WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H326953
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.
Hodoodo Cat#: H326953
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
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:
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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: | |
In vitro protocol: | |
In vivo protocol: |
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.