U-3, Medicinal Chemistry-I, Carewell Pharma

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Mediinal Cheustry
Unit-n
Drug Actiug on Aulonomic Nevous syslem
Drug (Part-2)
A
A
RM
RM
Aubnoic Nevous System ISa pat of nurvous System na
A
A
(odrols aud qvlats iwtrnod organs/ body.
PH
PH
T oudrolt inuoludany ponsLs eg. Beathiug Digestiom ek-
L
L
EL
EL
two typul
W
W
1) Synupathcic. - fAready Studied in wr-T4
RE
RE
)Paracyupaduhic n our body Co back from
CA
CA
Symupadnchc ntrvous System (maintananu) to
normal Conduhion.
e Moumol eant rat P diqustiom rate et e

Nevrotvauinmdttcr
A
tws ae chnical that ravsnit

RM
RM
nwssungU SLmals
-f1om nwvon a arge cell/nwm
A
A
PH
PH
Synapsa
L
L
Synupodtetic Releas Adrenalius (fhdreungic nuwrohansmdt
EL
Alrtady sudted in Uuit-r EL

W
W
. Pauasypatthutic
RE
RE
leleas > Aetylckoliu ( choliuugit

nwotmuuni)
CA
CA
Cholineqic newvotansilter
THos nwrotranumutttr which foumtd or eleased
rom poracynpothutic Mure endug
A
A
RM
RM
A
www.carewellpharma.in (free notes)

PH
PH
visit website to download free pdf notes

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fAcetylcholius.
|Ach
t is 4h majpr newrotrasmuttr a pot ganghionic
ynapsas of cholinugic o pabgsynpathetic urve ending

A
A
RM
RM
, Hh
A
A
N-G
PH
PH
CH-C-0- U-h
L
L
EL
EL
is 0 chenical AubsjarL wkich acts in u
. broin and
W
W
to
RE
RE
body a a nwrotansmitter majutaln
CA
CA
810 sYNTHECIS, STORAGE P RELEASE ofAcH.
Biosyutnesiy of AcctylcholjuL
-TF u acehc acid esten of dollus
Syntneci of aceyl choliuu (adh) s doud b colinargic

A
newrons.
RM
RM
firsty
firsHy choliu ic Syuthecizeod in tu live by reaction
A
betuween serin and ethanolamin, hlth taken up ind

PH
PH
t neve yeminal by cholin trauaport system (TS)

L
L
Arcetulchoit
EL
wlth t
is Synthezizad by cholint and fretyl Coenzymd
EL
W
W
A help of enzym Arehyl cholinutrauiftraL.
RE
RE
serin
HO-Uh-CH-Co0H S-adenosyl
detoabla HO-U4-Ch-NH
CA
CA
-
(O Meu
NH (thanol dmin.) trovufra
Csein)
,4elylolinu
h--0-h-t-N- Hrauftra Ch-instot +HO-0%-04-N-
Cheol
w[Ach) (ficuhyl to-A) (Chohiwa) dh
Arery
A
A
RM
RM
A

PH
PH

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CA
CA
Stoa
Th
Thu nuwly formud fAch Atprd nto th Atorags vesíctes
by tu vesicwlan Ath Hra ponky (VAukT). -Eath vesti veide
A
A
COutain atou molecules Of An.
000- 50.000
RM
RM
Wittin seseitle vesick Ach (hylaolina) is protrcted from
udrolysis.
A
A
PH
PH
Relea
t inftumu. df
An is redea ftom t qranules undur
L
L
+optning of a ion dhannl (vollag
EL
EL
Nere achiom potenial
Channul).
W
W
gakd
RE
RE
Stimulatom Adtivahim of a** ene through
in
nue volta qattd dhanu
CA
CA
mumba ul.
Vesicle disthang Vesiclu fuLA Activali tinaLl

patkin
thein coutnr (Ah) uih murb ran haF puesphonylat syuaps
p-ynaphit
A
Ach bind with Receptons(N AM) aud give h atim (uponsu).

RM
RM
Catabolim of fAtetylcholi
A
A
PH
PH
rellal and aciom of acctylcholiL, thu

funchon aud efkcs of Adh Can
tuminated wltn t
L
L
EL
help of enzym yduolyciu EL

W
W
Auhylchola daolinustrausCholiu+Arehic acid |
RE
RE
CA
CA
Cholinujerasu enzym also known a acehyl cuoliul estaau (AchE

ydolyses Aeylcholiu (Arh) uto inattive melabalikyA
choliu and auhe aid .
leleana of fh is inibitkd b
Botulinum toxiu.
A
A
RM
RM
A

