adipiplon - CAS 840486-93-3
Catalog number: 840486-93-3
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C18H18FN7
Molecular Weight:
351.39
COA:
Inquire
Targets:
GABA Receptor
Description:
Adipiplon is GABAA receptor partial agonist. It can bind to the α3 subtype. Adipiplon is one of the first drugs selected for clinical development which is able to discriminate between α2 and α3, as well as showing little affinity for the α1 or α5 subtypes .Adipiplon is being researched as a potential medication for the treatment of anxiety and insomnia, and in 2008 it was being used in Phase IIb trials. But these trials were suspended after next-day side effects were discovered.
Purity:
98%
Appearance:
Powder
Synonyms:
NG-273;7-((2-(3-fluoropyridin-2-yl)-1H-imidazol-1-yl)methyl)-2-methyl-8-propyl-[1,2,4]triazolo[1,5-c]pyrimidine
Solubility:
Soluble in DMSO
Storage:
-20℃ Freezer
MSDS:
Inquire
Application:
anxiety and insomnia
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
InChIKey:
UAMAIHOEGLEXSV-UHFFFAOYSA-N
InChI:
InChI=1S/C18H18FN7/c1-3-5-13-15(22-11-26-17(13)23-12(2)24-26)10-25-9-8-21-18(25)16-14(19)6-4-7-20-16/h4,6-9,11H,3,5,10H2,1-2H3
Canonical SMILES:
CCCC1=C(N=CN2C1=NC(=N2)C)CN3C=CN=C3C4=C(C=CC=N4)F
Current Developer:
Ligand Pharmaceuticals
1.Discriminative stimulus properties of GABAA receptor positive allosteric modulators TPA023, ocinaplon and NG2-73 in rats trained to discriminate chlordiazepoxide or zolpidem.
Vinkers CH;Olivier B;Hanania T;Min W;Schreiber R;Hopkins SC;Campbell U;Paterson N Eur J Pharmacol. 2011 Oct 1;668(1-2):190-3. doi: 10.1016/j.ejphar.2011.06.054. Epub 2011 Jul 8.
There is increased understanding that distinct GABA(A) receptor subtypes mediate different effects of classical benzodiazepines. Here, we aimed to define the contributions of α(1)-containing subtypes of the subtype-selective GABA(A) receptor positive allosteric modulators TPA023, ocinaplon, and NG2-73 using drug discrimination. We characterized these compounds with defined subunit preferences in rats that were trained to discriminate either the non-selective benzodiazepine chlordiazepoxide (CDP, 5.0 mg/kg) or the α(1)-selective drug zolpidem (1.5 mg/kg). In short, CDP but not zolpidem generalized to the CDP cue. In contrast, zolpidem-trained rats showed opposite effects and generalized to zolpidem but not to CDP, while the response rate reducing effects of both ligands were comparable. Moreover, TPA023, lacking efficacy at the GABA(A) receptor α(1) subunit, occasioned dose-dependent CDP-appropriate responding but generalized only to around 10% to zolpidem. Both ocinaplon and NG2-73 completely generalized to both the CDP and zolpidem cue. Overall, our data confirm and extend the previous findings in rats that compounds that lack efficacy at α(1)-containing GABA(A) receptors generalize to CDP, whereas the opposite holds true for α(1)-preferential compounds, which generalize to the α(1)-selective positive allosteric modulator zolpidem.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related GABA Receptor Products


CAS 130477-52-0 L-655,708

L-655,708
(CAS: 130477-52-0)

L-655,708, an inverse agonist of α5 subunit involved in GABAA receptor, has been found to exhibit cognitive performance improvement in biological studies.

CAS 188116-07-6 AWD 131-138

AWD 131-138
(CAS: 188116-07-6)

AWD 131-138 is a partial agonist of GABAA receptor with low affinity for the benzodiazepine binding site. AWD 131-138 exhibits potent anticonvulsant and anxioly...

CAS 783331-24-8 MRK 016

MRK 016
(CAS: 783331-24-8)

MRK-016 is a selective α5 subunit-containing GABAA negative allosteric modulator with EC50 value of 3 nM. It has nootropic properties. MRK-016 can produce rapid...

CAS 123557-91-5 rac BHFF

rac BHFF
(CAS: 123557-91-5)

BHFF is a positive allosteric modulator of GABAB receptor that increases the potency and efficacy of GABA. BHFF displays anxiolytic activity in vivo.

CAS 1236105-75-1 PHP 501 trifluoroacetate

PHP 501 trifluoroacetate
(CAS: 1236105-75-1)

PHP 501 trifluoroacetate is potent GABAA antagonist (Ki = 0.0028 μM at rat GABAA receptors; IC50 = 0.024 μM at human α1β2γ2 GABAA-expressing tsA201 cells), with...

CAS 21715-46-8 Etifoxine

Etifoxine
(CAS: 21715-46-8)

Etifoxine, also called as HOE 36801 or Stresam, is a positive allosteric modulator of GABAreceptors that produces anxiolytic effects by preferentially modulatin...

CAS 91917-65-6 Ro 15-4513

Ro 15-4513
(CAS: 91917-65-6)

Ro 15-4513, a high affinity benzodiazepine ligand, acts as a competitive antagonist, and can therefore be an antidote to the acute impairment caused by alcohol....

CAS 733717-87-8 SCH-50911

SCH-50911
(CAS: 733717-87-8)

CH-50911 is a selective GABA-B antagonist with IC50 value of 1.1 μM. It is developed by Schering-Plough Corporation. CH-50911 is often used in pharmacology rese...

Chemical Structure

CAS 840486-93-3 adipiplon

Quick Inquiry

Verification code

Featured Items