U 89843A

Positive allosteric modulator of GABAA receptors CAS# 157013-85-9

U 89843A

Catalog No. BCC7466----Order now to get a substantial discount!

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Chemical structure

U 89843A

3D structure

Chemical Properties of U 89843A

Cas No. 157013-85-9 SDF Download SDF
PubChem ID 56972182 Appearance Powder
Formula C16H24ClN5 M.Wt 321.85
Type of Compound N/A Storage Desiccate at -20°C
Synonyms PNU 89843
Solubility Soluble to 25 mM in water and to 50 mM in DMSO
Chemical Name 6,7-dimethyl-2,4-dipyrrolidin-1-ylpyrrolo[2,3-d]pyrimidine;hydrochloride
SMILES CC1=CC2=C(N1C)N=C(N=C2N3CCCC3)N4CCCC4.Cl
Standard InChIKey MNKBXPNQWKUSKU-UHFFFAOYSA-N
Standard InChI InChI=1S/C16H23N5.ClH/c1-12-11-13-14(19(12)2)17-16(21-9-5-6-10-21)18-15(13)20-7-3-4-8-20;/h11H,3-10H2,1-2H3;1H
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of U 89843A

DescriptionPositive allosteric modulator of GABAA receptors. Enhances GABA-induced Cl- currents in the α1β2γ2, α3β2γ2 and α6β2γ2 subtypes. Causes sedation in vivo following i.v. administration without losing "righting reflex". Also displays antioxidant activity.

U 89843A Dilution Calculator

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U 89843A Molarity Calculator

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Preparing Stock Solutions of U 89843A

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.107 mL 15.5352 mL 31.0704 mL 62.1407 mL 77.6759 mL
5 mM 0.6214 mL 3.107 mL 6.2141 mL 12.4281 mL 15.5352 mL
10 mM 0.3107 mL 1.5535 mL 3.107 mL 6.2141 mL 7.7676 mL
50 mM 0.0621 mL 0.3107 mL 0.6214 mL 1.2428 mL 1.5535 mL
100 mM 0.0311 mL 0.1554 mL 0.3107 mL 0.6214 mL 0.7768 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on U 89843A

U-89843A is a novel allosteric modulator of gamma-aminobutyric acidA receptors.[Pubmed:8531107]

J Pharmacol Exp Ther. 1995 Dec;275(3):1390-5.

A group of pyrrolopyrimidine derivatives were examined for their interaction with rat recombinant gamma-aminobutyric acid (GABA)A receptors using the whole cell patch clamp and equilibrium binding techniques. In the alpha 1 beta 2 gamma 2 subtype of GABAA receptors expressed in human embryonic kidney cells, a prototype pyrrolopyrimidine, U-89843A (7H-pyrrol[2,3-d]pyrimidine,6,7-methyl-2,4-di- 1-pyrrolidinyl,hydrochloride), dose-dependently enhanced 5 microM GABA-induced Cl- currents with a maximal enhancement of 362 +/- 91%, a half-maximal concentration of 2 +/- 0.4 microM and a slope factor of 1.1 +/- 0.4. The drug also inhibited [35S]t-butylbicyclophosphorothionate binding in rat cerebrocortical membranes with a similar half-maximal inhibitory concentration. The enhancement of Cl- currents by U-89843A was insensitive to Ro 15-1788 (a benzodiazepine antagonist), was also observed in the alpha 3 beta 2 gamma 2 and alpha 6 beta 2 gamma 2 subtypes (no selectivity to different alpha-isoforms unlike many benzodiazepines), but was absent in the receptor subtypes consisting of two subunits (alpha 1 beta 2, alpha 1 gamma 2 and beta 2 gamma 2). It has been known that neurosteroids and barbiturates are uniformly active in both the two subunit receptors, substituted pyrazinones are only active in the alpha 1 beta 2 subtype and loreclezole is active in the subtypes containing beta 2. We propose that U-89843A interacts with an allosteric site on GABAA receptors distinct from the sites for benzodiazepines, barbiturates, neurosteroids, substituted pyrazinones or loreclezole.(ABSTRACT TRUNCATED AT 250 WORDS)

Inhibition of Ca2+-pump ATPase and the Na+/K+-pump ATPase by iron-generated free radicals. Protection by 6,7-dimethyl-2,4-DI-1- pyrrolidinyl-7H-pyrrolo[2,3-d] pyrimidine sulfate (U-89843D), a potent, novel, antioxidant/free radical scavenger.[Pubmed:8619892]

Biochem Pharmacol. 1996 Feb 23;51(4):471-6.

Preincubation of red blood cell (RBC) membranes with a model system known to generate reactive oxygen species (ROS) and free radicals (200 microM ferrous sulfate and 200 microM EDTA, Fe2+/EDTA) resulted inhibition of the Na+/K+ -pump ATPases was also associated with membrane protein crosslinking and lipid peroxidation, the latter as monitored by the formation of thiobarbituric acid reactive substances (TBARS). Inhibition of the ion transport ATPases, protein cross-linking and formation of TBARS were prevented by U-89843D in a concentration-dependent manner, with half-maximal protection seen at 0.3 microM. U-89843D was more potent than the classical antioxidant butylated hydroxytoluene. Neither U-89843D nor the solvent DMSO had any effect on the assay of TBARS. U-89843D exerted only minimal inhibitory activity on ATPase activities. Thus, U-89843D was potent in vitro in preventing a variety of membrane-damaging reactions mediated by ROS. It is suggested that protection of membranes from ROS-mediated damage is of potential usefulness in the prevention and treatment of certain disease processes.

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