PH
PH

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CA
Cuolivongi c
Lue hwrons
Sein
+ cholin
Hhauolari
A
A
Choliu B10SYNDHESIS
RM
RM
fArehyl conzyuA o\
A
A
frehylcaliut a1
PH
PH
L
L
Eudnq
EL
EL
Choliua +
W
W
Trehic atid
Vesicl
RE
RE
choliua qvaph'
Calabolitm
Ueit
CA
CA
sferau
aetylcholiu Recepton
/M fpost)
Rexpae
Chdllurqi Recuptor dishibuhiom
and thir
A
A
RM
RM
Cholinwgic Hoptor ak hoce eeptor in whlth cholinugic

A
A
PH
PH
Mwotronumittr/ drugs bind ditHy to indu Variovs achion

L
L
or sponsA.
EL
classified into two ypu EL

W
W
RE
RE
) MUSCorinic (M) n) Nicotonic (N)

CA
CA
ML NM
M
M3
My
Ms
A
A
RM
RM
A

PH
PH

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CA
1) Muscorínic (M) tceptors >
Hcaptorsamily.
belongsb
belougs t -piotein coupla
cholinugic
,
A
A
isH is Rrown as useorinic Heptor, butaw whn
RM
RM
mustarinic.
ah/nwrotranimitle bind th t ghve
giue uponu ie
A
A
Muscavinic is wat Aolvbls toxin deived fom tu
PH
PH
MUCavinic a
MUShroorm Amanita MUSCOAla whih CasA acivahm of
L
L
EL ra
EL
paracympatuhte nuvovs suctem. efieus such as Aloued hn
W
W
MUCdes)."
aud inceacud athuilq of Sooth
RE
RE
Medhaigm> fAcehylholiuu (otn drng om Binds to mustaiic
CA
CA
Recuptors
a fAch)
Responshion frchivation of Coufonmationol changa
C-potin in Recapto
Typu
A
A
RM
RM
)My.PRseu in autoromic gavnglua, gasbic qlond,

, CN
A
A
PH
PH
fundion Histamina Releata,Acid cecetiom, fchs memoH,

Motor functionc
L
L
leaning
EL
M2 pen in hearE EL
W
W
condudtin.
function DeceaA veloit of hea
RE
RE
CA
CA
1 pk in SMooth MUSdes o t blood vesselk Cnd oF
luwg
functionon au Coutrachn of Amoctn Mdes (bronchotonsbicim)
Relen No (nirovS oxida) to produl valodilationm.
A
A
RM
RM
A

PH
PH

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CA
i M pxw in t CNS ad hea
unchin » Activation of MH Huptor inibik awlyldholin.
relea.
A
A
v)Ms
RM
RM
pHeCenF In t CN.
.funchiom T May cqvlaiti dopamin. cleas
A
A
PH
PH
fAcehylckoli, , Metmachalins Bethanncluol (Ms) Aoma
(n2)
L
L
dwgs wohich biud wth HLeptons
EL
EL
W
W
2) Nicotowic (N) Hceptors
RE
RE
an ioucthopic Hcaptor (Ton channl Hezpto).
Tt is
CA
CA
FecaporbecavsL wlun dholinuyic
is known as niotonle
drvq or nwrotranmittr bind wlth it, t gie Hsponu ik

NIcctoni
Nicotonic F stimulaks u pkasve ceute of thl brasn

A
T a dva, (higy addicive). t nicoti in dasette

RM
RM
changus yeu brain. "

A
nicotonie Hceptois
ftehylcholina (otu dwa Biuds to
PH
PH
udwium
L
L
opening oF Activahom
lapid -fo of-
EL
Cohios
ion chanl EL
W
W
RE
RE
kelutal nuromusuwbn.
CA
CA
) Nm (MUSde typi niLotonic Hteptor) > pHsant in

Jundhon.
.funthion skelctal MUsde (owractionminceaa cahin peLmabili (Nat,kt)
Roth (Nm4NA)
ca-Adh Nicot, DhnylimuHy! ee
NA (Nawonal tyba nicetonic receplor)> pecunt In adhtnal mudullmy calls,
spinal hcord, ganglionic cell, brain (contain anua).
hunthim Dupolanizaion, seeeim of takcholamiws. eg.Ah nicotbna, piperaztua,et,
A
A
RM
RM
A

PH
PH

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CA
SAR oF Porasympathomimutic
Parasumpathormimuhic Aguts a4s
Pavatympathommutic agus
A
A
Also known a cholinugic agonlsts. or Chlinwqic dg
RM
RM
parasympatho paauympothehic Nevovs
Sushem
A
A
Paracumpathomimutic
PH
PH
mimie mimic Lopy thi atinJ.
L
L
Porayrpatkomiuhic aguAT aR Hhos Chumical aginii (dng which
EL
EL
u achon o paraSympadudic nurvous ystom.
W
W
CopA
RE
RE
h agsor druga bind with cholinugic HCupo (N # M)
CA
CA
and give Hheir action. 4hy ac
aa dholinugi
wrotans muter)
SAR ofF Poraympathomimuic agunts.

