1955_boyd_1539_1.pdf

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@ri_nal
and file card
(§102a)
M
500 metabolism;
antagonism
to serotonin(§90e
VX LSD
No.73
_,
E.S.,
ROTHLIN,
E.,
BONNER, J.F., SLATER, I.H., HODGE, H.C.
(Dept._harmacol.,
Univ.Rochester, N.Y., and Sandoz Co., Switzerland)
A_llmlnary
studies on
the
metabolism of _ysergic acid
diethy!_m!de.
J.Pharmacol.Exper.Therap. i15,6 (1955).
Radioactive
_ic acid diethylamide
chain
with
Switzerland)
four female
(LSD-25),
labeled
ly_er-
in the side
C _, (supplied
by the
Sandoz
Co.,
was
giveni.p,
ata
doseof 1 mg./kg, to
rats which were maintained
in
a
me-
tabolism
apparatus
for
12 hours. The
total
radio-
activity
excreted
amounted
to
about
7% of the
administered
dose, about half of this being in the
expired
air, the rest in the urine and feces. The
C
_4 content
of the tissues
of these rats was low
except
for the g.i. tract which contained
8.5% of
the
administered
dose. The contents
of the g.i.
tract
contained
48.5% of the
administered
dose.
In a second experiment
invo|ving
two rats under
similar conditions,
71.2% of the administered
dose
was found in the contents
of
the g.i.
tract.
Since LSD is a very l)otent inhibitor
of seroto-
nin,
it has been possible
to
assay
mice
for serotonin
antagonism
hver
extracts
o!
in
the
isolated
uterus of castrated
and
estrogen
pretreate(l
rals.
Assayed
in this
way,
biologically
active amounts
of 5-10 microgm, of LSD per gin. of liver were cal-
culated
to be present
in the liver 1 hour after i.v.
injection
of 700 microgm./animal.
Experiments
involving
the growing of ergot on
rye
in a C_402 atmosphere
have been started in an
attempt
to
obtain ]ysergic acid derivatives
labeled
in
the
ring structure.
Although
no
alkaloids
have
•
yet been isolated,
is
been obtained.
radioactive
sclerotia
have
w8 (K7302)
NKT/bh
555 _)_o

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