Pagoclone
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 326953

CAS#: 133737-32-3

Description: Pagoclone, also known as CI-1043; IP-456; RP-62955; RP-59037, is a GABA receptor agonist potentially for the treatment of stuttering, panic disorder and generalised anxiety. It binds with roughly equivalent high affinity (0.7–9.1 nM) to the benzodiazepine binding site of human GABAA receptors containing either an α1, α2, α3 or α5 subunit. It is a partial agonist at α1-, α2- and α5-containing GABAA receptors and a full agonist at receptors containing an α3 subunit.


Price and Availability

Size
Price

10mg
USD 250
Size
Price

25mg
USD 450
Size
Price

Pagoclone, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 326953
Name: Pagoclone
CAS#: 133737-32-3
Chemical Formula: C23H22ClN3O2
Exact Mass: 407.1401
Molecular Weight: 407.898
Elemental Analysis: C, 67.73; H, 5.44; Cl, 8.69; N, 10.30; O, 7.84


Synonym: Pagoclone; CI-1043; IP-456; RP-62955; RP-59037; CI1043; IP456; RP62955; RP59037. Bextra.

IUPAC/Chemical Name: 2-(7-chloro-1,8-naphthyridin-2-yl)-3-(5-methyl-2-oxohexyl)isoindolin-1-one

InChi Key: HIUPRQPBWVEQJJ-UHFFFAOYSA-N

InChi Code: InChI=1S/C23H22ClN3O2/c1-14(2)7-10-16(28)13-19-17-5-3-4-6-18(17)23(29)27(19)21-12-9-15-8-11-20(24)25-22(15)26-21/h3-6,8-9,11-12,14,19H,7,10,13H2,1-2H3

SMILES Code: O=C1N(C2=NC3=NC(Cl)=CC=C3C=C2)C(CC(CCC(C)C)=O)C4=C1C=CC=C4


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


References

1: Ingham RJ. Comments on article by Maguire et al: pagoclone trial: questionable findings for stuttering treatment. J Clin Psychopharmacol. 2010 Oct;30(5):649-50; author reply 650-1. doi: 10.1097/JCP.0b013e3181f1f130. PubMed PMID: 20841975.

2: Maguire G, Franklin D, Vatakis NG, Morgenshtern E, Denko T, Yaruss JS, Spotts C, Davis L, Davis A, Fox P, Soni P, Blomgren M, Silverman A, Riley G. Exploratory randomized clinical study of pagoclone in persistent developmental stuttering: the EXamining Pagoclone for peRsistent dEvelopmental Stuttering Study. J Clin Psychopharmacol. 2010 Feb;30(1):48-56. doi: 10.1097/JCP.0b013e3181caebbe. PubMed PMID: 20075648.

3: Caveney AF, Giordani B, Haig GM. Preliminary effects of pagoclone, a partial GABA(A) agonist, on neuropsychological performance. Neuropsychiatr Dis Treat. 2008 Feb;4(1):277-82. PubMed PMID: 18728798; PubMed Central PMCID: PMC2515892.

4: de Wit H, Vicini L, Haig GM, Hunt T, Feltner D. Evaluation of the abuse potential of pagoclone, a partial GABAA agonist. J Clin Psychopharmacol. 2006 Jun;26(3):268-73. PubMed PMID: 16702891.

5: Atack JR, Pike A, Marshall G, Stanley J, Lincoln R, Cook SM, Lewis RT, Blackaby WP, Goodacre SC, McKernan RM, Dawson GR, Wafford KA, Reynolds DS. The in vivo properties of pagoclone in rat are most likely mediated by 5'-hydroxy pagoclone. Neuropharmacology. 2006 May;50(6):677-89. Epub 2006 Jan 20. PubMed PMID: 16430927.

6: Lingford-Hughes A, Wilson SJ, Feeney A, Grasby PG, Nutt DJ. A proof-of-concept study using [11C]flumazenil PET to demonstrate that pagoclone is a partial agonist. Psychopharmacology (Berl). 2005 Aug;180(4):789-91. Epub 2005 Sep 14. PubMed PMID: 15986186.

7: Bateson A. Pagoclone Indevus. Curr Opin Investig Drugs. 2003 Jan;4(1):91-5. Review. PubMed PMID: 12625036.

8: Sandford JJ, Forshall S, Bell C, Argyropoulos S, Rich A, D'Orlando KJ, Gammans RE, Nutt DJ. Crossover trial of pagoclone and placebo in patients with DSM-IV panic disorder. J Psychopharmacol. 2001 Sep;15(3):205-8. PubMed PMID: 11565630.