A
RelationshipP
SAR Struchut fctiit
RM
RM
Chumical
-IF is deffnud as th relatin shiup bttween t
A
Moletules aud is biologioal aciuuil.

Atructu of a
PH
PH
- This allbw modifiotion of t efe or poheny ef a

L
L
Chogn chumical Arvctu
Svbsjana by
EL
EL
W
W
a Parasympafomimutic ageis/dw
RE
RE
ACETYLHOLINE|
SAR
CA
CA
8-Cawbon o-0vbon
Quattnany
Ch--0-h-% nmmonjum
Copoun
trehy goup ehylen

dhain
A
A
RM
RM
A

PH
PH

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Page 8 of 27
CA
CA
Strvdurally, modificahion is possibll on
- fAcehy qoup
Ethylen chain (ox+ Carbon)
Quatenary ammonjum
A
A
RM
RM
COnpounds
Substituhiom on aceryl group

A
A
Carbamat group Inureaa achiuu
PH
PH
eoplaumunt of acelai group by
and also mo Atablo
Mou acive + Atahla
L
L
EL
EL
Carbathol than autylcholn
NH--o-h-0h-NEh
W
W
RE
RE
Replaumun cf eskr group by eth 4 kelont group givt chunically
CA
CA
stabl ad polent compourds and have Bom cholígic adiust.
p-meHkylcholina tR ethon
Substituhon on ethylen chain (x 4 B canbon)
Inctase in tu han lengh deueast th atius

A
On brandhing hen n thin attiuu.

RM
RM
aL alD Changs
-Broncing on -canbon > inuta atiuut fot nicotinit (N)

A
achiuitfor Musaninic (M)

PH
PH
deceo
- 6ranching on R-arbom inuea acriuifo Nustainit (M)
L
L
Nicotnic (N)
EL
decaca actiu for EL

W
W
Substitutm on Quakrnany fmmonium Conmpounda.
RE
RE
Replacenmunt Of ammoniun group by othn goup (bio-iour) ia

CA
CA
sulphovivm, phosphonium e. Caus loss of actiut

Replacomunt of mort than OnL Miu group off
quakmany amnonium group leads o Complek loss of
cholingic atiu
A
A
RM
RM
A

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PH

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Page 9 of 27
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CA
Classificaiom of Paacympatnomimuic agunts.
agtnts.
Diec auing aguii

Tndirt ating agus (choliustras inkibilos)
A
A
Cholinerasa tacivator
RM
RM
Parasypolhomimuic fguts |
A
A
PH
PH
Din fcting Lndirt aching
_
holineUasL
L
L
agunts aguts/ cholînesttrasa Hativator
EL
EL
inhibiors
Accylcholius .Pralidoximi|
W
W
Chlorida
Carbacho*
RE
RE
ehanecol REVERSIGL TRREVERSIBLE
CA
CA
Methachliuu | Physostigmina Isofluorphati
Pilocarpi Neostigminn Echothiophar
Pyridashigmina odids
Edrophovium chloridi Paration
Tacrin hydrotnori ds Malathiom
fAmbinonium chlonda
A
A
RM
RM
Direc ading fqui-

A
Thes ax hoss dnqs a agnts whih dintty bind witm

PH
PH
dholinugie Hupp N4 M)and give at athn.

L
L
EL
) Ahcehlcholins EL
W
W
-N-UHk
RE
RE
Ch--0-0-02
CA
CA
-
.Mehanism of achon
i diec acing cholinurgic
dts
dv
action is deswcted by dholinuterat
- T is poweaful bu
USLs widely uud aeudrop to ausa miosis dwig bunguuy +Horeuy.
-USe4 a Vasodilator t andiac dip«stun
A
ek.
RM
RM
A

PH
PH

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Page 10 of 27
CA
CA
) Cavdacho
N4-(-0-h-h -C4
A
A
Syndheu
RM
RM
y .
A
A
N-U, Coth CI-Co0-H-6 N
HO-h-(4-
PH
PH
PhDsqpn
cholint
L
L
NHDH
EL
EL
chlorida
W
W
is ppared by Hadtng chdliun
TF
RE
RE
-
chlovids with phosgon in chlorbsorm N4-C-0-4-04-N- .C

CA
CA
Bolution -followed y tstmurt of Cor bachol
t poduc wih ammoniun hudoxld
give Covbachol
Mehawism of acttom >

A
-Bind with both mus (arinit and nicotinic

RM
RM
T no inachivaltd by choliuwtrasu s0 it action

A
MOK prolongud han Octylcholiu

PH
PH
Usu
- Vsed in Caseof Savek chronic qlawcma
L
L
EL
give itra-owlarl to prduca iosis n owlar surguy and EL

W
W
to duce post operahive risk.
RE
RE
i) Bethanachol >
CA
CA
N4--0-H-0h-N-03
MEthanism of acion
- MOH Selective tAT On tu MUSCarini Huptors.
A
A
RM
RM
A

