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PH 110.1 - Pharmaceutical & Medicinal Organic Chemistry (Lab) > MIDTERM 03 - CNS Stimulants > Flashcards

MIDTERM 03 - CNS Stimulants Flashcards

1
Q

Are potent and relatively non-selective CNS stimulants; convulsive dose lies near their analeptic dose

A

Traditional analeptics

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2
Q

Picrotoxinin and pentylenetetrazole are examples of __________

A

Traditional analeptics

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3
Q

Are more selective CNS stimulants

A

Newer agents

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4
Q

Modafinil and doxapram are examples of __________

A

Newer agents

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5
Q

An active ingredient of picrotoxin; used for determining mechanisms of action of sedatives (Examples of traditional analeptics)

A

Picrotoxinin

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6
Q

__________ moiety is mandatory for the activity of picrotoxinin, with the 2-propenyl group assisting

A

Hydroxylactonyl

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7
Q

MOA of picrotoxinin

A

GABA-A receptor antagonist

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8
Q

Acts as a convulsant; used as a laboratory tool in determining potencies of potential anticonvulsant drugs in experimental animals (Examples of traditional analeptics)

A

Pentylenetetrazole

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9
Q

MOA of pentylenetetrazole

A

GABA-A receptor antagonist

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10
Q

Used to treat daytime sleepiness in narcolepsy patients (Examples of newer agent analeptics)

A

Modafinil

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11
Q

MOA of modafinil

A

Atypical α1-norepinephrine (NE) receptor stimulant

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12
Q

Used as respiratory stimulant; acts on peripheral carotid chemoreceptors (Examples of newer agent analeptics)

A

Doxapram

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13
Q

3 examples of naturally occurring methylxanthines (CTT)

A

Caffeine, Theophylline, Theobromine

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14
Q

Also known as 1,3,7-trimethylxanthine (Examples of methylxanthines)

A

Caffeine

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15
Q

Also known as 1,3-dimethylxanthine (Examples of methylxanthines)

A

Theophylline

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16
Q

Also known as 3,7-dimethylxanthine (Examples of methylxanthines)

A

Theobromine

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17
Q

Methylxanthines are __________ inhibitors

A

Phosphodiesterase

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18
Q

Methylxanthines act as __________ receptor antagonists

A

Adenosine

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19
Q

Are agents that are also known as psychomotor stimulants

A

Central sympathomimetic agents

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20
Q

Central sympathomimetic agents have a __________ moiety

A

β-phenethylamine

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21
Q

Branching with lower alkyl groups on the carbon atom adjacent to the amino nitrogen __________ CNS rather than peripheral activity (SAR of central sympathomimetic agents)

A

Increases

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22
Q

Hydroxylation of the ring or β-carbon (to the nitrogen) __________ activity, largely by decreasing the ability to cross the BBB (SAR of central sympathomimetic agents)

A

Decreases

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23
Q

Halogenation of the aromatic ring __________ sympathomimetic activity (SAR of central sympathomimetic agents)

A

Decreases

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24
Q

Methoxyl substitution on the ring tends to produce __________ agents (SAR of central sympathomimetic agents)

A

Psychotomimetic

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25
Q

N-methylation __________ activity (SAR of central sympathomimetic agents)

A

Increases

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26
Q

Di-N-methylation __________ activity (SAR of central sympathomimetic agents)

A

Decreases

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27
Q

Mono-N substituents larger than methyl __________ excitatory properties (SAR of central sympathomimetic agents)

A

Decrease

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28
Q

A racemic mixture that has a higher proportion of cardiovascular effects than the dextro isomer (Examples of central sympathomimetic agents)

A

Amphetamine sulfate

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29
Q

In dextroamphetamine sulfate, the dextrorotatory isomer has the __________ and fewer cardiovascular effects (Examples of central sympathomimetic agents)

A

S-configuration

30
Q

Has a very high abuse potential; more marked central and less peripheral action than dextroamphetamine (Examples of central sympathomimetic agents)

A

Methamphetamine hydrochloride (Shabu)

31
Q

__________ are also known as appetite suppressants (Examples of central sympathomimetic agents)

A

Anorexiants

32
Q

Phentermine HCl, benzphetamine HCl, and phendimetrazine tartrate are examples of __________ (Examples of central sympathomimetic agents)

A

Anorexiants

33
Q

Tends to produce sedation rather than excitation; is an anorexiant (Examples of central sympathomimetic agents)

A

Fenfluramine hydrochloride

34
Q

Uptake inhibitor of NE and 5-HT; an antidepressant and anorexiant drug (Examples of central sympathomimetic agents)

A

Sibutramine

35
Q

Indications include narcolepsy and ADHD (Examples of central sympathomimetic agents)

A

Methylphenidate hydrochloride

36
Q

Increases the rate of synthesis of DA (Examples of central sympathomimetic agents)

37
Q

Depression is caused by __________ serotonin, norepinephrine, and dopamine (Examples of central sympathomimetic agents)

A

Low/Decreased

38
Q

Selective and reversible inhibitor of MAO-A; an antidepressant without producing hypertensive crises (Examples of monoamine oxidase inhibitors)

