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Alpha2-adrenoreceptors profile modulation. 3.1 (R)-(+)-m-nitrobiphenyline, a new efficient and alpha2C-subtype selective agonist.

Pierre-Antoine Crassous 1 Claudia Cardinaletti 2 Antonio Carrieri 3 Bruno Bruni 4 Massimo Di Vaira 4 Francesco Gentili 2 Francesca Ghelfi 2 Mario Giannella 2 Hervé Paris 1 Alessandro Piergentili 2 Wilma Quaglia 2 Stéphane Schaak 1 Cristian Vesprini 2 Maria Pigini 2, *
* Corresponding author
1 I2MR - Institut de médecine moléculaire de Rangueil
2 Dipartimento di Scienze Chimiche
3 Dipartimento Farmaco-Chimico
4 Dipartimento di Chimica
Abstract : To assess the stereochemical requirements for efficient alpha2C-adrenoreceptor activation, the enantiomeric forms of m-nitrobiphenyline [(+/-)-5] were prepared and tested on cells expressing the human alpha2-adrenoreceptor subtypes. The importance of chirality was confirmed, since the enantiomer (R)-(+)-5 was much more efficient than (S)-(-)-5 in producing alpha2C-activation. Surprising reversal of enantioselectivity was observed with respect to structurally similar biphenyline [(+/-)-1] whose (S)-(-)-form proved the preferred alpha2C-configuration.
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https://www.hal.inserm.fr/inserm-00409859
Contributor : Marie Francoise Simon <>
Submitted on : Thursday, August 13, 2009 - 2:41:54 PM
Last modification on : Wednesday, April 15, 2020 - 9:56:12 AM

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Pierre-Antoine Crassous, Claudia Cardinaletti, Antonio Carrieri, Bruno Bruni, Massimo Di Vaira, et al.. Alpha2-adrenoreceptors profile modulation. 3.1 (R)-(+)-m-nitrobiphenyline, a new efficient and alpha2C-subtype selective agonist.. Journal of Medicinal Chemistry, American Chemical Society, 2007, 50 (16), pp.3964-8. ⟨10.1021/jm061487a⟩. ⟨inserm-00409859⟩

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