Tracazolate Hydrochloride | Medchemexpress

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Tracazolate Hydrochloride | Medchemexpress

Inhibitors Product Data Sheet Tracazolate hydrochloride • Agonists Cat. No.: HY-B1803A CAS No.: 1135210-68-2 Molecular Formula: C₁₆H₂₅ClN₄O₂ • Molecular Weight: 340.85 Screening Libraries Target: GABA Receptor Pathway: Membrane Transporter/Ion Channel; Neuronal Signaling Storage: Please store the product under the recommended conditions in the Certificate of Analysis. BIOLOGICAL ACTIVITY Description Tracazolate (ICI 136753) hydrochloride is a potent GABAA receptor modulator. Tracazolate hydrochloride has selectivity for β3 and potentiates α1β1γ2s (EC50=13.2 μM), α1β3γ2 (EC50=1.5 μM). Tracazolate hydrochloride has the potency (EC50) determined by the nature of the third subunit (γ1-3, δ, ε) within the receptor complex. Tracazolate hydrochloride possesses anxiolytic and anticonvulsant activity[1][2]. [1] IC₅₀ & Target GABAA In Vitro Tracazolate (ICI 136753) hydrochloride inhibits α1β1ε (EC50=4.0 μM) and α1β3ε (EC50=1.2 μM), α1β3 (EC50=2.7 μM) and α6β3γ (EC50=1.1 μM). Replacement of Ser265 within the β1 subunit with Asn (the β3 counterpart) increases the sensitivity of tracazolate, whereas the opposite mutation (Asnβ3 to Ser) decreases the sensitivity to Tracazolate. Tracazolate [1] hydrochloride interacts with γ-aminobutyric acid GABAA receptors, adenosinereceptors, and phosphodiesterases . Tracazolate hydrochloride (10 μM) increases the maximum current amplitude and enhances the sensitivity of α1β2δ- [2] containing GABAA receptors in oocytes . MCE has not independently confirmed the accuracy of these methods. They are for reference only. REFERENCES [1]. Sally-Anne Thompson, et al. Tracazolate reveals a novel type of allosteric interaction with recombinant gamma-aminobutyric acid(A) receptors. Mol Pharmacol. 2002 Apr;61(4):861-9. [2]. N Zheleznova, et al. alpha1beta2delta, a silent GABAA receptor: recruitment by tracazolate and neurosteroids. Br J Pharmacol. 2008 Mar;153(5):1062-71. McePdfHeight Caution: Product has not been fully validated for medical applications. For research use only. Tel: 609-228-6898 Fax: 609-228-5909 E-mail: [email protected] Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA Page 1 of 1 www.MedChemExpress.com.

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Efficient Synthesis of Pyrazolopyridines Containing a Chromane Backbone Through Domino Reaction
Efficient synthesis of pyrazolopyridines containing a chromane backbone through domino reaction Razieh Navari1, Saeed Balalaie*1,2, Saber Mehrparvar1, Fatemeh Darvish1, Frank Rominger3, Fatima Hamdan1 and Sattar Mirzaie1 Full Research Paper Open Access Address: Beilstein J. Org. Chem. 2019, 15, 874–880. 1Peptide Chemistry Research Center, K. N. Toosi University of doi:10.3762/bjoc.15.85 Technology, P. O. Box 15875-4416, Tehran, Iran, Tel: +98-21-23064226, Fax: +98-21-22889403, 2Medical Biology Received: 07 February 2019 Research Center, Kermanshah University of Medical Sciences, Accepted: 29 March 2019 Kermanshah, Iran and 3Organisch-Chemisches Institut der Published: 11 April 2019 Universitaet Heidelberg, Im Neuenheimer Feld 270, D-69120 Heidelberg, Germany Associate Editor: T. J. J. Müller Email: © 2019 Navari et al.; licensee Beilstein-Institut. Saeed Balalaie* - [email protected] License and terms: see end of document. * Corresponding author Keywords: chromane; domino reaction; fused heterocyclic skeletons; pyrazolopyridines Abstract An efficient approach for the synthesis of pyrazolopyridines containing the aminochromane motif through a base-catalyzed cycliza- tion reaction is reported. The synthesis was carried out through a three-component reaction of (arylhydrazono)methyl-4H-chromen- 4-one, malononitrile, primary amines in the presence of Et3N at room temperature. However, carrying out the reaction under the same conditions without base led to a fused chromanyl-cyanopyridine. High selectivity, high atom economy, and good to high yields in addition to mild reaction conditions are the advantages of this approach. Introduction The synthesis of new fused heterocyclic backbones has always Chromone derivatives have been found to exhibit a broad range been a major challenge in the field of organic synthesis [1-3].
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