PH
PH

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CA
CA
MOR Atablu than Corbachol dus to presuts of methyl
qoup On B-Cavbon
Us
A
A
stimuli 11 rot and ufnary bladuw aften surgar.
RM
RM
prolong effecr thon acyldholius
A
A
v) Mehacholiu
PH
PH
0
CH-C0 -CH-CH-
L
L
EL
EL
W
W
Mechanism of achn
RE
RE
-
1F has MUStavinic actions of acylholin
CA
CA
polonod acion than aahyltholín.
Usu and glawtoma-

- Vsed in tateatmn of rynawd's SyndromL
- USed in casA of tachytardia
v)iloapa
A
A
RM
RM
N
A
A
PH
PH
L
L
Mechanism ot acion
EL
- DiHc actng cholinergic drug thak has

musarinik
EL
W
W
efk of acehylholi
RE
RE
teatmunt of glawcoma and in tHatment of

CA
CA
- USAd in
dry y o dy mouth
Sun
SUrauy a part of emuguney teatmant of
- USAd bfon
aue atak of anglu-doSule glavto ma
A
A
RM
RM
A

PH
PH

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CA
CA
Indirt acting guxts Cholinesetacu innibitors
- Also knouwn anticholinesterases .
Thec a 4no dg wWch dotu not ditdty ac on Rcaptord

A
A
bu inhibir t hydrolycl of ahylcholint b acotyl dholinesteracu
RM
RM
dnd henca inceaA hu Lie of acehyldholina, D awrylcholin glve
qíve
A
A
heir adion.
PH
PH
-
he a of two typus
L
L
i)Reversibtu inhibitoH
EL
EL
) eversiblt nhibito
W
W
RE
RE
)Reveribla inhibitors
acery
Hose dug ohlch blnde Heversibaly to t
CA
CA
thek oK
cholinestesas enzyma.
The agpnts form an
eser ke Corborati o phosphat avd
biud with achie ie d enziymu
-
Now, ths enzyma does not hydnolyzud aceyldholfni
Inceass in th Concontation of acerylcholiu
A
A
RM
RM
1) Phy sostigmin >

A
CHh-NH--0.
PH
PH
L
L
AcHan
Mechanism of
EL
- Reveriblo cholinesjera sa EL
W
W
inniabos
RE
RE
both muscaínic and Nicotinic Fecuptor

IindiHy Aimulau
CA
CA
.UL miotic
- USed a a
fndraocula pRssUN in qlawcoma
USud to 66teet
deceas
A
A
RM
RM
A

PH
PH

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Page 13 of 27
CA
CA
Neostiqmina
N-0
Symthesi
N
A
A
(
RM
RM
N
+C--
A
A
OH
PH
PH
Chlorodimhul Carbomale
(3-dimelhul
CDimemyl carbomoyl culoriduJ
aninophunol
L
L
EL
EL
W
W
N-U
RE
RE
Ol
CA
CA
mehylaiom
Neoshiamin
CNeoshigmi n
Mechanism bromida]
of aiom
-
7indiH cHy Shimulates both muscorinic and nicodnic
A
Huptos
RM
RM
-1t bind th onioric aud eseuc silt of

A
cholinestuas and block Hu acivity of qcetylcholinesjtrase

PH
PH
Uses
L
L
- USed in t eohmunt of nyasthenia qravis.
EL
also usud in glaucoma lousen lvraowlan peAu). EL

W
W
Pyridostigminn
RE
RE
CH
Methaism ot atin»
CA
CA
-Block acuhyl cholineseasa enryma

and Inhibik tu destnchion d- o-N
kleoud qcehylcholi
- Usod in th teadmunt o myasthunia gravis.

also halbful In nuve gas polconing
A
A
RM
RM
A

PH
PH

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Page 14 of 27
CA
CA
4 fdrophonium chloricla
MechonicM of N-CH
cion HO
O
A
A
Revosilu dholinugic inhibitor
RM
RM
Ahort durahion of adion tuan
pyridostigmin
A
A
neostigminu and
PH
PH
Usu
Usahul fon tu teatmunt of myasthe io qravis (notl 2egvlon.)
L
L
EL
EL
Usud in t ttamn tt Anake biti.
W
W
5 Tacin hdocdlond
RE
RE
Nh
MAhajsnm of achion
CA
CA
- cextrolly acting
audichelineifoa u. IOK HU
.Ucd
Used tor h tratunt of AHzheimu't diteau
6fpioíuo Cdoyida
A
CH
RM
RM
N K-NH-AizNH;
A
A
PH
PH
h-
L
L
6) Ambunonium Chlorids
EL
Ch-0
GH EL
W
-N0h-0h-NH -t-NH-(h-0hN-
RE
RE
CA
CA
U-0h
methoicm ot ation
-Reversibly inhiki auhylcelineserass enzym
-Usud In t ttatmun/managunbt of myasthunia qravis

