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Medicinal Chemistry > Dopaminergic > Flashcards

Dopaminergic Flashcards

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1
Q

D1/D5 family are located where and are coupled with what G-protein?

A

Postsynaptic, Gs activation of adenylate cyclase, cAMP increase.

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2
Q

D2/D3/D4 are located where and are coupled with what G-protein?

A

Pre and post synaptic. Gi, inhibit adenylate cyclase, decrease cAMP

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3
Q

What is the alpha rotamer, and what selectivity does it have?

A

Meta hydroxy group and basic nitrogen group are on the same side. Non-selective D agonist.

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4
Q

What is the beta rotamer and what is the selectivity?

A

Meta hydroxy group and basic nitrogen group are on opposite sides. D2 agonist > D1 agonist selectivity.

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5
Q

How is dopamine activity terminated, which is primary mechanism?

A

Primarily by reuptake by active transporter located on presynaptic. Second by metabolism by MAO or COMT.

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6
Q

What does dopamine control in the basal ganglia?

A

Particularly in the nigrostriatal pathway, posture, muscle tone, movement coordination. Lack of DA cause EPS.

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7
Q

What does dopamine do in the mesolimbic system?

A

Control behavior and emotion

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8
Q

What does dopamine do in the tuberoinfunibular system?

A

Decreases prolactin release.

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9
Q

What does dopamine do in the mesoaccumbens pathway?

A

Controls locomotor functions.

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10
Q

What drus affect the biosynthesis of dopoamine?

A 
A-methyltyrosine = inhibits tyrosine hydroxylase
Carbidopa= inhibits LAAAD by reacting to pyridoxal
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11
Q

What drug affects the storage of dopamine?

A

Amantadine( looks like a cube)

It increases dopamine release, decreases reuptake.

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12
Q

What drugs affect the release of dopamine?

A

Y-butyrolactone(OH——–carboxylic acid)

Mimics GABA, decreases dopamine release.

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13
Q

Describe the non-selective agonists.

A

Mimic alpha rotamer(same side basic nitrogen and meta hydroxy)
4 cyclic, with 1 catechol
Br to 4 cyclic linked by amide to 3 cyclic

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14
Q

Describe the D2 selective agonists

A

Mimic the beta rotamer(meta hydroxy and basic nitrogen opposite sides)
Frog and 1-legged frog

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15
Q

What are the uses for dopamine agonists?

A

Parkinson’s disease

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16
Q

What are the uses for dopamine antagonists?

A

Antipsychotics , depression, bipolar disorder

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17
Q

Describe the phenothiazine system.

A

C-1, C-4 needs to be empty
C-2 EWG required for activity.
N-10 unbranched, otherwise decrease potency

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18
Q

Which would be best and worst for activity.

Thioether, sulfonium, quartnary amine, 3 amine.

A

Best 3 amine, 4 amine, sulfonium, thioether worst

19
Q

Which conformation is better with the phenothiazines?

A

CIS is better than trans for binding.

20
Q

Which antipsychotics are most potent, least potent?

A

Piperazines most, piperidine, dialkylamino

21
Q

Which antipsychotics cause the most EPS?

A

Piperazines most, dialkylamino, piperidine least

22
Q

Which antipsychotcs cause the most sedation?

A

Dialkylamino = pipieridines, piperazines

23
Q

Which antipsychotics cause the most hypotensive effects?

A

Dialkylamino ~ piperidines, piperazines

24
Q

What are the characterisitics of a typical antipsychotic?

A

Potent D2 antagonist
High EPS
No 5-HT2 antagonism

25
Q

Describe the thioxanthene.

A

Tricyclic sulfur containing.
sulfone in EWG
Double bond will abolish the free rotation and lock it into CIS
D2 antagonist

26
Q

Describe the dibenzooxazepines.

A

Tricyclic containing oxygen.
Cl EWG
Locked into CIS conformation, no free rotation.
D2 antagonist

27
Q

Describe the fluorobutyrophenones.

A

Fluorophenyl, 4 carbon chain, attaches to nitrogen of the piperidine.
D2 antagonists, high EPS

28
Q

What are the characteristics of the atypical agents?

A

Lower affinity for D2 receptors
Lower EPS
Second generation 5-HT2 antagonism

29
Q

Describe the diphenylbutylpiperidine.

A

D2 antagonist atypical, with lower EPS than typical antipsychotics.
Two Fluorophenyl

30
Q

Describe the benzoisoxazoles, benzoisothiazole.

A

D2 antagonist and 5-HT2 antagonist.

Very low EPS.

31
Q

Describe the dibenzodiazepines.

A

Atypical antipsychotics, low affinity for D2 receptors.
A1-antagonists, anticholinergic, antihistaminergic.
Selective for D2 in limbic versus basal ganglia.

32
Q

Which drug has selectivity for D4 receptors?

A

Clozapine.
Cl EWG opposite from the basic nitrogen. Trans conformation.
Can cause agranulocytosis.

33
Q

Describe the COMT inhibitors.

A

Catechol with nitro group. Disrupts the metabolism of dopamine.

34
Q

Describe the MAO inhibitors.

A

Irreversible, increases dopamine, by decreases the metabolism. Contain a triple C bond.

35
Q

Where does parkinson’s disease occur and what are the symptoms?

A

In nigrostriatal.

Symptoms: muscle tremor, rigidity, bradykinesia

36
Q

What drugs are used for parkinson’s?

A

Dopamine agonists, MAO-B inhibitors, anticholinergics, COMT inhibitor, amantidine, L-dopa, carbidopa

37
Q

What are the symptoms of schizophrenia and what drugs are used to treat it?

A

Positive= delusions, hallucination, behavior, disorganize speech
Negative=flattened affect, social withdrawal
Antipsychotics , lack euphoric effect, less sedation, less tolerance, less respiratory depression.

38
Q

Antagonism of the dopamine receptors in the basal ganglia results in?

A

EPS

39
Q

Antagonism of dopamine receptors in the tuberoinfundibular results in?

A

Increase release of prolactin

40
Q

Antagonist of D2 presynaptic receptors cause what initially, then what over time?

A

Initially increase in dopamine release.

Depolarization inactivation with decrease release and biosynthesis of dopamine.

41
Q

What drug classes are typical antipsychotics?

A

Phenothiazines
Thioxanthenes
Fluorobutyrophenones

42
Q

What drug classes are atypical antipsychotics?

A

Diphenylbutylpiperidine
Benzoisoxazole
Benzoisothiazole
Dibenzodiazepines

43
Q

Describe the long chain arylpiperazine.

A

High affibity for D2/D3, serotonin 5-HT1/5-HT2a
Partial agonist at D2, 5-HT1a
Antagonist at 5-HT2a
Orthostatic hypotension antagonist at alpha1

Medicinal Chemistry (3 decks)

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