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PHARMACOLOGICAL
Rxvixws
Copyright
© 1980
by The
American
Society
for Pharmacology
and Experimental
Vol. 31, No. 4
Printed
in U.S.A.
Therapeutics
Index
Pharmacological
Reviews
Volume
31
1979
Acetylcholine,
effect
(fig.),
Acrosin,
on hypothalamic
CRF
content
pharmacology
in vitro
innervation
Adrenergic
nervous
tion,
8
of,
Adrenergic
of kidney,
system,
169
effect
on
sodium
reabsorption
and
stimulation
metabolites,
refractory
on,
cortico8terone
blockade,
and
of,
period,
171
their
role
of
excretion,
nervous
system
201
digitalis
on
conduction,
role
of nervous
system
in digitalis
of, from
Bethanechol,
effect
(fig.),
H.
blockade,
rabbit
liver
on hypothalamic
CRF
release
and
content
in vitro
plasma
See
kallikrein,
Trendelenburg
and
et al.,
kininogen,
5
from
rabbit
lung
studies,
metabolism,
Carcinogens,
effects
regiospecificity
in cultured
Cardiac arrhythmia,
Cardiac
output,
of cytochrome
hepatic
role of nervous
role
of
nervous
cells,
system
system
effects of digitalis, role
Cardiovascular
surgery,
heparin
in, 290
effect
effect
on,
system
on,
64
liver
on renal
tissue
cyclic
effect
on sodium
transport
effect
on sodium
reabsorption
metabolites
eliminated
metabolites,
lipophilicity
gation
intact,
nervous
in
170
the
179,
of,
kidney,
peptide
mapping
and
hydroxylation
Diet,
in, 229
study
in, 231
eliminated
from,
chemical
nature
of
factor,
266
evidence
hypothalamic
mechanism
and
microsomes,
forms
bethanechol
(fig.),
on
hypothalamic
of action,
after
stress
(fig.),
286
mutagen,
and
carcinogen
279
243
21
system,
systems,
of
25
30
sodium
nervous
Dopamine,
slices
261
pump,
260
264
297
51
52
mechanisms,
51
effects
of, in therapy
arrhythmiaa
system
(table),
heart
failure
of, 19, 52
cardiovascular
rate
conatanta
(table),
194
of congestive
79
in
effects
Dopaminergic
stimulation,
Drug conjugation,
factors
246
of, 253
content
287
of, 288
toxic cardiovascular
of, 259
and
in drug,
of,
metabolism,
systems,
nervous
therapeutic
in vitro
236
membrane,
(table),
286;
control,
drug
on
cardiovascular
253
nicotine,
liver,
microsomal
279
specific
receptor
neurocardiovascular
role
content
perfused
in
the
ofmultiple
290
electrogenic
of, 254
of
liver
specificity,
central
194
activity
acetyicholine,
277
of,
of, 288
and cardiac
of secretion
release
of,
electrophoresis
effects
on
afferent
releasing
cortiCotrophin
factor,
285
279
neurotransmitters,
41
poatsynaptic
membranes,
of, 256
releasing
(table),
multiplicity
of, within
studies,
influence
of, 256
quantification
284;
Digitalis
8
Corticotrophin
287
278
289
of,
and
efferent
on
(table),
conju-
246
releasing
detection
kidney
SDS-gel
of drug
286;
state
separation
substrate
rates
287
278
studies,
regio8peciflcity
metabolism,
169
preparations,
278
of forms
purification
185
of, in microsomal
278
studies,
partial
pig
194
system,
188
metabolism
oxidase
effect
Corticotrophin
effects
excretion,
174
283
286
studies,
microsomal
gland
in, 9
kinogenase,
control
and
central
of metabolites
whole,
mixed-function
Central
nervous
system
catecholamine
metabolites
digitalis
effects
on, 25
Coagulating
kallikreina
tiasues,
influence
drug
Chiorpromazine
in epithelial
of,
in (table),
hepatic
175
from
rate constants
for efflux
sodium
transport
and,
Cells
factors that
nucleotides,
283
282
oxidation:reduction
effect
175
of, 289
microsomes,
studies,
number
Catecholamines
intact,
(table),
studies,
kinetic
in, 52
on,
of
inhibition
128
(table),
microsomes
quantification
developmental
54
260
279
analysis
induction
in digitalis
of nervous
in, 126,
P.450
218
digitalis
in
Cardiovascular
205,
microsomes
(table), 283
and
multiplicity
Carcinogen
liver
multiple
forms,
279
in rabbit
microsomes,
179
(fig.),
of catecholamines
microsomes
in mouse
liver microsomes,
