Pagoclone | CI-1043 | RP-62955 | IP-456 | CAS#133737-32-3 | GABA receptor agonist

Pagoclone
featured

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.

Chemical Structure

Pagoclone

CAS# 133737-32-3

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 326953
Name: Pagoclone
CAS#: 133737-32-3
Chemical Formula: C23H22ClN3O2
Exact Mass: 407.14
Molecular Weight: 407.898
Elemental Analysis: C, 67.73; H, 5.44; Cl, 8.69; N, 10.30; O, 7.84

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 325
25mg	USD 950
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

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

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).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:

Product Data

Instruction:

View handling instruction

Biological target:	Pagoclone, also known as CI-1043; IP-456; RP-62955; RP-59037, is a GABA receptor agonist.
In vitro activity:	TBD
In vivo activity:	TBD

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	10.0	24.52

Preparing Stock Solutions

The following data is based on the product molecular weight 407.90 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:	TBD
In vitro protocol:	TBD
In vivo protocol:	TBD

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.

Mass

Concentration

Volume

M. Wt* g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Dilution Calculator

Calculate the dilution required to prepare a stock solution.

Concentration 1

Volume 1

Concentration 2

Volume 2

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.

Your view history

Pagoclone featured