A

Moclobemide

39
Q

Selective and irreversible inhibitor of MAO-B; has value in treating Parkinson diseases (Examples of monoamine oxidase inhibitors) (SR)

A

Selegiline, Rasagiline

40
Q

Nonselective and irreversible inhibitor of MAO-A and MAO-B; was used for its hypotensive action (Examples of monoamine oxidase inhibitors)

41
Q

Nonselective and irreversible inhibitor of MAO-A and MAO-B (Examples of monoamine oxidase inhibitors) (PIT)

A

Phenelzine, Isocarboxazid, Tranylcypromine

42
Q

__________ undergoes isosteric replacement of phenothiazines’ “S” with a “C-C” isostere

A

Tricyclic antidepressants

43
Q

Prototype of tricyclic antidepressants

A

Imipramine

44
Q

__________ contains an iminodibenzyl ring (Types of tricyclic antidepressants)

A

Dihydrodibenzazepine

45
Q

Tricyclic antidepressants contain a __________ ring arrangement in which the central seven-membered ring is either carbocyclic or heterocyclic, and saturated or unsaturated, which is fused to two phenyl rings (SAR of tricyclic antidepressants)

46
Q

The side chain may be attached to any one of the atoms in the central 7-membered ring, but it must be __________ carbon atoms, either saturated or unsaturated, and have a terminal amine group (SAR of tricyclic antidepressants)

47
Q

Substituting a halogen or cyano group into the __________-position of the dihydrodibenzazepine ring enhanced preferential affinity for SERT (SAR of tricyclic antidepressants)

48
Q

__________ amines are sedatives (SAR of tricyclic antidepressants)

49
Q

__________ amines are stimulants (SAR of tricyclic antidepressants)

50
Q

__________ amines have more affinity for inhibiting 5-HT reuptake (SAR of tricyclic antidepressants)

51
Q

__________ amines have more affinity for inhibiting NE uptake (SAR of tricyclic antidepressants)

52
Q

__________ amines have higher anti-HAM side effects (SAR of tricyclic antidepressants)

53
Q

Tertiary amines block __________ receptors, causing orthostatic hypotension (SAR of tricyclic antidepressants)

A

α1 adrenergic

54
Q

Tertiary amines block __________ receptors, causing dry mouth, constipation, urinary retention, and blurred vision (SAR of tricyclic antidepressants)

A

Muscarinic

55
Q

Tertiary amines block __________ receptors, causing weight gain and sedation (SAR of tricyclic antidepressants)

A

Histaminic

56
Q

__________ are drugs that differ from the tricyclics, in that the tricyclic system has been taken apart in the center

A

Selective serotonin reuptake inhibitors (SSRIs)

57
Q

By breaking up the tricyclic system (ex. in SSRIs), it gives compounds with __________ anticholinergic effects

A

Diminished

58
Q

Fluoxetine, fluvoxamine, paroxetine, sertraline, and citalopram are examples of __________

A

Selective serotonin reuptake inhibitors (SSRIs)

59
Q

Nisoxetine, reboxetine, and venlafaxine are examples of __________

A

Serotonin-norepinephrine reuptake inhibitors (SNRI)

60
Q

Selective serotoninergic reuptake inhibitors and 5-HT2A antagonists such as trazodone and nefazodone are also used as __________

61
Q

Has anxiolytic and antidepressant activities (Examples of 5-HT1A agonists and partial agonists)

62
Q

Its MOA is increased NE release via α2-NE receptor antagonism (Examples of α2 Antagonists)

A

Mirtazapine

63
Q

Its MOA is block of DA reuptake via the dopamine transporter (Examples of miscellaneous antidepressants)

64
Q

It has structural resemblance to the central neurotransmitter, serotonin/5-HT; examples include dimethyltryptamine, psilocybin, and psilocin (Examples of 1β-arylamino hallucinogens)

A

Indolethylamines

65
Q

Has a structural resemblance to NE and DA; examples include mescaline, DOM/STP, MDA, and ecstasy (Examples of 1β-arylamino hallucinogens)

A

2-Phenylethylamines

66
Q

Has marked effects on serotoninergic and dopaminergic neurons; possesses both indolethylamine and phenylethylamine moiety (Examples of 1β-arylamino hallucinogens)

A

(+)-Lysergic acid diethylamide (LSD)

67
Q

Was introduced as a dissociative anesthetic for animals; its close structural relative is ketamine (Examples of dissociative agents)

A

Phenycyclidine

68
Q

A psychotomimetic and drug of abuse; a potent DA reuptake blocker (Examples of euphoriant-stimulant)

69
Q

A phenolic OH is required for activity; binds to cannabinoid receptors, CB1 and CB2 (Examples of depressant-intoxicant)

A

Δ1-Tetrahydrocannabinol/Δ9-THC

70
Q

Cannabinoid receptor responsible for CNS actions

71
Q

Cannabinoid receptor responsible for immune tissues

PH 110.1 - Pharmaceutical & Medicinal Organic Chemistry (Lab) (11 decks)

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