in rat liver microsomes,
mammalian
microsomal,
173
261
coagulation,
B#{246}nisch,
and
effect
260
stress
of, 289
probes,
287
rabbit
from
in human
stimulation
260
(fig.),
after
tissue,
by chemical
immunological
Beta-adrenergic
Blood
in renal
identification
effect
(fig.),
stress
concentration,
chromatography
genetic
62
stress
after
P.450
forms
renal
after
concentration,
nucleotides
estimation
61
Atrioventricular
on,
plasma
column
21
243
and
ionization
muscle
on,
content,
ACTH
Cytochrome
Alpha-adrsnergic
effect
of, 265
ACTH
plasma
Cyclic
excre-
170
Afferent
systems, digitalis
effecth
Age, influence
on drug metabolism,
Atrial
and
pituitary
inhibitors
Amine
release
261
actions
of, 79
actions of, 80
for
efflux
of
metabolites
of,
from
striatal
174
that
influence
rates
of, in intact
cells
(table),
298
INDEX
hydroxylation,
Drug
(table),
factors
that
influence
of, in intact
rates
factors
cells
regulating
isOlated,
246
Drug metabolism.
Drugs
Metabolism
See under
polyelectrolyte.
See Polyelectrolytes
transport
of, biotransformation
drug
L. B.
Jaques,
and,
in, 229
in, 233
and renal
Hypertension
reactions
metabolism
drug
metabolism
kauikrein,
Heparins-anionic
7
polyelectrolyte
drugs,
99
235
Kallikreins
Efferent
systems,
digitalis
effects
on,
bioregulatory
cell proliferation
30
Enzymes
anionic
effects
Ethanol,
Gilhis,
polyelectrolyte
of commercial
reaction
heparin
with,
110
and heparinoids
effect
metabolism,
240
on drug
Richard
A.,
and
John
A. Quest.
in the cardiovascular
Glucocorticoids,
effect
effects
on
corticotrophin
inhibition
of, 234
Glucuromdation,
regulation
of,
rate-controlling
role
of digitalis,
Gluconeogenesis,
Glutathione,
The
functions
on
(table),
of the
nervous
system
19
releasing
268
of,
of, 4
factors in
stimulation
Graefe,
to anionic
See Trendelenburg
rate,
role
Hemorrhage,
conjugation
of,
in intact
polyelectrolytes,
et al.,
nervous
105
179
in digitalis
system
spontaneous,
with
heparin,
M. See Trendelenburg
Henseling,
Heparinoids,
chemistry
See aLso under
Hepatic.
Hepatic
of
of,
effect
on,
drug
effects
of
104
metabolism
in, 205
in, 205
Heparin
anionic
polyelectrolyte
drugs,
99
anticoagulant
action of, 112
blocking
agents for, 121
chemistry
cells,
time
response,
heparin
unit
and,
system
subcellular
localization
effects
complex-forming
therapeutics,
monitoring
(table),
on
of use
(table),
(table),
and
106
diagnosis,
organs,
4
169
of,
and,
coagulation,
5
of,
properties
Stuart
141
L See Kim
inhibition
of cultured
use
119
of, as a drug,
109
anionic
polyelectrolytes
and, in biology,
mutes
and modes of administration,
117
spontaneous
hemorrhage
with, 122
thrombosis
related
to clinical
effects
of, 125
toxicity
of, 124
Hepatocytes
in cell culture,
drug
metabolism
in, 233
intact
related
metabolism
in,
236
cells
for
investigation
of
xenobiotic
206
use
of cultured
cells
for
investigation
of xenobiotic
me-
206
DNA
(table),
culture
of carcinogens,
repair
219
of, in short-term
mutagens,
cytochromes
and
toxins
suspension
on,
or
pri-
218
of, 213
of, 212
properties
of transformed,
221; (table),
221
regulation
of xenobiotic
metabolism
in, 214
“induction”
of microsomal
cytochromes
and monooxygenase
activity
in primary
culture
by xenobiotics,
chemicals,
cofactors,
and
136
metabolism,
aL, 169
et
of, 235
cells
effects
128
and
cells
monooxygenases
of, in therapy,
on drug
in bovine
145
of,
mary
cultured
111
129
of standardization
of oxygen
mast
microsomal
and
8
polyvalent,
blood
carcinogen-induced
125
pharmacokinetics
7
Kallikreins
metabolism,
Liver
enzymes
substances
surgery
thromboembolism,
tissues,
137
effect
See
vertebrate,
113
problem
kallilcrein,
mammalian,
of, 108
114
of
and,
(Kunitz)
plasma
tabOlism,
effects
5
of, 9
innervation
Lipogenesis,
Liver
biological
cardiovascular
inhibitor
Kininogenases.