A
A
RM
RM
A

PH
PH

R
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Page 15 of 27
CA
CA
Lvenibl inhibitors
Thesa ae tnos dng which produas irreversihl
inactivoion of acehylholinesjvosu enzym.
A
A
These dwgs bind ireversibly by covalen bond to t
RM
RM
actiue it of enzymL Cmd CawSA inactivation of enzym
A
A
This totgony induda varlovs Organophosphorovs copoundi
PH
PH
L
L
EL ,
EL
W
W
CH-0-P-0-CH
RE
RE
CH
CA
CA
Mechouicm of acion
-
irrtrersib Inach votion of t acyl cholinestera
Ucu
- USed a miotic aqen in tHastmunt of glaucoma.
2
2Etotiophali Todidlu
A
A
RM
RM
,C
A
A
PH
PH
CH,h-0-P-S-h-C N
L
L
O
EL
MLthaism of achon EL
W
W
- itreversibl acetyl CholinestbatL inWblor
RE
RE
- pemonevHy inactiue
t enzms
CA
CA
USU
used a an ocular antiypetengive in u teamunt of
of
chronic
qlavtoma
A
A
RM
RM
A

PH
PH

R
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Page 16 of 27
CA
CA
$7 Parodthiont
S
A
A
O - NOL
RM
RM
aH-0
ot achon
A
A
Sy mechavism
PH
PH
- indiiecHy inhibitor
L
L
U
EL
EL
Used a insecticida in aqricultu
W
W
4) Malation
RE
RE
0
CA
CA
0-0
MOA lindin seune Rsidua on
cholinteasl enzyms f inachve 4tievtsi
-USd fon teamanr of staojes

A
A
USAd a insactiids
RM
RM
in Cholfnesterass Hochivabrs
A
thesA a thosa dwgs which CoU&A activationm of dholineskeo

PH
PH
enzyma. theca mainly

at ud in eatrunt of poisoning by
L
L
orqanopnosphales, sulfonales
EL
Pralidoxima chlorida
and aceylcholinesteraca inhibibrs.
EL
W
W
RE
RE
Mechaism of adion CH=N-0H

- kaivali enzymL
CA
CA
by
binding to th anionic sitt t enzymt
and displa ces te phospha seuns Hsidus
ftom thu
. Us
- UsAd fou tu teatmunt of poisonlng by orqanophbsphowe
ConapoundyA
A
A
RM
RM
A

PH
PH

R
R
Page 17 of 27
CA
CA
CHOLINERGIC BLOCKING A4ENTS: SAR_ of Cholinalytic cguds
AHo cnown a bloceing ag
Cholingic
A
A
Choliuolytic aquts
RM
RM
fAicholiuaugle aguds/ dugs
A
A
Choliwngic audagouis
PH
PH
ParasympaHulytic agut
L
L
dutinustarluic ageuts
EL
EL
Thea ae thosA aguds whidh nkibik th
dvs
W
W
etc of
RE
RE
acctylholiu or paratypcthendmeic agpts
CA
CA
buy bloceiug tu Chelinugic eceptork
AAndijdelini
Aretykwaliul aguts
Receptprs
A
oay
RM
RM
Sonuim natwally or duu to eahsn, eleas ot

A
acetyldoliua iuueoas aud du to ecescive elea

PH
PH
tgives MOL esponca (whidn aw body dots ust ut)

L
L
as n , contaction et
EL
Sydh incHaA Salia

EL
W
W
AHLo used n Condihon of chaliungic poisniug
RE
RE
So, Arucidhelinangic ageuts eduaH dver-esponse of

CA
CA
acetylckolin
-Lxamplus Abopin, Diuylomlu hyduoclulolda, 1prahopium

bromiclL
ek
A
A
RM
RM
A

PH
PH

R
R
Page 18 of 27
CA
CA
SAR Stnucwt Aeriuti Relationship
of aidholiuungicfguts or Cholinolytic agens

A
A
Genetal avcicholinergic COMpoundA
stuctue of
RM
RM
SAR ofL
A Amicholinerqic Aqents|
A
A
Cyclic
N
PH
PH
Substitutiom chain
-C
L
L
EL
EL
s Qvater nany ammonium
H/oH
W
W
Stwcturully, svbstitin Conpound (cationic heaol)
RE
RE
Modi fiahion is posibla ou
CA
CA
alut qroup ( Catoie had)
chan
Gyclic Svhsjituion
-Hydhoxyl group Avbsitution.
Modificahion in Cattonic head ( ammonium Copovnds)
A
Qvadenay ammonlum CDwpounda possusS Most poleut aucidholinergkc

