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Principles of Drug Action > Exam 2 > Flashcards

Exam 2 Flashcards

1
Q

cox enzymes convert ___ into _____

A

convert aracadonic acid/ prostaglandin H2

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2
Q

what cofactor goes with alcohol dehydrogenase?

A

Zn2+

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3
Q

difunisal is

A

a cox inhibitor

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4
Q

frovatriptan is a

A

5-HT1 receptor agonist

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5
Q

what kind of enzyme is farnesyl diphosphate synthase?

A

transferase

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6
Q

farnesylated proteins are incorporated into proteins such as ____ and have effects on signaling through these

A

small GTPase proteins

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7
Q

EGFR complex with erlotinib is ___ inhibitor with respect to ATP

A

a competitive inhibitor

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8
Q

ketanserin is

A

a 5-HT2 antagonist

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9
Q

pamidrone is

A

a 2nd generation bisphosphonate

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10
Q

what enzyme do bisphosphynate drugs for the treatment of osteoporosis inhibit?

A

farnesyl diphosphate synthase

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11
Q

panitumumab is

A

an antibody to EGFR. Prevents EGFR signaling

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12
Q

PKC is

A

a serine/threonine kinase

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13
Q

for a noncompetitive inhibitor, Km

A

appears unaltered

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14
Q

Gefitinib is

A

a small molecule EGFR inhibitor

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15
Q

diltiazem is a _____ ______

A

benzothiazepine calcium channel blocker

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16
Q

alendronate is a ___ generation bisphosphonate

A

2nd

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17
Q

Cox __ inducible, primarily in __ during __

A

2/ macrophages/ inflammation

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18
Q

methyl salicylate is

A

a cox inhibitor

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19
Q

naratriptan is

A

a receptor 5-HT1 agonist

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20
Q

celecoxib is

A

a Cox inhibitor

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21
Q

a ________ is exposed in Cox-2, allowing for specificity

A

hydrophobic pocket

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22
Q

raloxifene is

A

an estrogen receptor antagonist

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23
Q

raloxifene is

A

a bisphosphonate

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24
Q

cetuximab is

A

an antibody to EGFR. prevents EGFR signaling

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25
Q

risedronate is ____ with respect to IPP

A

un-competitive

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26
Q

the NR3 subfamily includes the

A

steroid hormone receptors

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27
Q

mianserin is

A

a 5-HT2 antagonist

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28
Q

what cofactor goes with cytochromes?

A

Fe3+ or Fe2+

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29
Q

zolendronate is

A

a 3rd generation bisphosphonate

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30
Q

tamoxifen is

A

an estrogen receptor antagonist

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31
Q

risendronate is _____ with respect to GPP

A

competitive

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32
Q

Cox___ is constitutively expressed in most tissues

A

1

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33
Q

what cofactor goes with DNA polymerase?

A

Mg2+

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34
Q

sumatriptan is a

A

5-Ht1 receptor agonist

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35
Q

cyclooxygenases are also known as

A

prostaglandin H synthases

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36
Q

what cofactor goes with cytochrome oxidase?

A

Cu2+ or Cu+

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37
Q

prosatglandins bind to

A

GPCRs

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38
Q

what cofactor goes with carbonic anhydrase?

A

Zn2+

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39
Q

ATP –> ADP +Pi = what change in delta G?

A

-7.3 kcal/mol

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40
Q

asprin and ibuprofin are ______ inhibitors

A

Cox1 and Cox2

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41
Q

Erlotinib is

A

a small molecule EGFR inhibitor

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42
Q

what cofactor does HMG-CoA reductase use?

A

NADH

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43
Q

for an uncompetitive inhibitor, Km

A

is decreased

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44
Q

what cofactor goes with pyruvate phosphokinase?

