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Raney , ~ .
4 Dig al, 8 MMi dees ht se
Whal a druq does to a oe A
When a dtvq es to the body, ik then starts inte-
yacting with cell receptors which in turn Seads be a
formation of agnal and bhis signal bb a ene
yeac ions PlGmntela results 7 SOE vidlo gical effect ©
Giana can rel) DNA to stop replicating- Cells
Fferent receptors which
unique *¢ Sponses:
p
£
wn our body ipve 0 Ne of ai
when
TcAMP feamp — TeAMP
3- ENZYME LINKED
RECEPTORS ”
On A ad
receptor just G- se receptor have extracdular
binding sites where the Viganel typically Harmone or
a growth factor can attach and this stimulates
ero numa et nside the cebl- Most enzyme linked
receptors are Tursine kina type which Simply mean
Rhey display Kinase ackue os and the amino acid
“his
“Tyrosine involved in Uhat- So the way they works is
when Sigane binds to 2 of theereceplors, it causes
Grrnational change Unat results in aggregation of
both hese receptors- One the dimer is formed, Tyrosine
odnes om activated and causes PIP to become fOP
in autophosphorylation of the receptors.
cine fixed up with Phosphate qroup, » dif fer-
ms come up and attach themselves to
Tyrosine This in turn causes confirmational
ched protein ultimatdy Seading to
ati Hat produces celular response
SS, in
ae - ea ~ , Mavary (blulaw Raper ing
6
5
9
¢w .
4. INTRACELLULAR
RESPONSE "
We
; : pinside
is receptor is Yocatecl entirely eh aatl. vata tae on
cell membrane Therefore, the” Ligand has 1st bo cross
the Lipid membrane and once inside the cell, it then
binds to the veceptor Now the activated Vigand receptor
complex Can move into the nucleus, bind to DNA & reqplate
gene expression ullimatdy leading to the synthesis of specific
Ligand Ba
proteins
Ce
Memo sane
"LIFE CYCLE OF
RECEPTORS”
Pray
ise DNA contains code which
is used bo synthesize
sp sae from clifferent receptor assemble , Ona avemble
Ure receptors get embedded into the cell, membrane and
tan recieve & a rnotecuile ;
% df calf recieves foo much lation which can potent-
i Ces have ability to down
ialty damage the cell, © a ae —
receptors meaning they can @
cecycle them ubich Yeads to few
sand thus decreased sensitivity
response bo sign
[ skime!
sequlate
Khe membrane and
member express vec epro
a signal molecules }
es ae
Care? DNA aheas
cell receptors _ Gost and cell veci
ewe abi fity to uprequiate tha
receptors ct inserted on
cal sensitivity to signal
most of the
signal, cells
more
x OF
very weak
which means
hos increasing
Example Signal molecule is
of a drug . As comcentvation of Aroq
pharmacological effect also increases until it
all the receptors ar occ ied -
receptors
!
membrane
molecwles
actually a some kind
increases , its
reach the
pant where
Sf we plot this, we cletermine ECSO From the
graph €CSO. os simply the concentration of a 21a
of the maxiroum effect GME
nat produces So]
tells us how the potent oq 1S
Dwg whch nas Vouwes ECSO is more potent Because
Ness drug is needed bo get half of the max response
Drvq ® also reach the same Devel of pharmacaleqical
effect as ang Q-And this is due fo its EFFICACY -
4 ts Ae presented by
So maximum efficacy of each dru
which all the receptors are occupied by the
don't produce larger effect
potent but also move effi-
Emax at
dog and high concentration
Dug As nok only more
caci ow in the diagram ‘
i _"_—E—E rrr400}:
Graph dose response
MAX
Phavmarelogical a8 Sciik
—— | efficacy -
“neTRINSIC ACTWITY ©
hte PES eemcaaaees
activity refers to, the ability of the chug &
Sout a drug binds to the
maximal effect
our bod-
Jnbinsic
produce marimal effect
and vt is able produce
receptors
that is compavakle to the effect produced ou
ies on endogenous Vigand - We called wo FOU
| AGONIST’
oP ok ue veceptors chow some Kind=eols: the aaa
«ky when, thee 15 no agonist around This is called
BASAL ACWWITY a
Sn presence eli Fol agonist , wonee Boe een
effect
PARATIAL AGONIST: The agonist that ts unable to pro:
due maximal effect even if ik occupies all the receptors:
IAWERSE AGONIST: the agent that binds to the veceptors,
| inskeack of activating trem, ak stabilizes veceptors 19
ahi inactive form We called & inverse agonist - Because
at snap ‘iminales barat activi
l g i 1}. CBS gonist
Pastiay 9
ical
ae
eae ee AS“ANTAGONIST”
Aaa
, On the other side of the spechum, we have anta ote
which refers to a Viganel that can bind to the Compchtive
3 4 Pawn antagonist
> Agonist + Competit-
Biologic we antagonist
effeck “3
tt oP Agonist + drreversible
: antagonist
FcsO £CSO
(Agonist )
04 Phenoxybenram ine Ana? advencdine ark
aw adsenegic «cceplo's': 4
o : “ALLOSTERIC ANTAGONISTS ”
“These bind to the ske different from agonist bindin
vespont
fo of
Population 2