CNS stimulants

Question 1

naturally occurring methylxanthines

Answer 1

caffeine
theophylline
theobromine

Question 2

caffeine

Answer 2

coffee, tea
1,3,7-trimethylxanthine
most potent cns stimulant

Question 3

theophylline

Answer 3

tea
1,3-dimethylxanthine
less potent cns stimulant than caffeine

Question 4

theobromine

Answer 4

cocoa
3,7-dimethylxanthine
the least potent cns stimulant

Question 5

central sympathomimetic agents

Answer 5

aka psychomotor stimulants
*b-phenethylamine moiety

Question 6

SAR: branching with lower alkyl groups on the carbon atom adjacent (a) to the amino nitrogen increases CNS rather than peripheral activity

Answer 6

central sympathomimetic agents

Question 7

SAR: Hydroxylation of the ring or hydroxylation on the β-carbon (to the nitrogen) decreases activity, largely by decreasing the ability to cross the blood-brain barrier

Answer 7

phenylephrine
central sympathomimetic agents

Question 8

SAR: Halogenation of the aromatic ring decreases sympathomimetic activity

Answer 8

central sympathomimetic agents

Question 9

3,4,5-trimethoxyphenethylamine

Answer 9

aka mescaline

Question 10

methylenedioxymethampethamine

Answer 10

MDMA
aka Ecstacy

Question 11

SAR: Methoxyl or methylenedioxy substitution on the ring tends to produce psychotomimetic agents, suggesting tropism for dopaminergic (D2) receptors

Answer 11

3,4,5-trimethoxyphenethylamine
aka Mescaline

CENTRAL SYMPATHOMIMETIC AGENTS

Question 12

SAR: Methoxyl or methylenedioxy substitution on the ring tends to produce psychotomimetic agents, suggesting tropism for dopaminergic (D2) receptors

Answer 12

Methylenedioxymethamphetamine (MDMA) aka Ecstasy

CENTRAL SYMPATHOMIMETIC AGENTS

Question 13

n-methylation

Answer 13

increases activity

Question 14

di-n-methylation

Answer 14

decreases activity

Question 15

shabu
has a very high abuse potential
more marked central and less peripheral action than dextroamphetamine.

Answer 15

Methamphetamine Hydrochloride

Question 16

appetite suppressants

Answer 16

Anorexiants
Phentermine HCl
Benzphetamine HCl
Phendimetrazine tartrate

Question 17

tends to produce sedation rather than excitation
mediated principally by central serotoninergic, rather than central noradrenergic mechanism
Anorexiant

Answer 17

Fenfluramine hydrochloride
3 Fluorine

Question 18

Indications include narcolepsy and attention-deficit disorder (ADHD)

Answer 18

Methylphenidate hydrochloride

Question 19

Problem:
↓Serotonin, Norepinephrine, Dopamine

Answer 19

depression

Question 20

dopamine and noepinephrine

Answer 20

catechol

Question 21

serotonin

Answer 21

indole

Question 22

Selective and Reversible inhibitor of MAO-A (RIMA)
antidepressant without producing hypertensive crises

Answer 22

Moclobemide