- contraction of skeletal muscles
- exocytosis
.
|
|
|
|
|
|
| b1 | cardiomyocytes (high in SA node, atria, AV node, His-Purkinje system,
and ventricles => positive batmo-, dromo- and inotropic effects),
juxtaglomerular cells, renal arterioles, adipocytes, neurohypophysis |
adrenaline
= noadrenaline |
isoproterenol / isopropylarterenol
/ isopropylnorepinephrine / isoprenaline / isopropylnoradrenaline / d,l-b-[3,4-dihydroxyphenyl]-
a-isoprylaminoethanol
hydrochloride (Isuprel®)
dobutamine hydrochloride (Dobutrex®) SNRI :
|
selective :
|
| b2 (after phosphorylation by BARK, it couples to Gi) | cardiomyocytes (low in SA node, atria, AV node, His-Purkinje system,
and ventricles),
skeletal muscles, smooth muscle (vascular, tracheal and bronchial, stomach, intestine, and gallbladder, detrusor muscle of urinary bladder, uterus), hepatocytes, adipocytes, bronchial glands, ciliary muscle of eye; arterioles (except skin, mucosa and brain) and veins, spleen capsule, b cells of Langerhans' islets in endocrine pancreas, T cells, B cells, monocytes, macrophages |
adrenaline
>> noadrenaline |
isoproterenol / isopropylarterenol / isopropylnorepinephrine / isoprenaline
/ isopropylnoradrenaline / d,l-b-[3,4-dihydroxyphenyl]
-a-isoprylaminoethanol hydrochloride (Isuprel®)
dobutamine hydrochloride (Dobutrex®) clenbuterol (Broncodil®, Broncoterol®, Cesbron®, Clenbuterol Pharmachim®, Contrasmina®, Contraspasmina®, Monores®, Novegam®, Planipart®, Prontovent®, Spiropent®, Spasmo-Mucosolvan®, Ventolase®, Ventipulmin®) selective agonists :
|
ICI 118551
salmeterol albuterol butoxamine dopexamine (Dopacard®) non-subtype-selective b-adrenergic antagonists:
|
| b3 | adipocytes | adrenaline
< noadrenaline |
isoproterenol / isopropylarterenol / isopropylnorepinephrine / isoprenaline
/ isopropylnoradrenaline / d,l-b-[3,4-dihydroxyphenyl]
-a-isoprylaminoethanol hydrochloride (Isuprel®)
dobutamine hydrochloride (Dobutrex®) BRL 37344 |
ICI 118551
BRL 37344 CGP 20712A non-subtype-selective b-adrenergic antagonists:
|
| glucagon receptor | hepatocytes | glucagon |
||
| GLP-1 receptor (GLP1R) | brain, pancreatic b-cell | GLP-1 |
exendin-4 / exenatide (Byetta®), a natural peptide with >50% sequence homology to GLP-1, but with greater potency and longer duration of action, produced in the saliva of the Gila monster (Heloderma suspectum) | exendin-(9-39) |
| GLP-2 receptor (GLP2R) | gastrointestinal tract | GLP-2 |
||
| D1 | postsynaptic in striatum, neocortex | dopamine |
apomorphine
fenoldopam (Corlopam®) SKF38393 pergolide (Celance®, Pharken®, Permax®) |
SCH-23390
SCH-39166 / ecopipam SKF-83566 butyrrophenons phenothiazines thioxanthenes diphenylbutylpiperidine bromocriptine (Ergoset®, Lactismine®, Parlodel®, Parlodel-LAR®, Parlodel-MR®, Pravidel®, Pravidel-Depot®, Serocryptin®) cabergoline (Cabasex®, Sogilen/Dostinex®) (partial antagonist) |
| D5
(it can heterodimerize with g2-containing
GABAA) |
hippocampus, hypothalamus | dopamine |
apomorphine | butyrrophenons
phenothiazines thioxanthenes diphenylbutylpiperidine |
| V2 | distal convoluted tubule and collecting ducts, fetal lung tissue and lung cancer | AVP
/ ADH |
1-deamino-8-D-Arg vasopressin (DDAVP)
/ desmopressin / d[dArg8]VP
desmopressin acetate (Minirin®) deamino[Val4, D-Arg8]AVP |
des Gly-NH29-d(CH2)5[D-Ile2,
Ile4]AVP
d(CH2)5[dIle2, Ile4, Ala-NH29]AVP OPC-31260 SR 121463A VPA-985 YM 087 / conivaptan (Vaprisol®) (also antagonist on V1a ) |
| H2 | vascular smooth muscle cells, ventricular and right atrial cardiomyocytes,
basolateral membrane of parietal cells of stomach, Th2
lymphocytes,
DCs |
histamine |
dimaprit
4(5)-methylhistamine impromidine amthamine |
ranitidine (Ranidil®, Zantac®;
in combination with bismuth subcitrate or subsalicylate as Tritec®,
Pylorid®)
cimetidine (Tagamet®) famotidine (Pepcid®) nizatidine (Axid®, Antizid®, Calmaxid®, Cronizat®, Distaxid®, Gastrax®, Naxidine®, Nizax®, Nizaxid®, Panaxid®, Tazac®, Zanizal®) burimamide (partial agonist in humans, antagonist in rats; also on H3 )