A

Mg2+

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45
Q

rizatriptan is a

A

5-HT1 receptor agonist

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46
Q

temsirolimus = ______ and is

A

Torisel/ mTOR serine/ threonine kinase inhibitor

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47
Q

vorinostat is used to treat

A

T cell lymphoma

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48
Q

_______ ion channels are very important in the heart

A

voltage gated

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49
Q

mTOR is

A

a serine/threonine kinase

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50
Q

teriparatide is

A

a bisphosphonate

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51
Q

nifedipine is a _______ _______

A

dihydropyridine calcium channel blocker

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52
Q

do antineoplastic compounds bind covalently?

A

yes

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53
Q

3rd generation bisphosphonates have

A

aromatic groups that increase affinity for farnasyl diphosphate synthase

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54
Q

Src is

A

a cytoplasmic tyrosine kinase

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55
Q

do nitrosoureas bind DNA covalently?

A

yes

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56
Q

The R1 position of a bisphosphonate must be ___ –> this is necessary for interacting with the enzyme & with bone->”bone hook”

A

OH (hydroxyl group)

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57
Q

risedronate is a ____ generation bisphosphonate

A

3rd

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58
Q

alendronate is

A

a bisphosphonate

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59
Q

histone deacetylases are _____ enzymes

A

hydrolase

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60
Q

ENT transports

A

neucleotides

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61
Q

_______ increase bone mineral density

A

bisphosphonates

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62
Q

does mitomycin C bind DNA covalently?

A

yes

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63
Q

bisphosphonates decrease ______ activity

A

farnasylPP synthase and ultimately osteoclast

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64
Q

calcitonin is

A

a bisphosphonate

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65
Q

vorinostat = ______, also called ____. It is _____

A

Zolina/ SAHA/ a HDAC inhibitor

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66
Q

ibandronate is

A

a 2nd generation bisphosphonate

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67
Q

carcinomas are derived from ____ cells

A

epithelial

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68
Q

flecainide is a class ___ _______ and it is _____ wrt association/dissociation

A

Ic/ sodium channel blocker/ slow

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69
Q

chlorambucil forms

A

between strands cross-links

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70
Q

JAK-2 is

A

a cytoplasmic tyrosine kinase

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71
Q

imatinib = ______ and is

A

gleevec/ Abl tyrosine kinase inhibitor

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72
Q

Can GPCRs directly modify ion channels?

A

yes

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73
Q

exemestane is

A

an aromatase inhibitor

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74
Q

phosphorylation by ___ or ___ on the inside of the cell at the voltage gated ionchannel can affect the magnitude of voltage needed to affect a change or can inactivate the channel

A

PKA/ PKC

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75
Q

Her-2 is

A

a receptor tyrosine kinase

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76
Q

the ____ transmembrane domain is most important for determining change in voltage - change in conformation of ___ transmembrane domain leads to conformational change and opening of pore

A

4th/ 4th

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77
Q

crizotinib = ______ and is

A

Xalkori/ ALK tyrosine kinase inhibitor

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78
Q

_______ ion channels are very important in the nervous system

A

ligand-gated

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79
Q

Gleevec is a drug for

A

chronic myeloid leukemia

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80
Q

AKT is

A

a serine/threonine kinase

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81
Q

JaK-2 is

A

a cytoplasmic tyrosine kinase

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82
Q

5-fluorouracil targets

A

thymdylate synthase

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83
Q

vemurafenib is a drug for

A

late stage melanoma in patients with a V600E mutation

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84
Q

topotecan targets

A

topoisomerase

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85
Q

vemurafenib = ________ and is

A

Zelboraf/ B-Raf serine/threonine kinase

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86
Q

histone deacetylases remove acetyl groups from _______ amino acid on a histone

A

lysine

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87
Q

Abl is

A

a cytoplasmic tyrosine kinase

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88
Q

etoposide targets

A

topoisomerase

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89
Q

exemestane is used for ER positive breast cancer if disease progresses after _____ therapy

A

tamoxifen

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90
Q

what kind of enzyme is aromatase?