Lines,
115
salts
and,
Kidney
126
actions on cells and tissues,
commercial,
in
in
in
in
60
and,
reproductive
and
heparinoids
coagulation,
prostaglandins,
functions
pharmacology
of, 110
properties
of, 106
complexing
2
blood
hypertension,
basophilic,
clinical
effectiveness
in cardiovascular
surgery,
in thromboembolism,
126
clinical
uses of, 133
commercial,
1
Leucocytes
of, 103
clotting
actions,
catecholamines
and sodium transport
in, 169
kallikreins
in, 9
Kidney
microsomes,
pig, cytochrome
P450 in, 286; (table),
286
Kim, Jin K., Stuart
L Linas,
and RObert
W. Schrier.
Catecholamines
and sodium transport
in the kidney,
169
Kininogen,
4
179
Liver
carcinogens
and,
kininogen,
adrenergic
122
et al.,
cells
cultured,
bioregulatory
10
kininogenases
-trypsin
Heart
with
and,
renin and, 7
urinary
and, 7
relation
K.-H.
10
renal
235
of,
Glycosaminoglycans,
development,
10
11
proteases
plasma,
241
and
and,
inhibitors
242
Glycolysis,
factors
serine
11
11
homology
other
proteases,
10
differentiation,
neoplasia
factor,
and,
of,
growth,
growth
111
serine
hormones
136
Liver
Liver
See
microsomes
cells.
(table),
also
Hepatic
215
cells
and
Hepatocytes
cytochrome
P450 in, 286; (table),
287
mouse,
cytochrome
P450 in, 286; (table), 286
pig, cytochrome
P.450 in, 286; (table), 286
rabbit,
cytochrome
P450
from
(table), 283
rat, cytochrome
P450
in, 284; (table), 285
Lung microsomes,
rabbit,
cytochrome
P450
from
human,
(table),
283
299
INDEX
Mast cells
basophilic
Oxygen,
of, 145
of, 141
functions
properties
metabolism
on drug
effect
Pancreas,
kallikrems
effect on
drug
Pentobarbitone/morphine,
influence
of diet,
inducing
in
cultured
of carcinogens
intermediary
and,
in intact
hepatocytes,
in intact
ethanol
effect
hepatic
cells,
cells,
interaction
regulating
on,
and age, 243
agents,
factors,
Plasma
240
heparin
of,
and,
relationship,
non-mast
reactions
239
oxidation,
Quest,
function
oxidation
on,
Rate
for the investigation
cells
of, 206
efflux,
consequences
distribution
of, into multiple
rate
constants
and
of catecholamines
the rate constants
compartments,
for
(table),
for,
195
190
effect
and renal kallikrein,
on,
110
52
7
Gillis and Quest,
A. See
19
of metabolites
H-dopamine
from
between,
and phenethylamines,
striatal
for efflux
constants
of,
digitalis
of amine
194
51
201
studies, 170
7
physiology,
effect
on,
and denervation
and renal kallikrein,
Reserpine,
effect
metabolites,
stimulation
nerve,
195
179, 185
slices
(table),
180
to measure,
mechanisms,
excretion
Reproductive
rate
digitalis
of differences
Renal
Renal
llama
189
phenethylamines,
106
136
procedures
used
tables, 186, 190
188
between
of,
membranes,
John
Receptor
of,
110
108
consequences
catecholamines
206
194
lipophilicity
of differences
with,
constants
Metabolites
carrier-mediated
catechola.mine,
reactions
cell, including
heparin,
149
with plasma proteins and enzymes,
for effluz
in cell cultures from liver, enzymology
of, 209
in hepatocyte
suspensions
from rats (table), 210
regulation
of, in cultured
liver cells,
214
studies
with mammalian
and vertebrate
liver cells,
in, 5
234
xenobiotic
cultured
268
185
relationship
235
mixed
for
in nutrition,
179,
99
Poatsynaptic
changes
to acute
factor,
of,
101
in biology,
in, 290