RM
RM
aciuul. So,
A
Replacemunt of quakno o u tertiary setondary cr porimany

PH
PH
Cousa deceases in activity

L
L
EL
EL
W
W
actiu
RE
RE
Modifiation in dhain » 0-P P-0-R (-H

CA
CA
,alcokel
Tw Substituhon may bba esjer, eth or amina
Sur, Es goup provide ta mos poten anticholinngiu
aciu. e: Aopina e
Somtims Kubstitulion s abta.
A
A
RM
RM
A

PH
PH

R
R
Page 19 of 27
CA
CA
Modification in
ad b
Substitujon Could b uydoalkyl, aomaic rings or heltoujdi rings.
Cubocydic ring qve
cd helerocyclic maximum Cutagonisr
A
A
acivity
RM
RM
Keplacemunt df neeocyciHc ugs to avomatic achui.
decm
A
A
Th riug4 Could
b idenial bur th mo pote com pounds
PH
PH
O o have
tound diffent ring Substitution
L
L
EL
EL
cDialonut ec
W
W
SubstHuien in C Hydroxy qoup Avbstituttan.
RE
RE
Svbstitutton Can bA hydrogun (H) or Hydroxyl (oH) or hydroxy
CA
CA
group.
H O OH gtiachud auagonis- au MOHE pokent (actiuutiy1).
n H+ OH ,
OH
1),
fActin (actiui durahion of acttan
Action (Actiit), of action 4T
A
A
H dwation
RM
RM
.CLASSIHAATMON OF ANTIOHoLINERGICfeENTS
A
A
PH
PH
L
L
EL
Solanaceous alkalids
Synthetic onolinerqíc
EL
W
W
ond analoqus
blocking agnts
RE
RE
Atropl sulphal Propenthelin bromida

CA
CA
.Tropicamids
Hyosyamin. sulphat Cydopewltlali Benzthopina mesuylati
Scopolamius hudobromids Jidinium brouide Crphunadriu irat
hydrouuorid
HomahoptuL hydobrdmide Dicycdloomiul
Dicycloomi u huodid51perldins
hidrodugna.protutlidinu nydrocileordli
prafopium bomids lyopymolek Tridihexetmyl chlorid
Methanthdiun bromids Isopropamidt iodida
A
Ethopropazine iydrchlorids.
RM
RM
A

PH
PH

R
R
Page 20 of 27
CA
CA
SolanacOUS
alkalbida and Analoguu
Solanacuous alkalofds are th ester of th tropiua, thesn
alkabids obtalud from plauts SUdh Aopa balladona,
A
A
Hyostyamus
RM
RM
higer, Datua stramonivm ek.
Thes al alkaloid Called a Solanaaous alkalojds as
A
A
PH
PH
Hhesa pauts belongs o tuaily Aolanactal
Thesa ettus o oraumpothormeic aguts

L
L
altalolds inkibit
EL
EL
CgHyosuamint,fAhopi tyostina et
W
W
RE
RE
) Anopiua Sulphali
N -oH
CA
CA
7 is a raemic mixtuau
0 . S0y
of hyoscyamina obtainud
from oot of bellodona
Medhauism Of achion
A
nas both contTal and periphurad atian.

RM
RM
-
t ffrst Stimulaks and Hhen depresses a CNS.
A
Usus
PH
PH
-Usud in tu teamunt of gasbic and duodenal uces.

musue spasm.
u teatmut off SMOoth
L
L
used in
EL
2) Hyosuami Sulphai >

EL
W
W
RE
RE
Mechanigm of attion
N
CA
CA
- Similr to aropn oH
mo Potent +han dropine. o.
.USuy H
eatment of qasic and duedénal uder

paukinconlsm
also uud In heatunt of
peven
A
Mohion sidRnes
RM
RM
A

PH
PH

R
R
Page 21 of 27
CA
CA
Scopolaun hydrobiomide. > (Hyoscluu)
Methoism of CH -
acHon
H- 4OH
h-N CH-0- CH-
A
A
-
RM
RM
has mok rapid
Oncu bur shorter
.H8r
A
A
duration of action OR
PH
PH
han athopin
L
L
-
MOH polen thman Hr
EL
EL
N-U4
attopine
W
W
-Moktoxic. oH
RE
RE
CA
CA
Used in t tatmut of motiom sinss
Somutims uced befo Surgy to decHas saliva
4) Homatopixt Hydrobromida 4
A
A
.mechaism oF
RM
RM
adfon N
It is a conmpetitive
- OH
A
inhiotor of acotylcholinL or
PH
PH
H8r
MUScarínic Hcoptdr, blotks
L
L
paracypathetic stimuladion.
TO3
EL
EL
W
W
CH -CH -CHh OH
RE
RE
is USed to HRr
dilake ot enlaMI
Hc-N H
CA
CA
Pupils in e. -0H -h
A
A
RM
RM
A

PH
PH

R
R
Page 22 of 27
CA
CA
5protropium bromidl
Synthesu Aropns is acr uwith sopropy bromidu and givt
tso ipratropivm bromldu.
A
A
N
RM
RM
h-0H
A
A
(Anopin)
PH
PH
L
L
(4) HBr (1sop>opyl
EL
bromida) U
EL
W
W
RE
RE
N
C2OH
CA
CA
(Ipratropium bromida)
Mechoism of achion »
A
quaenary ammonium tompovnd which blocRs musCarinlc

- 1 i
RM
RM
acelyl cholius Hcepto.