A

oxidoreductase

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91
Q

acetylation removes _____ on the histones, so they ___

A

the positve charge/ interact less closely with DNA

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92
Q

cyclophosphamide targets

A

DNA

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93
Q

____________ are characteristic of irreversible inhibitors

A

covalent bonds

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94
Q

methotrexate targets

A

dihydrofolate reductase

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95
Q

dihydropyridine calcium channel blockers act on the _______ of the cell

A

outside

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96
Q

sarcomas are derived from ____ cells

A

mesencymal

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97
Q

exemestane ________ binds aromatase

A

irreversibly

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98
Q

dexamethasone targets

A

glucocorticoid receptor

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99
Q

IGF is

A

a receptor tyrosine kinase

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100
Q

doxorubicin targets

A

DNA

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101
Q

cisplatin is

A

an alkylating agent

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102
Q

lidocane is a class ______ _____ and it is _____ wrt association/dissociation

A

IB/ sodium channel blocker/ fast

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103
Q

melphalan is _____

A

an alkylating agent

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104
Q

what percent of proteins are druggable?

A

10-15

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105
Q

many drugs that covalently bind DNA are _______ agents that target __ of ____ that is exposed in the ___ groove of DNA

A

alkylating/ N7/ guanine/ major

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106
Q

what percent of proteins are disease modifying?

A

10-15%

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107
Q

purines are more ___ than pyrimidines

A

neucleophilic

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108
Q

quinidine is a class _____ _________ and it is ___ wrt association/dissociation

A

Ia/ sodium channel blocker/ intermediate

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109
Q

melphalan forms

A

between strands cross links

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110
Q

chlorambucil is

A

an alkylating agent

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111
Q

distamycin binds ___ with ______

A

the minor groove/ hydrogen bonding and hydrophobic interactions

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112
Q

calcium channel alpha 1 D is inhibited by

A

phenylalkylamines

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113
Q

do intercalators bind covalently?

A

no

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114
Q

what is the primary receptor type in the heart?

A

B1

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115
Q

calcium channel blockers work by

A

blocking the part of the cardiac action potential that depends on calcium influx, and also by causing blood vessels to dilate

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116
Q

parasympathetic: ___ preganglionic nerves and _____ post ganglionic nerves

A

long/ short

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117
Q

in vessels, cAMP cause _____ while PI causes ____

A

vaso-relaxation/ vasoconstriction

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118
Q

calcium channel alpha 1 C is inhibited by

A

dihydropyridines

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119
Q

do groove binders bind covalently?

A

no

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120
Q

calcium channel alpha 1 F is inhibited by

A

benzothiazepines

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121
Q

calcium channel alpha 1 D are in

A

endocrine

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122
Q

do nitrogen mustards bind DNA covalently?

A

yes

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123
Q

nicardipine is a ________ _____

A

dihydropyridine calcium channel blocker

124
Q

saxitoxin is

A

a sodium channel blocker

125
Q

dynemicin A does what?

A

binds to DNA and cleaves it

126
Q

calcium channel alpha 1 F are in

A

retinal

127
Q

Is saxitoxin extracellular or intracellular?

A

extracellular

128
Q

do platinum complexes bind DNA covalently?

A

yes

129
Q

the _____ system has a single nerve, no ganglia

A

somatic

130
Q

class IA sodium channel blockers are __ and __

A

moderate/ elongate cell recovery after action potential

131
Q

ABC transporters are ____ of ____

A

dimers/ 6 helices

132
Q

what is the major use of calcium channels as drug targets?

