ADRENCRGIC eLOOKER
ock h actian c Sqpathei acio by ardajm F
euptey
L -blacke
Non Selkchve
Pher0xbe2ehe - 1D5VSibl
phebtolamins
ola2elina
Ouhydo eAgotanI
Diydao egotoxiDe
blocke 20sin
eV Paosib Atu2s1"- bolbddIrg
Silodos tn BPH
Doxano St
TamsulosiPq
d blocke
e h Yobimbna
Raywol sina
gda 20xgn
a n s u n
Labetald 'e cL" Cerped An
Gepa diray
I e block -
C v e d i l o
"2 gehera"
Bblocke = Lol
= Pro PiTin
Prd PiTim
Bbloc
NonSludve
Proorarolo frsFGoeralten..
Pindolo- IA
Tmolo
tuolv..
Seladie) block
Ne
B-Blocke Acing
PCCardeo A t Myo Condiqum
-Celijaola
N e b j v o l o
Betaxolo P b l e k a -
utoamia
Bis p n l o
Acebutolo - geenan
ALesmo Es mols
Ateno
meroprols
ADRENERGIC ANTAGONIST
(SyMPA74HOLy TIC AGenT9
The dougs uhich block
h e achon dh Adrenaline Noracenaline
adreno receptors ( and receptor)
by 0ntagdnisi
1.Alfa CA)-Blockers
PhenOxyber2ernine, Dihydoergolamine
Tola2stne, Phentolane,
Mekylsergide
CSHT-alo mtqonisD
Poa20Sin,
2. BeaCg)
Bockers -
SAR of p-blockerS
Beladstet, Bisoprstat
Atenstsf,
Mehbrahstot,
sDpranstol Carvedilst
Labetols,
Metopstst,
esmotst,
AIfa Blockers
blockers
a) Non-SelecHue , bab.amine
> PhenOxy
alkylamine 1s1apoine
#Halo PhentaamIne,
1Imidaasune s >
ergotamine
deriuetiues
Dihydio
4 Ergot
blocker
b)
SelecHue ox
4 t G s t e t a m A e S
ieaLosin
-
roSIn,
nes
C u n q p e f i n a h m |
ldg20xah
Voh1mbine,
-
blockes
CX
Tola 2oine N 2-ben24l-4,S-duhyo-1H-imidq2ste
2 - benyl-2-Imidaoine
o-CH
elocina
MOA o,dok2 receptor
ethylerdjamine
Synthesis
CH- oGHs NH-CH
CHCN GHOH, H N-CH
NH. HC
benyl Cyahde
.C HU
Tolgaetine
hyoluochleide
Uses of 7slardine -Vasodilator
neusbn
punmonany hypelensim in
exsistant
4Raynauo's disease
Cerebral vanoulan acydents
4 AnHhype tehsive agents
9 t may retfux Sympahonimelur achm on heal
Phen lolamine
8- N-(2-1midastin-2y! mehyy
-P-ofuid1no] phen
N-CH
2 -C4-mehylphenyl)
ami06
-hydmxy phebyl)
-
meyI-imdqastine
s h t dwat
MOA d, i d2 bBocker,
in patient with
uses # To CoDtoaf hypertension
Pheochomoytoma
Atso use intq-operahue mahagement o
Pheochrbmocytoma
T Conmst hypertensim due to elonjdine wi
Phenoxy benaamine
N-benayl-N-(2-CHornePy)-1-Deky
2 CH
o-ocH -2-phehoxy- Ehylamine
-HC
MOA btock the KidK receptr>T PR 4 tNorAd releape
Uses # tratment oh Pheochromð uytomq
4 Rynad's Synrome
y t e a n e h t o urinaAy e fehHon
Dihydroergotamine
btoeke
ana geheally ,
HydrogenaB
Egolomine a Ergotoxin
Shouw prslia
Natwal alkalod
& ahtagon/sa eceptr
agooist
hydary
(s)-9, 0-dhydo0 -12-
H
A ametyl-s-Cpheny/mehy-
ergotamah-316, 28'-trione
MOA block o re ceptor
igTaine 4 Headad
#featment
Oses pphylaxis o
Combinatim wih hepaNn in
yein +hrornbosis
pos apeyatue dep
Pra2osin
N J-co-
cho aurmino-G,1-dimethaxy- 2 y-(2-5unoyi-
NH Piperqin-1-yT| Gunaaeeine
MOA-SelechueX, blocken> TPR
t AntbypertensiUr agent
Ses
at Kayauel'S Synerne
Symptemadiedreatmento
U s e d as an adjucent io he
uTinay obstactron CouSe be fpdstatje bypertaophy
B-Blockers
ANon Selecttve odaß blocker Labeltt6t Caruedilsf
pindstol
Non Selectjue Pbtocke Padpranofol,
Cadioselectue ea ocke Atenstot, Melopo
Esimstst, isoproj
aketocko Butoxmine
SAR OF B-Bockers
Clases
0 s u c h a Boloclkers clagsi fied into two
nodA
1 Hoylehahstamines -
Sotalst, LebeBa)t
Atenstat, meroprstt,
2. Aryloxy poponstamioe - Propransts,
Acebutast, eh
Asylet ouhstamine
CH-CH- NH- R
Ay ethahs Amine2
ttSussHtuhon o -OH a 3 at R, AR, wit, bulky alkyi qup
at NH-R Sho Hgonis AeHuily
CH
HO CHOCH-NH-CH
g0pmerenst
c/soporeraine
ubsHtuhon dh -c apaR2Ra> Htntagonistie Aetiuily