A
MUS COrinic autagonls

is nm-selecive
PH
PH
Uses
L
L
- Used in tu teatmun of Aisthma
EL
atu of chronic obstrvcive pulmonany dicua (toPD) EL

W
W
RE
RE
STNTHETIC CHOLINERGIC BLOCkING AeENTS

CA
CA
Solanaceous alkaloids hove lack selectiuy and also have

SonL Sida etkds, tus lead totu developmu of
syndheic auticholinngic aguds
Vanjovs Modification have been Made In tu svduA of
aopina to give Vanjous
A
dholinngic antagonist
RM
RM
A

PH
PH

R
R
Page 23 of 27
CA
CA
1 Topicamid
CH-OH
M-0A
ac aa a CompuiHve
CH-CN.
O
A
A
atagouis- fo fh.
RM
RM
A
A
uGud -for dilatin cf pup(lofou f aften eyn pugp).
PH
PH
2 ydo putdls
L
L
udhochlouide
EL
EL
M0-A
W
W
acF a compuitive O 0
RE
RE
HU
autusouist fon Auh --0-h-0h-N
-ac
CA
CA
Mou quicrly han aopin OH
-Usd in a dop for mydiasis (dilahon of pupil).
Clidinium bromida
N
A
M-0-9
G).
RM
RM
- bind wih muxaailnl kceptor -i-0-

on Smooth musdes and
A
DH
seLvetony gland4 Ihhlbik tuptor.
PH
PH
USL
billiary dac cuuetn
L
L
itrlazu mooth mvstles and deceatu
EL
VSd in eatmun of iahte bowel Sunel roma EL

W
W
4) Dicyconmiu hudrochloud
RE
RE
CA
CA
M.0.A
- acts as nm selechive smooh
Musde relangvt: Hd
-T has Apeifie avdidelinmgic C-0CH-t2-N
efftc at Mustorinic Heepto
ud has diHc effuk on Amooth
A
MUtl.
RM
RM
A

PH
PH

R
R
Page 24 of 27
CA
CA
- usu in t trestmut of ivitahl bouel Syndrom

also uud in u htatmunt of gasbic and dudon uller
A
A
Suuthesis of Diuylomin ydhochloida '
RM
RM
CEN r
A
A
PH
PH
NaNk
CN
L
L
EL
EL
Gyanotydo Cycdoxy Cl-4-0h-N
hexanl bonid:3
W
W
CL-upupbicyoluxaua)
RE
RE
Q
CA
CA
i-0-4h-0hN
HC
Diugloamn)
5) Glyopyrrolati
A
M.0.A OH
RM
RM
-Blod MUSCArinic uuptor

iphibishirg inkibitHng
A
4us
PH
PH
cholinurgictanisin.
L
L
EL
- usd to ttear Qaxtric lter

Hedv
by Kdvdn
salivary
addic SACetin.
broncnlal and gastric
gastnic.
EL
W
W
usad before surgury
RE
RE
SeCetin.
CA
CA
Methonthelie btonid
M-0A bind muscmnic HaptorP
blbds ta adtion of Ach. c-0-CH-C4-N GHs
B
ULLL
t is
qiven in
Conubination ot antaud
to a peptit vlu
A
A
RM
RM
A

PH
PH

R
R
Page 25 of 27
CA
CA
7Properdhebive bomidu
M.0.A ,0
- blocksof tl action i-0-4h- h- N-UCH
aceylnolina by bínding to
A
A
RM
RM
MUSCarinickuptot pecut
in vavious smoth mMustlu ur
A
A
qut bladdur and eye.
PH
PH
USL
. n L excess ive Aweohing
L
L
uted Htaun of
EL
EL
-uu in combinatHon with axtadd eat qasic ulce
W
W
+tamunt of spasm ofHa stomadh,,IutesHua f-bladdur
RE
RE
8 Benztropius mesylai »
CA
CA
CHh
H -Uh
M0.A
centrally ading avticholinugi¢
- He-N-H CH-0-H .
Co
O avdihistavnins agu
Aelecive ML MUSarinic antagonist.
Ch CH O)
UstA
A
-ysd in teamu of pakinsonism

RM
RM
- awiistamins. aud lotal anaestuhic actiu.