A

to decrease blood pressure

133
Q

P-gp= ___ = _____

A

ABCB1/ MDR1

134
Q

verapamil is a _______ _______

A

phenylalkylamine calcium channel blocker

135
Q

class IB sodium channel blockers are ____ and ____

A

weak/ shorten cell recovery after action potential

136
Q

The ATP binding domain of an ABC transporter is

A

inside the cell

137
Q

phenylalkylamine calcium channel blockers act on the _______ of the cell

A

inside

138
Q

class IC sodium channel blockers are ____ and _____

A

strong/ cause no change to time for cell recovery after action potential

139
Q

Penicillans are transported by

A

OAT

140
Q

cis platin forms

A

intrastrand cross links

141
Q

zidovudine is transported by

A

ENT1

142
Q

folic acid is transported by

A

OAT

143
Q

Voltage gated ion channels have ___ groups of _____ transmembrane domains

A

4/6

144
Q

calcium channel alpha 1 C are in

A

cardiac muscle

145
Q

minor groove binders bind _____ rich regions because

A

AT/ 2-amino group of guanine prevents binding to GC regions

146
Q

dynemicin A combines ___ and ____

A

intercalation/ minor groove binding

147
Q

Sodium channel blockers are used to treat ___, ____, ___ and as ____

A

cardiac arrhythmia/ high blood pressure/ epilepsy/ local anesthetics

148
Q

netropsin binds _____ with ______

A

the minor groove/ hydrogen bonding and hydrophobic interactions

149
Q

calcium channel alpha 1 S are in

A

skeletal muscle

150
Q

metformin is transported by

A

OCT

151
Q

sweat glands are unique because

A

though they are part of the sympathetic nervous system, the postganglionic nerves secrete Ach instead of NE

152
Q

prostaglandins are transported by

A

OAT

153
Q

_____ stabilize the inward facing state of PEPT1

A

extracellular salt bridges between arginine and glutamic acid

154
Q

NSAIDs are transported by

A

OAT

155
Q

choline is transported by

A

OCT

156
Q

what kind of receptor is on sweat glands?

A

muscarinic

157
Q

P-gp expression is regulated by

A

nuclear receptors

158
Q

what percent of proteins interact with used drugs?

A

2%

159
Q

PepT1 takes an amino acid or a small peptide and couples its transport to ___

A

H+ symport

160
Q

nicotine is transported by

A

OCT

161
Q

valacyclovir is a ______ substrate that is hydrolyzed to acyclovir once in the cell

A

Pept1

162
Q

what neurotransmitter is involved with renal vascular smooth muscle?

A

dopamine

163
Q

Zidovudine =

A

AZT

164
Q

tight and narrow protein interactions give the ___ affinity

A

best

165
Q

dopamine is transported by

A

OCT

166
Q

________ activity stimulates glucose release by the liver

A

sympathetic

167
Q

p53 binds to MDM2 using a ______, _____ binding cleft

A

deep/ hydrophobic

168
Q

what kind of receptor is associated with parasympathetic nervous system?

A

muscarinic

169
Q

do SLC transporters require ATP to function?

A

no

170
Q

taxol binds tubulin via

A

hydrogen bonds and hydrophobic interactions

171
Q

SLC transporters can be ___ or _____

A

facilitative transporters/ secondary active transporters

172
Q

ACh receptor(s) of the CNS:

A

M & N

173
Q

blood goes from the liver to the ______ heart, to the lungs, to the _______ heart

A

right/ left

174
Q

OATP1 is _______ that ___

A

an SLC transporter/ absorbs statin drugs

175
Q

ACh receptor(s) of the autonomic nervous system:

A

M & N

176
Q

Do ABC transporters require ATP to function?

A

yes

177
Q

in humans, ABC transporters generally

A

export

178
Q

binding of ____ to ______ makes _____ inactive

A

Bcl-2, Bax/Bac, Bax/Bac

179
Q

Bax/Bac precipitates

A

apoptotic cascade when it is free

180
Q

cancer cells have up-regulated _____

A

Bcl2

181
Q

taxol blocks

A

tubulin disassembly

182
Q

list the layers on your head:

A

skin, periosteum, bone, dura mater, arachnoid mater, subarachnoid space (with CSF), pia mater, brain

183
Q

_____ are the resident immune cells of the CNS

A

microglia

184
Q

beta-tubulin binds

A

GTP that hydrolyzes to GDP

185
Q

the _________ cells have tight junctions, making an active process necessary for the formation of cerebrospinal fluid

A

choroidal ependymal

186
Q

___ form the epithelial lining of the ventricles in the CNS

A

ependymal cells

187
Q

cAMP and PI are complementary when they both work to

A

stimulate glucose release from the liver

188
Q

vinca alkaloids block

A

tubulin addembly

189
Q

ACh receptor(s) of the NMJ:

A

N

190
Q

Cytarabine =

A

AraC

191
Q

what three things do muscarinic acetylcholine receptors do?

