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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
N-methylation __________ activity (SAR of central sympathomimetic agents)
Increases
26
Di-N-methylation __________ activity (SAR of central sympathomimetic agents)
Decreases
27
Mono-N substituents larger than methyl __________ excitatory properties (SAR of central sympathomimetic agents)
Decrease
28
A racemic mixture that has a higher proportion of cardiovascular effects than the dextro isomer (Examples of central sympathomimetic agents)
Amphetamine sulfate
29
In dextroamphetamine sulfate, the dextrorotatory isomer has the __________ and fewer cardiovascular effects (Examples of central sympathomimetic agents)
S-configuration
30
Has a very high abuse potential; more marked central and less peripheral action than dextroamphetamine (Examples of central sympathomimetic agents)
Methamphetamine hydrochloride (Shabu)
31
__________ are also known as appetite suppressants (Examples of central sympathomimetic agents)
Anorexiants
32
Phentermine HCl, benzphetamine HCl, and phendimetrazine tartrate are examples of __________ (Examples of central sympathomimetic agents)
Anorexiants
33
Tends to produce sedation rather than excitation; is an anorexiant (Examples of central sympathomimetic agents)
Fenfluramine hydrochloride
34
Uptake inhibitor of NE and 5-HT; an antidepressant and anorexiant drug (Examples of central sympathomimetic agents)
Sibutramine
35
Indications include narcolepsy and ADHD (Examples of central sympathomimetic agents)
Methylphenidate hydrochloride
36
Increases the rate of synthesis of DA (Examples of central sympathomimetic agents)
Pemoline
37
Depression is caused by __________ serotonin, norepinephrine, and dopamine (Examples of central sympathomimetic agents)
Low/Decreased
38
Selective and reversible inhibitor of MAO-A; an antidepressant without producing hypertensive crises (Examples of monoamine oxidase inhibitors)
Moclobemide
39
Selective and irreversible inhibitor of MAO-B; has value in treating Parkinson diseases (Examples of monoamine oxidase inhibitors) (SR)
Selegiline, Rasagiline
40
Nonselective and irreversible inhibitor of MAO-A and MAO-B; was used for its hypotensive action (Examples of monoamine oxidase inhibitors)
Pargyline
41
Nonselective and irreversible inhibitor of MAO-A and MAO-B (Examples of monoamine oxidase inhibitors) (PIT)
Phenelzine, Isocarboxazid, Tranylcypromine
42
__________ undergoes isosteric replacement of phenothiazines' "S" with a "C-C" isostere
Tricyclic antidepressants
43
Prototype of tricyclic antidepressants
Imipramine
44
__________ contains an iminodibenzyl ring (Types of tricyclic antidepressants)
Dihydrodibenzazepine
45
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)
6-7-6
46
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)
3
47
Substituting a halogen or cyano group into the __________-position of the dihydrodibenzazepine ring enhanced preferential affinity for SERT (SAR of tricyclic antidepressants)
3
48
__________ amines are sedatives (SAR of tricyclic antidepressants)
Tertiary
49
__________ amines are stimulants (SAR of tricyclic antidepressants)
Secondary
50
__________ amines have more affinity for inhibiting 5-HT reuptake (SAR of tricyclic antidepressants)
Tertiary
51
__________ amines have more affinity for inhibiting NE uptake (SAR of tricyclic antidepressants)
Secondary
52
__________ amines have higher anti-HAM side effects (SAR of tricyclic antidepressants)
Tertiary
53
Tertiary amines block __________ receptors, causing orthostatic hypotension (SAR of tricyclic antidepressants)
α1 adrenergic
54
Tertiary amines block __________ receptors, causing dry mouth, constipation, urinary retention, and blurred vision (SAR of tricyclic antidepressants)
Muscarinic
55
Tertiary amines block __________ receptors, causing weight gain and sedation (SAR of tricyclic antidepressants)
Histaminic
56
__________ are drugs that differ from the tricyclics, in that the tricyclic system has been taken apart in the center
Selective serotonin reuptake inhibitors (SSRIs)
57
By breaking up the tricyclic system (ex. in SSRIs), it gives compounds with __________ anticholinergic effects
Diminished
58
Fluoxetine, fluvoxamine, paroxetine, sertraline, and citalopram are examples of __________
Selective serotonin reuptake inhibitors (SSRIs)
59
Nisoxetine, reboxetine, and venlafaxine are examples of __________
Serotonin-norepinephrine reuptake inhibitors (SNRI)
60
Selective serotoninergic reuptake inhibitors and 5-HT2A antagonists such as trazodone and nefazodone are also used as __________
Hypnotics
61
Has anxiolytic and antidepressant activities (Examples of 5-HT1A agonists and partial agonists)
Buspirone
62
Its MOA is increased NE release via α2-NE receptor antagonism (Examples of α2 Antagonists)
Mirtazapine
63
Its MOA is block of DA reuptake via the dopamine transporter (Examples of miscellaneous antidepressants)
Bupropion
64
It has structural resemblance to the central neurotransmitter, serotonin/5-HT; examples include dimethyltryptamine, psilocybin, and psilocin (Examples of 1β-arylamino hallucinogens)
Indolethylamines
65
Has a structural resemblance to NE and DA; examples include mescaline, DOM/STP, MDA, and ecstasy (Examples of 1β-arylamino hallucinogens)
2-Phenylethylamines
66
Has marked effects on serotoninergic and dopaminergic neurons; possesses both indolethylamine and phenylethylamine moiety (Examples of 1β-arylamino hallucinogens)
(+)-Lysergic acid diethylamide (LSD)
67
Was introduced as a dissociative anesthetic for animals; its close structural relative is ketamine (Examples of dissociative agents)
Phenycyclidine
68
A psychotomimetic and drug of abuse; a potent DA reuptake blocker (Examples of euphoriant-stimulant)
Cocaine
69
A phenolic OH is required for activity; binds to cannabinoid receptors, CB1 and CB2 (Examples of depressant-intoxicant)
Δ1-Tetrahydrocannabinol/Δ9-THC
70
Cannabinoid receptor responsible for CNS actions
CB1
71
Cannabinoid receptor responsible for immune tissues
CB2

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

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