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Drug-Target Interaction

Drug

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PubChem ID:4680
Structure:
Synonyms:
1-((3,4-Dimethoxyphenyl)methyl)-6,7-dimethoxyisoquinoline
1-(3,4-Dimethoxy-benzyl)-6,7-dimethoxy-isoquinoline
1-(3,4-dimethoxybenzyl)-6,7-dimethoxyisoquinoline
1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxyisoquinoline
1-[(3,4-Dimethoxyphenyl)methyl]6,7-dimethoxyisoquinoline
1-[(3,4-Dimethoxyphenyl)methyl]6,7-dimethoxyisoquinoline;
1-{[3,4-bis(methyloxy)phenyl]methyl}-6,7-bis(methyloxy)isoquinoline
4-[(6,7-Dimethoxyisoquinolyl)methyl]-1,2-dimethoxybenzene
5-21-06-00182 (Beilstein Handbook Reference)
58-74-2
58-74-2 (FREE BASE )
6,7-Dimethoxy-1-(3,4-dimethoxybenzyl)isoquinoline
6,7-Dimethoxy-1-veratrylisoquinoline
61-25-6
61-25-6 (HCL)
61-25-6 (hydrochloride)
AB00053515
AC1L1IPM
AC1Q4CFN
ACon1_000238
ACon1_002094
AIDS-000185
AIDS000185
AKOS000277460
Alapav
BAS 00674058
BPBio1_000470
BRD-K15567136-001-01-1
BRD-K15567136-003-06-6
BRN 0312930
BSPBio_000426
BSPBio_002153
C06533
C20H21NO4
Cardiospan
Cardoverina
CAS-61-25-6
CCG-202821
Ceraspan
Cerebid
Cerespan
CHEMBL19224
Chlorhydrate de Papaverine
D07425
DB01113
DB07725
Delapav
Dilaves
Dispamil
DivK1c_000321
Drapavel
Durapav
Dynovas
EINECS 200-397-2
EV1
Forpavin
Genabid
HSDB 3147
IDI1_000321
Isoquinoline, 1-((3,4-dimethoxyphenyl)methyl)-6,7-dimethoxy-
Isoquinoline, 1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxy-
Isoquinoline, 6,7-dimethoxy-1-veratryl-
Isoquinoline, 6,7-dimethoxy-1-veratryl- (8CI)
Isoquinoline, 6,7-dimethoxy-1-veratryl-(8Cl)
KBio1_000321
KBio2_000471
KBio2_003039
KBio2_005607
KBio3_001653
KBioGR_000914
KBioSS_000471
Lopac-P-3510
Lopac0_000957
LS-85584
MEGxp0_001880
Mesotina (TN)
Myobid
NCGC00015810-01
NCGC00015810-02
NCGC00015810-03
NCGC00015810-04
NCGC00015810-05
NCGC00015810-06
NCGC00015810-07
NCGC00015810-08
NCGC00015810-09
NCGC00024428-03
NCGC00024428-04
nchembio.317-comp11
NCI60_003183
NINDS_000321
NSC 136630
NSC136630
NSC35443
NSC35443 (HCL)
Oprea1_387689
Oprea1_810508
Pameion
Pamelon
Panergon
PAP H
Papacon
Papalease
Papanerin
Papanerin-hcl
Papanerine
Papavarine Chlorhydrate
Papaverin
Papaverina
Papaverina [Italian]
Papaverine
Papaverine (BAN)
Papaverine Chlorohydrate
Papaverine Hcl
Papaverine Hydrochloride
Papaverine Monohydrochloride
Papaverine [BAN]
Papaverinium Chloride
Papaversan
Papital T.R.
Paptial T.R.
Pavabid
Pavabid Hp
Pavacap
Pavacels
Pavacen
Pavacot
Pavagen
Pavarine
Pavatest
Pavatine
Pavatym
Paverolan
Paveron
Pavnell
Prestwick0_000583
Prestwick1_000583
Prestwick2_000583
Prestwick3_000583
Qua bid
Ro-Papav
Robaxapap
RS 47
S-M-R
SDCCGMLS-0003037.P003
SPBio_001015
SPBio_002645
Spectrum2_000978
Spectrum3_000537
Spectrum4_000467
Spectrum5_001188
Spectrum_000071
ST023301
STK039035
STOCK1N-09376
TNP00305
UNII-DAA13NKG2Q
Vasal
Vaso-Pav
WLN: T66 CNJ B1R CO1 DO1& HO1 IO1
ZINC00056555
ATC-Codes:

Target

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Uniprot ID:PDE4B_HUMAN
Synonyms:
cAMP-specific 3',5'-cyclic phosphodiesterase 4B
DPDE4
PDE32
EC-Numbers:3.1.4.17
Organism:Homo sapiens
Human
PDB IDs:1F0J 1JP1 1JP2 1RO6 1RO9 1ROR 1TB5 1XLX 1XLZ 1XM4 1XM6 1XMU 1XMY 1XN0 1XOS 1XOT 1Y2H 1Y2J 2CHM 2QYL 3D3P 3HC8 3HDZ
Structure:
3HDZ

Binding Affinities:

Ki: Kd:Ic 50:Ec50/Ic50:
----
----
----

References:

210235
Papaverine and Ro 20-1724 inhibit cyclic nucleotide phosphodiesterase activity and increase cyclic AMP levels in psoriatic epidermis in vitro.. L J Rusin; E A Duell; J J Voorhees (1978) The Journal of investigative dermatology display abstract
The comparative inhibitory potency of papaverine and Ro 20-1724 (4-(3-butoxy-4-methoxybenzyl)-2-imidazolidinone) on cyclic AMP-phosphodiesterase (cAMP-PDE) and cyclic GMP-phosphodiesterase (cGMP-PDE) activities and their effect on the levels of cAMP and cGMP were examined in psoriatic epidermis. At concentrations of 5 X 10(-4) M, papaverine inhibited the hydrolysis of both cAMP and cGMP by either the low or high Km psoriatic epidermal PDE nearly 100% (p less than .0001) while Ro 20-1724 selectively inhibited the hydrolysis of cAMP 94% (p less than .0001) but had no significant effect on cGMP hydrolysis. When keratomed psoriatic epidermal slices were incubated in 5 X 10(-4) M papaverine or Ro 20-1724 the tissue levels of cAMP were increased 343% or 1395% respectively (p less than .001) with no concomitant change in the levels of cGMP. Selective inhibition of cAMP hydrolysis by Ro 20-1724 and its greater effectiveness in elevating cAMP levels in slices of psoriatic epidermis is one explanation for its clinical superiority in treating psoriatic lesions.
2995647
7-Bromo-1,5-dihydro-3,6-dimethylimidazo[2,1-b]quinazolin-2(3H)- one (Ro 15-2041), a potent antithrombotic agent that selectively inhibits platelet cyclic AMP-phosphodiesterase.. R Muggli; T B Tschopp; E Mittelholzer; H R Baumgartner (1985) The Journal of pharmacology and experimental therapeutics display abstract
This study with the new analog Ro 15-2041 (7-bromo-1,5-dihydro-3,6-dimethylimidazo[2,1-b]quinazolin-2(3H)-on e) confirms and substantially extends the activity spectrum of imidazoquinazolinones as potent platelet function inhibitors. Ro 15-2041 inhibited platelet aggregation induced by all common platelet agonists in platelet-rich plasma obtained from various species including man (IC50 = 1-3 microM). The compound potentiated platelet inhibition by prostacyclin, the prostacyclin-induced increase of intraplatelet cyclic (c) AMP levels and inhibited the collagen-induced release of serotonin and beta-thromboglobulin. Ro 15-2041 reduced the increase and accelerated the normalization of cytosolic free Ca++ in thrombin-stimulated human platelets. Ro 15-2041 is a potent (IC50 = 70 nM) and selective inhibitor of platelet cAMP-phosphodiesterase activity. Whereas Ro 15-2041 caused complete inhibition of cAMP-phosphodiesterase activity in human platelet supernatants, breakdown of cAMP in cardiac homogenates was depressed to maximally 50%. In human brain and rabbit uterus Ro 15-2041 was at least 1000 times less potent. By comparison, papaverine fully inhibited phosphodiesterase activity in all four tissues with similar IC50 values of about 5 microM. Furthermore, Ro 15-2041 selectively inhibited cAMP-phosphodiesterase activity of a bovine calmodulin-independent but not of a calmodulin-dependent enzyme preparation. The compound exhibited significant p.o. activity in various ex vivo and in vivo platelet function tests.
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