A

inhibit AC/ stimulate PLC/ regulate K+ channels

192
Q

organophosphates and carbamates are used as

A

AChE-I

193
Q

alpha-tubulin binds

A

GTP that does not hydrolyze

194
Q

_______ provide metabolic support for the neurons in peripheral ganglia

A

satellite cells

195
Q

You can counteract excessive Bcl production with

A

BH3 binding ligand

196
Q

sympathetic: ____ preganglionic nerves and _____ post ganglionic nerves

A

short/ long

197
Q

Cytarabine is transported by

A

ENT1

198
Q

p53 blocks

A

BCl-2 function

199
Q

p53 and ____ keep each other in check. In cancer you have too little p53 and too much _____

A

MDM2/ MDM2

200
Q

COMT is found

A

outside the cell, in the synapse

201
Q

what does cevimeline do and what is it?

A

increases salivation/ M3 agonist

202
Q

_____ receptors: renal vasculature, dilation of blood vessels

A

D1

203
Q

Ergots are

A

alpha blockers

204
Q

______ receptors are involved in regulation of the tone of the CNS

A

alpha 2

205
Q

Does B1 increase renin release?

A

yes

206
Q

_____ receptors: fat cells, metabolic effects

A

B3

207
Q

B2 receptor agonists cause broncho____

A

dilation

208
Q

why are long acting beta agonist long acting?

A

they have a long side chain that binds to a site near the receptor - if the drug comes off it is still nearby and so has the opportunity to come back and bind again

209
Q

AChE is a ___ protease - the ____ group on the ____ acts as a ____. The ___ group is transferred to ____, then water breaks that bone

A

serine/ hydroxyl/ serine/ neucleophile/ acyl/ serine

210
Q

Alpha 1 agonists have _____ action on the heart, and they ___ heart rate.

A

Indirect/ decrease

211
Q

Nitrous oxide ______ the GI tract

A

relaxes

212
Q

Orthostatic hypotension is a side effect of ____

A

A1 blockers

213
Q

_____ brings a positively charge group to stabilize the negative charge on oxygen, allowing carbon to act as ____

A

histidine/ an electrophile

214
Q

Which receptor subtypes may be associated with early onset of smoking?

A

A5B4

215
Q

What is the sympathetic effect of a ganglionic blocker?

A

vasodilation

216
Q

how does aricept (donepezil) interact with AChE?

A

non covalent weak interactions, no acylation step

217
Q

phenylethanolamine n-methyltransferase changes norepinephrine to

A

epinephrine

218
Q

What is the most common form of nicotinic receptor subtypes?

A

A4B2

219
Q

irreversible AChE-Is have

A

phosphate group

220
Q

dopamine, epinephrine and norepinephrine are metabolized by _____ and _____

A

MAO/ COMT

221
Q

alpha stimulation in the brain

A

reduces sympathetic activity

222
Q

small groups on the alpha carbon of a catecholamine are tolerated and have the effect of

A

decreasing degradation by MAO

223
Q

muscarinic stimulation in the CNS

A

increase sympathetic activity

224
Q

nicotene’s positive charge is

A

reversible because it is hydrogenated

225
Q

what system provides homeostatic regulation that is appropriate for whatever is going on in the body at that point in time?

A

the limbic system

226
Q

the hypothalamus influences a lot of _____ function

A

autonomic

227
Q

antimuscarinics ______ sweat

A

reduce

228
Q

muscarine has an OH group - can it cross the blood brain barrier?