releasing
of metabolites
efflux
polyelectrolyte
properties
complexing
determination
236
for
anionic
Prostaglandins
secondary
with mixed-function
effect
of substrates
alteration
of,
anionic
of,
chemistry
on corticotrophin
constants
inhibitors
proteins,
Polyelectrolytes,
intermediary
efflux
rate
kallikrein
Plasma,
230
229
in hepatocytes
in cell culture, 233
inhibition
by direct binding and inactivation,
in isOlated hepatocytes,
233
in perfused
organs,
231
regiospecificity
of cytochrome
P450
energy,
and mixed-function
oxidation,
heparin,
119
effect
Phenethylamines
205
(fig.),
fac-
releasing
COFtICOtFOphIn
267
tor,
effects
236
hepatocytes,
9
in,
Pentobarbitone/chlorpromazine
Metabolism
chronic
in intact
and
leucocytes
kallikreuze,
role
on corticotrophin
in, 8,9
releasing
factor,
265
185
procedures
used to measure rate constants
rate constants
for effluz of,
from striatal
slices (table), 194
of catecholamines
and phenethylamines,
table, 186
Mixed-function
oxidase
Mixed-function
oxidation
effect
study,
in whole
for efflux
cells,
for, on intermediary
changes
effects
Nervous
Schrier,
231
Serine
Since,
metabolism,
234
metabolism
secondary
to
cultured
of cytochrome
liver
P.450
in, 290
218
cells,
in therapeutic
sodium
on
effects
cardiovascular
in toxic cardiovascular
Neurotransmitters,
and
reabsorption
digitalis,
of
excretion,
170
pump,
in cultured
electrogenic,
hepatic
reabsorption
and
and catecholamines
Sodium
transport
catecholamines
and, in
cells,
205
effect on, 50
effect of adrenergic
digitalis
excretion,
nervous
system
170
on,
the
kidney,
169
catecholamines
of
174
on,
actions
digitalis
of
effects
of
digitalis,
on,
digitalis
80
(table),
releasing
hypothalaxno-pituitary
adrenocorticotrophic
Sulfation,
79
and content
release
in vitro
in,
in
intermediary
relationship
secondary
metabolism
to mixed-function
oxidation,
to
235
acute
of,
etiology
Toxin
of
of heparin, 124
effects, on cultured
Trendelenburg,
rate
related
effect
Oxidase,
mixed-function.
on corticotrophm
releasing
See Mixed-function
260
activity
U.,
constants
factor,
to
clinical
effectiveness
liver
cells,
for
the
efflux
effects
of hepai,n
in
rats
before
of heparin,
in,
125
126,129
218
H. B#{246}nisch, K..H.
and phenethylamines,
Opioids,
factor (fig.),
242
clinical
Thromboembolism,
Toxicity
261
alteration
regulation
Thrombosis,
41
CRF
effect on corticotrophin
and after (fig.), 263
19,52
actions
effect on hypothalamic
changes
in, 9
(kinogenases)-a
group of serine proteases
with bioregulatory
actions,
1
Robert
W. See Kim et aL, 169
proteases
with bioregulatory
actions (kallikreins), 1
Alphonse
E., and Henry C. Pitot Drug metabolism
and effects
Kallikreins
in epithelial
tissues,
effect
Sperm, kallikreins
in, 9
of,
(fig.),
kallikreins
M.
Stress
effect
Nicotine,
glands,
Sodium
Sodium
235
nutrition,
regiospecificity
of, on
in cardiovascular
Nutrition,
179
system
adrenergic,
role
in
metabolism,
Mutagens,
Salivary
Schachter,
regulation of, in intact cells, 236
relationship with alteration in intermediary
acute
180
of carcinogens
of substrates
Mutagen
of,
Graefe,
of
metabolites
and
M.
Henseling.
of catecholamines
179
267
oxidase
Vascular
tone,
role
of nervous
system
in digitalis
effect
on,
54
The