoceptor selectivity for adrenergic agonists.

1 point

Addition of an a-methyl group (alpha to the carbon bearing the amine)

Removal of one of the catechol OH groups

Introduction of a bulky N-alkyl substituent

Introduction of a naphthalene ring

Clear selection

Albuterol (Salbutamol) is an important clinical agent

1 point

What role does the t-butyl group play?

It introduces selectivity for B- adrenoceptor

It acts as steric shield to reduce metabolism

It increases hydrophobicity such that the molecule can cross cell membranes

It introduces selectivity for a- adrenoceptors

Clear selection

Choose the incorrect statement:

1 point

Only compound D has an adrenergic antagonist activity

Compound B can penetrate BBB better than compound A

Compound C has the highest ionization at the physiological pH

All of them have more activity for alpha receptors than beta receptors

Clear selection

All the following modifications on Norepinephrine will increase the selectivity for beta receptors except

1 point

Replacing the OH group at position 3 by H atom

Adding a tert-butyl group to the amine group

Changing the position of both catechol hydroxyl groups to be at 2 and 6

Replacing the OH group at position 3 by CH2OH group

Clear selection

The following figure shows the binding interactions of Epinephrine with adrenergic receptors

1 point

The binding interaction (a) is:

Hydrogen bonding

Ionic bond

Covalent bond

Hydrophobic (pi pistacking) interaction

Clear selection

Choose the correct statement:

1 point

All of them are selective alpha receptor agonists

Compound C has the highest ionization at the physiological pH

Compound B has the imidazoline ring part of a guanidino group

Only compound A has a selective adrenergic agonist activity

Clear selection

All the binding interactions are found except

1 point

Olonic bond

Hydrophobic (pi pi stacking) interaction

Covalent bond

Hydrogen bonding

Clear selection

Choose the incorrect SAR statement

1 point

It is a Quinazoline-based analogue

Removing the NH2 group will decrease its activity

The propylenediamine is a linker and can be replaced by other linkers with no effect on activity

If the tetrahydrofuran ring is replaced by furan this is predicted to increase its duration of action

Clear selection

.Choose the incorrect statement:

1 point

Compound B has an imidazoline ring

Only compound D has an adrenergic antagonist activity

Compound C has the highest ionization at the physiological pH

All of them are selective alpha receptor agonists

Clear selection

.Choose the correct description for the following modification on Norepinephrine:

1 point

It becomes resistant to both COMT and MAO enzymes

It becomes more selective for alpha receptors

It becomes non-selective adrenergic agonist

It becomes adrenergic antagonist

Clear selection

Choose the correct SAR statement

1 point

It is a Quinazoline-based analogue with a selective agonist activity on alpha receptors

Removing the NH2 group will decrease its activity

If the tetrahydrofuran ring is replaced by furan this is predicted to increase its duration of action

The propylenediamine is an essential linker and if replaced by other linkers this will decrease its activity

Clear selection

Regarding the following b-blocker, what the structure can tell you:

1 point

Its selective because of the aryloxypropanolamine

Its non-selective because of the aryloxypropanolamine

Its selective because of the substitution at position 4

Its non-selective because it is not substituted at position 4

Clear selection

which of the following statements is correct regarding the following agent:

1 point

Its stable because of the double bond in the middle of its chain

It is undergoing a self-destruct

Doesn't undergo hofmann elimination

Its lipophilic

Clear selection

Choose the incorrect statement:

1 point

Compound B can penetrate BBB better than compound A

Only compound D has an adrenergic antagonist activity

All of them have more activity for alpha receptors than beta receptors

Compound C has the highest ionization at the physiological pH

Clear selection

Regarding Amphetamine all of the following statements are correct, EXCEPT:

1 point

are methyl-substituted phenylethylamines

CNS stimulant

Selective ẞ1 receptor agonist

Mixed-acting Sympathomimetics

Clear selection

For the following molecules, choose the CORRECT statement from the choices below

1 point

Compound D is not a substrate for COMT

The presence of bulky-ortho chlorine atoms is not important for compound B selectivity

Compound C has an aminoimidazoline group

All of the molecules are selective alpha-1 receptor agonists

Clear selection

For phenylethanolamine-based sympathomimetic agents, choose the INCORRECT SAR statement

1 point

R3 is H this provides agents with selective agonist activity on alpha receptors

For direct agonist activity, R3 should be at least one OH group

If R1 is isopropyl, selectivity increases on beta receptors and decreases alpha receptors

R2 substitution has an effect on activity and/or selectivity depending on the substituents

Clear selection

Ephedrine is:

1 point

Selective ẞ1 receptor antagonist

Selective ẞ1 receptor agonist

Phenylpropanolamines derivative

cannot cross BBB

Clear selection

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