A

yes

229
Q

alpha substitution of a catecholamine ___ the activity of direct-acting compounds and ______ the activity of indirect-acting compounds

A

reduces/ increases

230
Q

GABAa receptor =

A

chloride channel

231
Q

MAO is found

A

in the cell, in the mitochondria

232
Q

in the AChE active site, there is a ____ hole looking for a ______ charge

A

negative/ positive

233
Q

The _____ receptor in pain pathways responds to noxious stimuli, chemicals, and it is a Calcium channel

A

TRV1

234
Q

Oxidative stress from inflammation, tissue injury modulates ___ which increase sensitivity of receptor

A

sulfhydryls

235
Q

beta carbon hydroxylation of a catecholamine ____ activity of direct-acting agents, especially those acting at _____ receptors

A

increases/ Beta

236
Q

direct desensitization effects:

A

change receptor number or sensitivity

237
Q

indirect desensitization effects:

A

change sensitivity

238
Q

The alpha 1 receptor acts via __ to increase ___ resulting in ___

A

phosphoinositide pathway/ increase intracellular concentration of calcium/ cause vasoconstriction

239
Q

________ –>Renin–> _____ –>Angiotensin Converting Enzyme –> ______

A

Angiotensinogen/ Angiotensin I/ Angiotensin II

240
Q

repeated cocaine decreases DA transporter ___

A

mRNA

241
Q

At physiological concentrations, epinephrine primarily targets____. At high concentrations _____

A

B2 receptors/ it looses specificity and affects alpha

242
Q

activated receptor-hormone complex alters

A

gene expression

243
Q

B1 works indirectly to increase blood pressure through

A

stimulating renin which is involved in the production of Angiotensin II, which causes an increase in blood pressure

244
Q

would you use epinephrine or norepinephrine as a nasal decongestant?

A

epinephrine

245
Q

Dopamine ________ heart contractility and ________ heart rate

A

increases/ doesn’t change

246
Q

what is the parasympathetic effect of a ganglionic blocker?

A

tachycardia, constipation, urine retention

247
Q

epinephrine has more _____ activity than norepinephrine

A

neta

248
Q

Distributive (_________) shock: ___, ___, and _____ shock.

A

vasodilatory/ septic/ anaphylactic/ neurogenic

249
Q

alpha 2 on presynaptic neuron acts to ____

A

reduce the release of NE

250
Q

D1 receptor is a ____ receptor that causes activation of ____, It acts on blood vessels to cause _____, and _____ blood supply to the kidney

A

G protein coupled/ AC and cAMP/ vasodilation/ increase

251
Q

muscarinic agonists should have ____ atom capable of H bond

A

O

252
Q

Beta 1 signaling: In heart, ____ activates __ that _______ causing _____

A

cAMP/ PK-A/ L-type calcium channels/ increased calcium entry into the cells

253
Q

Acetylcholine is a neurotransmitter in the

A

CNS & PNS

254
Q

B1: G_ protein coupled

A

s

255
Q

In Beta 2 signaling in the vascular smooth muscle, _____ inhibits ____ causing _____

A

cAMP/ myosin light chain kinase/ less contractile force

256
Q

atropine and scopolamine are

A

antimuscarinics

257
Q

what are the three parts to acetylcholine?

A

acetyl group, ethylene bridge, quaternary amonium group

258
Q

Beta 2 blockers found presynaptically

A

facilitate NE release

259
Q

Dopamine B-hydroxylase changes dopamine to

A

norepinephrine

260
Q

The size of alkyl groups on the N of a muscarinic agonist should not exceed ___

A

the size of a methyl

261
Q

Is ACh water soluble?

A

Yes, very much so

262
Q

will muscarinic agonists increase motility of GI and urinary tract?