A
9 Orphunadrin urar >

PH
PH
MOA
L
L
EL
selective acehylcholiu tupot CH-0-U-Uh-N EL

W
W
Outogenict and also autiistorin.
O)
RE
RE
CA
CA
,CH-(0oH
- is uged to reltere pain
HO-C - Co0H
du to ApaAm of voluntany mucle. Sm-DON

aluo usd n -teatmunt of pavkinson's disease
A
A
RM
RM
A

PH
PH

R
R
Page 26 of 27
CA
CA
10 Biparidins Hydrochloridu
MOA h- h-N H
- acs as a (etrallu blouaiug
A
A
agtnt ad blouk ML
RM
RM
musarinsc HCaptors.
A
A
.Uu
PH
PH
-Used in eamut of parkinson's diseaso
L
L
teduce mUscle rigidity
EL
EL
Hdvu abnormal Auweahhg aud alivatn.
W
W
I4) Prouclidins hudrodnlonida
RE
RE
CA
CA
Ssge MOA
olotablock muscarinic Rceptdr
U drug
-usud for teatmt o** induud pavkinsoniám-
disordur) and
-uLd in tamunt of ARatisin (movenut
acule dystoua (Nevrologtal movemunt disordur).
A
Syntmey
RM
RM
A
NH-h-t:0 -mgbr NH-h-C-OH HU

PH
PH
HU
L
L
3-pyrolidiny)
EL
proplophunon Prodidin
hydrochoridu
EL
W
W
RE
RE
12) Tridihuxemyl dulonida

,GHs
CA
CA
MOA
-bind t blodk mustainic
O JU-u-N-GHu
Huptor
. Uu
- USLd a atipasmcdic
anivlcar.
A
A
RM
RM
A

PH
PH

R
R
Page 27 of 27
CA
CA
Isopropamidu Todidt
.MOA
-bínd + blotk
O h-0hN-M I
A
A
MUSCAPiwic Huptor LDNH
RM
RM
.U
A
A
- uced in Peptic ular
PH
PH
- used for Heamunt of musula Cortrotion that caua pain,cold,
L
L
gastritc and hyprchlorhydria.
EL
EL
W
W
14 opropazin hydrocloridl
RE
RE
Hu
CA
CA
.MOA
parially blouk Centtod
dholiurgic ecaptor ahd hulbi to balancl CH2-H-N

choliwgit and dopamdnungic actiu
in gangti
A
A
RM
RM
- USAd n t teamant of paykinsonim.

A
have anausthehc, anglionic blocking,autikictamiaic

PH
PH
propouhe.
L
L
EL
EL
W
W
--000-HANK YoU-000--
RE
RE
CA
CA
A
A
RM
RM
A

PH
PH

U-3, Medicinal Chemistry-I, Carewell Pharma

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R

e Moumol eant rat P diqustiom rate et e

tws ae chnical that ravsnit

Alrtady sudted in Uuit-r EL

leleas > Aetylckoliu ( choliuugit

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ynapsas of cholinugic o pabgsynpathetic urve ending

Syntneci of aceyl choliuu (adh) s doud b colinargic

betuween serin and ethanolamin, hlth taken up ind

t neve yeminal by cholin trauaport system (TS)

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Vesicle disthang Vesiclu fuLA Activali tinaLl

Ach bind with Receptons(N AM) aud give h atim (uponsu).

rellal and aciom of acctylcholiL, thu

help of enzym yduolyciu EL

Cholinujerasu enzym also known a acehyl cuoliul estaau (AchE

choliu and auhe aid .

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Cholinwgic Hoptor ak hoce eeptor in whlth cholinugic

Mwotronumittr/ drugs bind ditHy to indu Variovs achion

classified into two ypu EL

) MUSCorinic (M) n) Nicotonic (N)

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Responshion frchivation of Coufonmationol changa

)My.PRseu in autoromic gavnglua, gasbic qlond,

fundion Histamina Releata,Acid cecetiom, fchs memoH,

1 pk in SMooth MUSdes o t blood vesselk Cnd oF

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drvq or nwrotranmittr bind wlth it, t gie Hsponu ik

Nicotonic F stimulaks u pkasve ceute of thl brasn

T a dva, (higy addicive). t nicoti in dasette

changus yeu brain. "

) Nm (MUSde typi niLotonic Hteptor) > pHsant in

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SAR ofF Poraympathomimuic agunts.

Moletules aud is biologioal aciuuil.

- This allbw modifiotion of t efe or poheny ef a

trehy goup ehylen

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Substituhiom on aceryl group

Inctase in tu han lengh deueast th atius

On brandhing hen n thin attiuu.

-Broncing on -canbon > inuta atiuut fot nicotinit (N)

achiuitfor Musaninic (M)

decaca actiu for EL

Replacenmunt Of ammoniun group by othn goup (bio-iour) ia

sulphovivm, phosphonium e. Caus loss of actiut

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Diec auing aguii

Direc ading fqui-

Thes ax hoss dnqs a agnts whih dintty bind witm

dholinugie Hupp N4 M)and give at athn.

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