CH
c CHOH-CH- NH-CH
C Dichloropnterensf
-OHqoup at ben 2ene 7in,ust bar agmst oplasung with
other shoos
aion
ahtanoniHc aisn
Slonamide
enhanceBlbloceng action
metylswfsmte atol af p0s1 Hon -
,CH
CHOH-CH- NH-CHc
cH
Sotols
mauntaun
addod to'N
LPhenyl ehyl, hydioxypheylelyl q y
Hhe B:aloclang acuur
C
CH
CHOH-CH,-NHH CH CHO
HO
Lebetala
.R
N,N-disubsHtuia - Inactiue -N
2
-methyl Subs+tua> Activiy - CH NHR
AOO,
AayloxyY P D P a s t a m i n e
-CHCH-CH- NH-R
NHR CH c
A
Ayl oxy prtpahsf
Amin NIOre potent ha
oryl ethoUhstaminee
auThese ane as
alnhe ouelal
Vavious modificas" may
olloco 4 ehahulamine
between
aaomaie TINa
-OCH gnup
essettal for acuiul
L A s - o C - C H O H - C H - 1 ,
be w o e l in plae q
n e m a l eTiDg may
F Diboeent types
phehy- C9
H -p
CHOH-CH-NH-CHCCH
Pappoahstst
Non Selecive p blcker
H O-CH-CHOH-CH-NH-HCCH
Pindstt
P-CH-CHO-CH-NH-CHCH
Ateholst P blocker
OHCHO > Metopstsf
CHCONH
AHkehy) d alkehyly paesent in ortho posi Hon
asoups ushen
Phehy! ring giues gooad Batagonist actiol
OCH-CHO1-C-N-CH 3
CH-CHOH-CH-NH-CHCC' CH
CH-CH-CH OCHCH-CH
Alprented Oxprenstst
Eegdl
StusHfulia o-CH-Oc, NO, gnup on pheyl
done a 2,23 POsiHon, o 4posit jon is less 5auounid.
,C
Ch-CHOH-CHNH-CH c
C
1O c
Mehprahstst
OCoch
1. Pnpranolo C forn mre poten
OCHCHOH-CH-H-OH
C-c
CRS) +sopopylaino-3-Ct-naphthyloxy)
propurh-2-61
MOA bloceing he Bi4 Ba actuil
yocandu a) atiuiL demone, LReninreleqse
Aso have men Stali i a ppe
Sunthesis -naphths
O NJaDH -CH-CH-CH
folo+ CCH-OH-C
-naphHs
epichlo hydin
Ch
NH-OH
soppy/ amine
CCnoy-Ch Propraneft
NH-CHC
Uses # HypAfengjon
Caduac arylhmIq
Myoeadial nfaneton
2. MetPTanool
OCH-CHOH-CH-NH-CH
CH (RS) y-(2-hydoXy-3-isoproplamino prpoy)
0 - 2,2,6-trimethy! phenyl acelote
cH,
OCOCH
bloeken with out 1A
Non SeleciueB
MOA Staliui Proprty
aso has mem,
Glaucoma
tratment ok
USes tteye covps in
10P
3. Atenslel
QH Che
0 - C H - C H - C H - N H - C H O
(RS) 4-C-hydoxy-s-isopmpylamino prnpoxy)-
- phenylacetamjdes
CHCON
o i h o u t isA
bloctce
SelecHue B,
MOA
t Hpetension
Uses H A 9 t n a pechoiS
Caydiqc arMhn|9 jhehrawal,
Syptors d al cshst us
fnanagement dk
4. Betaxsl6l Ch
pCh-CH-C NH-C _cch u-C2-Cyclopvopyl meoxy) et
CRS)--1-
phenoxyJ-3-| 1sopmpl amino
C ch0-Ch
propab-2+6
blocke
wthout SA
IDA SelecHue B, Glaueomna
# eyedops in
# Hypetensim
Ses NeuLoprtectr in gucormaeatrmeh
S. Bisoprblot
Ch 2-isoprnpoxyeho)
(RS)-1-Ju-C
-Cu CH-C-NH-CH Ch
OH mehyl) phenoxy1-3-Isopropy
min0 propo-2-0
CL-0-Ch, Ch O-Ct
ISH
B blocke wibou
MOA SelecHue
Uses t Hypentension
Cardiac rscheni
Management io disease,
aoytmia
hemt
Coonany
used to toeat
y e c a n d i a tnhancHon
GEsmolol
-Ch CH-CH- NH-CH
Methy31y-2-bycdouxy -3-(soprp
ch-Ch-Co0- en aumin0) prpoy Pheyy prpaboate
OA Bbtocker wihou ISA
Uses t used io SupTauentsjcuda tachycansd49
MManagoment atias fibrilah
4HyperlenSim
ealy tacaBoen myocardia 1tacho
Meoprsis
0-CHCHCH-NH-CH3
RS)-1-Isopropylaino -3-|4-(2:mehoy et)
Ch-Ch Co-C phenox4-propa- 2-6
B o e k e r oi out iSA
M0A
ses Hyperensim
candiac amy rniq d
Argina pectoriss
eanly mahgemert acte myocOAdial
* beat bailuna
Used ap an
adjuce»t in he
hy pehyuidism teaent o
8.Labe tadol
C
CHOH-Q4-NH-CH (RS-2-hydtxy- s-[hydxya1-meyl
C 3-phelpmpyt anmino) emy1
CONM benoamde
OH
MOA NO Selec HUE - d,B blocker, with ISA
, blocking TPR
Use per len sim S1m
nduced hypeafes
pregnauh y-
9. Caruedils
OH
HN CM-CH-Ch NH-CH-C%-O
N- 3-CO4-CaThazst4yl-oxy)-2-hydmxy propy!|-2-(2-methoxy
Phenoxy) ehyl ay ine
MjOA 4B-bl ocee
Oses yahagomentok CH
Hyper ehsim