tiotidine iodoaminopotentidine iodoazidopotentidine olopatadine / AL-4943A / KW-4679 (Opatanol®, Patanase®, Patanol®) (low affinity; high affinity for H1 ) |
| CRHR1 | CRF
/ CRH |
cortagine is a CRF1-specific peptidic agonist by synthesis of chimeric peptides derived from human/rat CRF, ovine CRF (oCRF), and sauvagine (Svg) | antalarmin | |
| CRHR2 | CRF
/ CRH |
|||
| LH / hCG receptor | Leydig cells, internal techa, granulosa cells | LH
hCG |
||
| FSH receptor | Sertoli cells, granulosa cells | FSHref |
||
| TSH receptor | thyroid cell,
fibroblast, preadipocytes and adipocytes |
TSH |
||
| calcitonin receptor | calcitonin |
|||
| CGRP receptor (+ CGRPRCP) | CGRP |
BIBN 4096 BS | ||
| adrenomedullin receptor (ADMR) | adrenomedullin |
|||
| GIP receptor | pancreatic islet b-cells | GIP |
||
| PACAPR1 | trigeminal, otic and superior cervical ganglia (prejunctional) and cerebral arteries (postjunctional) | PACAP |
||
| VIPR1 / VPAC1 / PACAPR2 | T cells | PACAP
= VIP
>> helodermin-like peptide
= secretin |
K(15), R(16,) L(27)]VIP(1-7)/GRF(8-27)
[R(16)]ChSn |
|
| VIPR2 / VPAC2 | VIP
PACAP |
RO 25-1553 | ||
| secretin receptor | exocrine pancreas | secretin |
||
| 5-HT4 | hippocampus , gastrointestinal tract | 5-HT |
enantiomeric, substituted benzamides
BIMU8 RS67506 ML10302 |
tropisetron (Navoban®) (weak)
ondansetron (Zofran®) (weak) GR113808 SB204070 |
| 5-HT6 | striatum | 5-HT |
||
| 5-HT7 | hypothalamus, intestine | 5-HT |
||
| EP2 | monocyte-derived dendritic cells | PGE2 |
ONO-AE1-259-01
gemeprost 11-deoxy-PGE1 |
|
| EP3
(also on nuclear envelope) (also GiPCR
and GqPCR) |
neurons, endothelial cells of CNS | PGE2 |
ONO-AE-248;
sulprostone; misoprostol (Cytotec®; Mifeprex® in combination with mifepristone )
gemeprost |
L-826266 |
| EP4 | monocyte-derived dendritic cells, T cells | PGE2 |
gemeprost
11-deoxy-PGE1 |
L-161982 |
| IP | platelets,
smooth muscle cells |
PGI2 / PC
PGE1 |
misoprostol (Cytotec®; Mifeprex® in combination
with mifepristone) |
|
| DP / DP1 | PGD2 |
BW245C | ||
| DP2 / CRTH2 / GPR44 | PGD2 |
|||
| Frizzled homolog 1 | ||||
| Frizzled homolog 2 | fetal kidney and lung and in adult colon and ovary. | |||
| Frizzled homolog 3 | hair follicle | |||
| Frizzled homolog 4 | ||||
| Frizzled homolog 5 | Wnt-5A | |||
| Frizzled homolog 6 | ||||
| Frizzled homolog 7 | poorly differentiated human esophageal carcinomas | |||
| Frizzled homolog 8 | ||||
| Frizzled homolog 9 | brain, testis, eye, skeletal muscle, and kidney | |||
| Frizzled homolog 10 | primary colon cancer | |||
| GC / GBG | ||||
| some odorantsref | tongue | |||
| some sweet molecules | tongue | aspartame
saccharine  |
||
| some bitter molecules | tongue | |||
| A2a | basal ganglia, neutrophils,
vasculature and platelets |
P1 for Ado |
CGS
21680
APEC HENECA ATL-146e |
CSC
ZM241385 DMPX SCH58261 CO66713 xanthines :
|
| A2b | blood vessels, enterocytes | netrin-1
P1 for Ado |
xanthines :
|
|
| P2Y11
(also GqPCR) |
ATP |
|||
| PTHR1 | osteoblasts | PTH
PTHrp |
||
| PTHR2 | osteoblasts | PTH |
||
| MC1R | melanocytes | a-MSH
(agonist)
AgRP
(antagonist) |
melanotan II
PT-141 |
|
| MC2R / ACTH receptor (ACTHR | zonae fasciculata and reticularis of the adrenal cortex | ACTH |
||
| MC3R | tissues other than the adrenal cortex and melanocytes (including arcuate nucleus) | g1-MSH
(agonist)
AgRP
(inverse agonist) |
SHU 9119 | |
| MC4R | arcuate nucleus | AgRP
(inverse agonist) |
SHU 9119
HS014 |
|
| MC5R | ||||
| G protein-coupled receptor 3 (GPR3) / adenylate cyclase constitutive activator (ACCA) | ovarian follicle | |||
| G protein-coupled bile acid receptor 1 (GPBAR1) / TGR5 | placenta and spleen > lung and fetal liver ; resting CD14+ monocytes | bile acids
at 25 µM :
|
Copyright © 2001-2005 Daniele Focosi.
All rights reserved
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