A

yes

263
Q

M2 –>

A

reduced heart rate

264
Q

effective catecholamins should have ____ configuation at the beta carbon

A

R

265
Q

for catecholamines, the substituent on the N

A

strongly influences receptor subtype affinity

266
Q

what does MAO do to norepinephrine?

A

it replaces the amine with an aldehyde

267
Q

As you increase the size of the R group on the N of a catacholamine, you ______ the beta activity and _____ the alpha activity

A

increase/ decrease

268
Q

methacholine chloride is selective for

A

muscarinic receptors

269
Q

for a catecholamine, there should be at least one __ on the N

A

H

270
Q

are epinephrine or norepinephrine orally bioavailable?

A

no

271
Q

B2: G__ protein coupled

A

s

272
Q

M3 –>

A

bronchiolar constriction, GI contraction, vascular relaxation, increased secretions

273
Q

NO diffuses from ____ to _____ and activates ______, which produces __, resulting in ___

A

endothelial cells/ smooth muscle cells/ guanylate cyclase/ cGMP/ dilation of blood vessel

274
Q

hydroxyl substituent at C3 of a catecholamine ring favors ____ selectivity

A

alpha

275
Q

what can you give to treat myasthenia gravis?

A

an acetylcholinesterase inhibitor

276
Q

is d-tubocurarine depolarizing?

A

no

277
Q

does a carbamate terminus on acetylcholine make it selective? more resistant to nydrolysis?

A

no, yes

278
Q

solanaceous alkaloids are

A

Ach antagonists

279
Q

N1 –>

A

skeletal muscle, contraction

280
Q

ganglionic blockers should be able to cross

A

the blood brain barrier

281
Q

as you increase electron donors on the carbonyl group of acetylcholine, you

A

slow down electrophilic attack

282
Q

acetylcholine receptors have a ____ pocket as well as lots of ____

A

negative/ hydrophobicity

283
Q

d-tubocurarine is

A

a neuromuscular junction blocker

284
Q

would an ideal nmj blocker be rapidly eliminated?

A

yes

285
Q

does beta carbon hydroxylation of a catecholamine reduce the dutation of action?

A

yes, somewhat

286
Q

the most important effect of hydrozyls on the ring of a catecholamine is

A

to provide direct action at postsynaptic receptors

287
Q

unlike other antimuscarinic agents, _____ acts as a CNS depressant at therapeutic doses

A

scopolamine

288
Q

tyrosine hydroxylase changes tyrosine to

A

DOPA

289
Q

you can use ________ for asthma treatment

A

anticholinergics

290
Q

succinylcholine chloride is a ____ _____

A

depolarizing NMJ blocker

291
Q

In myasthenia gravis, ________ is produced and ________ resulting in ____

A

an antibody to the nicotinic receptor/ acethylcholine cannot stimulate the receptor/ muscle weakness and paralysis

292
Q

catecholamine synthesis starts with

A

tyrosine

293
Q

Atropa belladonna is

A

an ACh antagonist

294
Q

Ar-NH - imidazoline ring =

A

alpha 2 agonist

295
Q

_________ prevents the release of acetylcholine

A

botox

296
Q

ganglionic blockers act in the

A

CNS

297
Q

muscarine’s positive charge is

A

permanent because it has 4 R groups

298
Q

would an ideal NMJ blocker be depolarizing?

A

no

299
Q

non H-bonding substituents on the ring of a catecholamine tend to

A

produce antagonists

300
Q

would an ideal nmj blocker be metabolically inactivated?

A

yes

301
Q

AR - CH2 - imidazoline ring =

A

alpha1 agonist

302
Q

Aromatic L-amino acid decarboxylase changes DOPA to

A

dopamine

303
Q

AChE has a _____ pocket, and a ____ pocket

A

negatively charged/ hydrophobic

304
Q

A2: G_ protein coupled

A

i

305
Q

hydroxyl substituent at C4 of a catecholamine ring favors ____ selectivity

A

beta

Principles of Drug Action (1 decks)

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