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Drug-Target Interaction

Drug

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PubChem ID:4553
Structure:
Synonyms:
123653-11-2
AC1L1IF7
AC1Q20LP
AR-1K3665
Bio2_000472
Bio2_000952
BRD-K53364951-001-02-6
BSPBio_001264
C080955
C13H18N2O5S
CCRIS 8523
CHEBI:101699
CHEMBL7162
HMS1362P05
HMS1792P05
HMS1990P05
I14-10018
IDI1_002227
IN1319
KBio2_000604
KBio2_003172
KBio2_005740
KBio3_001067
KBio3_001068
KBioGR_000604
KBioSS_000604
LS-90104
Methanesulfonamide, N-(2-(cyclohexyloxy)-4-nitrophenyl)-
N-(2-Cyclohexyloxy-4-nitrophenyl)methanesulfonamide
N-[2-(Cyclohexyloxy)-4-nitrophenyl]methanesulfonamide
N194_SIGMA
NCGC00024892-01
NCGC00024892-02
NCGC00024892-03
nchembio.147-comp10
NS 398
NS-398
NS398
NS4
Tocris-0942
ZINC03791739

Target

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Uniprot ID:PGH2_CAVPO
Synonyms:
COX-2
Cyclooxygenase-2
PGH synthase 2
PGHS-2
PHS II
Prostaglandin G/H synthase 2
Prostaglandin H2 synthase 2
Prostaglandin-endoperoxide synthase 2
EC-Numbers:1.14.99.1
Organism:Cavia porcellus
Guinea pig
PDB IDs:-

Binding Affinities:

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

References:

16945943
Prostaglandin E2 release in gastric antral mucosa of guinea-pigs: basal PGE2 release by cyclo-oxygenase 2 and ACh-stimulated PGE2 release by cyclo-oxygenase 1.. Chikao Shimamoto; Yoshihiko Nakanishi; Ken-ichi Katsu; Takashi Nakano; Takahiro Kubota; Hiroshi Mori; Takashi Nakahari (2006) Experimental physiology display abstract
Prostaglandin E(2) (PGE(2)), which is generated by two isoforms of cyclo-oxygenase (COX(1) and COX(2)), is a key mediator in gastric mucosal defense. In the present study, antral mucosa of guinea-pigs was incubated with various agonists or antagonists in a medium, the PGE(2) concentration of which was measured using a PGE(2) EIA kit. Prostaglandin E(2) was released from the antral mucosa spontaneously (basal PGE(2) release) and acetylcholine (ACh, 10 microM) enhanced the PGE(2) release (ACh-stimulated PGE(2) release) was mediated via intracellular Ca(2+) concentration ([Ca(2+)](i)). Arachidonic acid enhanced both forms of PGE(2) release, and a phospholipase A(2) inhibitor (amylcinnamoyl anthranilic acid) and COX inhibitors (acetylsalicylic acid and indomethacin) decreased them. 5-(4-Chlorophenyl)-1-(4-methoxyphenyl)-3-trifluoromethylpyrazol (SC560, 100 nm, a COX(1)-selective inhibitor) inhibited ACh-stimulated PGE(2) release without any decrease in basal PGE(2) release. N-(2-Cyclohexyloxy-4-nitrophenyl) methanesulphonamide (NS398, 20 microM, a COX(2)-selective inhibitor) decreased basal PGE(2) release without any reduction of ACh-stimulated PGE(2) release. However, ionomycin (a Ca(2+) ionophore) increased PGE(2) release from antral mucosa in the presence of SC560 or NS398, suggesting that COX(1) and COX(2) are regulated by [Ca(2+)](i). These findings indicate that COX(1)-containing cells have ACh receptors but COX(2)-containing cells do not. Moreover, in isolated antral epithelial cells, SC560 decreased basal and ACh-stimulated PGE(2) release, but NS398 did not. In conclusion, in antral mucosa, basal PGE(2) release is mainly maintained by COX(2) of non-epithelial cells, and ACh-stimulated PGE(2) release is maintained by COX(1) of epithelial cells.