Pagoclone Inhibitor

Pagoclone is a GABA receptor agonist potentially for the treatment,of stuttering, panic disorder, and generalized anxiety. It is a partial agonist at alpha1-, alpha2- and alpha5-containing GABAA receptors and a full agonist at receptors containing an alpha3 subunit. It binds with roughly equivalent high affinity (0.7-9.1nM) to the benzodiazepine binding site of human GABAA receptors containing either an alpha1, alpha2, alpha3, or alpha5 subunit.

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.
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.
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.
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.

Small volumes of Pagoclone, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

MBS5758687 is an inhibitor targeting Pagoclone.