Synthesis and biological characterization of [3H] (2-amino-4,5,6,7-tetrahydrobenzo[b]thiophen-3-yl)-(4-chlorophenyl)-methanone, the first radiolabelled adenosine A1 allosteric enhancer

Pier Giovanni Baraldi; Maria Giovanna Pavani; Edward Leung; Allan R. Moorman; Katia Varani; Fabrizio Vincenzi; Pier Andrea Borea; Romeo Romagnoli

doi:10.1016/j.bmcl.2005.11.037

Synthesis and biological characterization of [3H] (2-amino-4,5,6,7-tetrahydrobenzo[b]thiophen-3-yl)-(4-chlorophenyl)-methanone, the first radiolabelled adenosine A1 allosteric enhancer

Pier Giovanni Baraldi
, Maria Giovanna Pavani
, Edward Leung
, Allan R. Moorman
, Katia Varani
, Fabrizio Vincenzi
, Pier Andrea Borea
, Romeo Romagnoli

University of Ferrara
King Pharmaceuticals

Research output: Contribution to journal › Article › Academic › peer-review

Abstract

Among the adenosine A1 allosteric enhancers reported so far, compound (2-amino-4,5,6,7-tetrahydrobenzo[b]thiophen-3-yl)-(4-chlorophenyl)- methanone 1 (named T-62) has shown biological properties similar to those of PD 81,723, the reference A1 allosteric enhancer and it has been more fully pharmacologically investigated. The preparation of the radiolabelled form of compound 1 and its characterization by saturation binding experiments are reported. These studies allowed us to demonstrate for the first time the existence of a specific, allosteric site on the A1 receptor. © 2005 Elsevier Ltd. All rights reserved.

Original language	English
Pages (from-to)	1402-1404
Journal	Bioorganic & medicinal chemistry letters
Volume	16
Issue number	5
DOIs	https://doi.org/10.1016/j.bmcl.2005.11.037
Publication status	Published - 1 Mar 2006
Externally published	Yes

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10.1016/j.bmcl.2005.11.037

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Baraldi, P. G., Pavani, M. G., Leung, E., Moorman, A. R., Varani, K., Vincenzi, F., Borea, P. A., & Romagnoli, R. (2006). Synthesis and biological characterization of [3H] (2-amino-4,5,6,7-tetrahydrobenzo[b]thiophen-3-yl)-(4-chlorophenyl)-methanone, the first radiolabelled adenosine A1 allosteric enhancer. Bioorganic & medicinal chemistry letters, 16(5), 1402-1404. https://doi.org/10.1016/j.bmcl.2005.11.037

@article{00e14a2b48884e7cae6b95b9a7e0232d,

title = "Synthesis and biological characterization of [3H] (2-amino-4,5,6,7-tetrahydrobenzo[b]thiophen-3-yl)-(4-chlorophenyl)-methanone, the first radiolabelled adenosine A1 allosteric enhancer",

abstract = "Among the adenosine A1 allosteric enhancers reported so far, compound (2-amino-4,5,6,7-tetrahydrobenzo[b]thiophen-3-yl)-(4-chlorophenyl)- methanone 1 (named T-62) has shown biological properties similar to those of PD 81,723, the reference A1 allosteric enhancer and it has been more fully pharmacologically investigated. The preparation of the radiolabelled form of compound 1 and its characterization by saturation binding experiments are reported. These studies allowed us to demonstrate for the first time the existence of a specific, allosteric site on the A1 receptor. {\textcopyright} 2005 Elsevier Ltd. All rights reserved.",

author = "Baraldi, \{Pier Giovanni\} and Pavani, \{Maria Giovanna\} and Edward Leung and Moorman, \{Allan R.\} and Katia Varani and Fabrizio Vincenzi and Borea, \{Pier Andrea\} and Romeo Romagnoli",

year = "2006",

month = mar,

day = "1",

doi = "10.1016/j.bmcl.2005.11.037",

language = "English",

volume = "16",

pages = "1402--1404",

journal = "Bioorganic \& medicinal chemistry letters",

issn = "0960-894X",

publisher = "Elsevier Limited",

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}

Baraldi, PG, Pavani, MG, Leung, E, Moorman, AR, Varani, K, Vincenzi, F, Borea, PA & Romagnoli, R 2006, 'Synthesis and biological characterization of [3H] (2-amino-4,5,6,7-tetrahydrobenzo[b]thiophen-3-yl)-(4-chlorophenyl)-methanone, the first radiolabelled adenosine A1 allosteric enhancer', Bioorganic & medicinal chemistry letters, vol. 16, no. 5, pp. 1402-1404. https://doi.org/10.1016/j.bmcl.2005.11.037

Synthesis and biological characterization of [3H] (2-amino-4,5,6,7-tetrahydrobenzo[b]thiophen-3-yl)-(4-chlorophenyl)-methanone, the first radiolabelled adenosine A1 allosteric enhancer. / Baraldi, Pier Giovanni; Pavani, Maria Giovanna; Leung, Edward et al.
In: Bioorganic & medicinal chemistry letters, Vol. 16, No. 5, 01.03.2006, p. 1402-1404.

Research output: Contribution to journal › Article › Academic › peer-review

TY - JOUR

T1 - Synthesis and biological characterization of [3H] (2-amino-4,5,6,7-tetrahydrobenzo[b]thiophen-3-yl)-(4-chlorophenyl)-methanone, the first radiolabelled adenosine A1 allosteric enhancer

AU - Baraldi, Pier Giovanni

AU - Pavani, Maria Giovanna

AU - Leung, Edward

AU - Moorman, Allan R.

AU - Varani, Katia

AU - Vincenzi, Fabrizio

AU - Borea, Pier Andrea

AU - Romagnoli, Romeo

PY - 2006/3/1

Y1 - 2006/3/1

N2 - Among the adenosine A1 allosteric enhancers reported so far, compound (2-amino-4,5,6,7-tetrahydrobenzo[b]thiophen-3-yl)-(4-chlorophenyl)- methanone 1 (named T-62) has shown biological properties similar to those of PD 81,723, the reference A1 allosteric enhancer and it has been more fully pharmacologically investigated. The preparation of the radiolabelled form of compound 1 and its characterization by saturation binding experiments are reported. These studies allowed us to demonstrate for the first time the existence of a specific, allosteric site on the A1 receptor. © 2005 Elsevier Ltd. All rights reserved.

AB - Among the adenosine A1 allosteric enhancers reported so far, compound (2-amino-4,5,6,7-tetrahydrobenzo[b]thiophen-3-yl)-(4-chlorophenyl)- methanone 1 (named T-62) has shown biological properties similar to those of PD 81,723, the reference A1 allosteric enhancer and it has been more fully pharmacologically investigated. The preparation of the radiolabelled form of compound 1 and its characterization by saturation binding experiments are reported. These studies allowed us to demonstrate for the first time the existence of a specific, allosteric site on the A1 receptor. © 2005 Elsevier Ltd. All rights reserved.

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UR - https://www.ncbi.nlm.nih.gov/pubmed/16321527

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SP - 1402

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ER -

Synthesis and biological characterization of [3H] (2-amino-4,5,6,7-tetrahydrobenzo[b]thiophen-3-yl)-(4-chlorophenyl)-methanone, the first radiolabelled adenosine A1 allosteric enhancer

Abstract

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