Home
Drugs
Targets
Pathways
Ontologies
Cyp450s
Adv.search
Help/FAQ

Drug-Target Interaction

Drug

show drug details
PubChem ID:5278
Structure:
Synonyms:
1-Phthalazineacetic acid,
1-Phthalazineacetic acid, 3-((4-bromo-2-fluorophenyl)methyl)-3,4-dihydro-4-oxo-
3-(4-Bromo-2-fluorobenzyl)-3,4-dihydro-4-oxo-1-phthalazineacetic acid
3-(4-bromo-2-fluorobenzyl)-3,4-dihydro-4-oxo-3H-phthalazin-1-ylacetic acid
3-(4-bromo-2-fluorobenzyl)-4-oxo-3h-phthalazin-1-ylacetic acid
72702-95-5
Bio1_000383
Bio1_000872
Bio1_001361
BSPBio_002576
C17H12BrFN2O3
D03806
DivK1c_006939
ICI 128,436
ICI 128436
ICI-128436
KBio1_001883
KBio2_001963
KBio2_004531
KBio2_007099
KBio3_001796
KBioGR_001855
KBioSS_001963
LS-176986
MK-538
NCGC00024824-01
PONALRESTAT
Ponalrestat (USAN/INN)
Ponalrestat [USAN:BAN:INN]
Ponalrestatum [Latin]
Prodiax
SPBio_001393
SpecPlus_000843
Spectrum2_001467
Spectrum3_001048
Spectrum4_001188
Spectrum_001483
Statil
Tocris-0847

Target

show target details
Uniprot ID:CLAT_RAT
Synonyms:
ChAT
CHOACTase
Choline acetylase
Choline O-acetyltransferase
EC-Numbers:2.3.1.6
Organism:Rat
Rattus norvegicus
PDB IDs:1Q6X 1T1U
Structure:
1T1U

Binding Affinities:

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

References:

2452959
Studies on peripheral nerve and lens in long-term experimental diabetes: effects of the aldose reductase inhibitor statil.. G B Willars; J Townsend; D R Tomlinson; A M Compton; R D Churchill (1988) Metabolism: clinical and experimental display abstract
This study determined the axonal transport of choline acetyltransferase (ChAT) activity and its content in several tissues in nondiabetic control rats and in four groups of rats with streptozotocin-induced diabetes of 6-months duration. Diabetic rats were either untreated, treated only with either the aldose reductase inhibitor Statil (Imperial Chemical Industries, Pharmaceuticals Division, Macclesfield, UK) or insulin, or were given the two in combination. Insulin treatment consisted of a single weekly injection of a long-acting insulin, a regime designed not to control the diabetes, but to provide regular respite from the catabolic dominance of uncontrolled diabetes. Elevated levels of sugars and polyols in the sciatic nerves of untreated diabetic animals were markedly attenuated by Statil. The reduced myo-inositol content and reduced axonal transport of ChAT activity also seen in these nerves were prevented by Statil, but a reduced motor nerve conduction velocity was attenuated only by Statil and insulin in combination. The presence of cataracts in all diabetic animals was associated with hyperhydration of the lens. The level of hydration and presence of cataracts were reduced by Statil, particularly in combination with insulin. ChAT activities of the iris, adrenal gland, and superior cervical ganglion were similar in all groups. Skeletal muscles showed wasting while the ileum showed an increased weight per unit length in diabetic rats. These tissues also displayed alterations in ChAT activities, particularly when referenced to unit weight of tissue, which may have been a consequence of the weight changes rather than diabetes per se.