Centre National De La Recherche Scientifique

Université Paris Descartes

Université D'auvergne

Cyril Goudet

Jean-Philippe Pin

Francine Acher

Alain Eschalier

Jérôme Busserolles

Bruno Commare

Florence Gaven

Delphine Rigault

Laurent Prezeau

Isabelle Lemasson

Sara Cesarini

The invention relates to hypophosphorous acid derivatives of formula (I) wherein &#x2014;X is H or OH, &#x2014;R represents one or several radicals R-R, identical or different, two of R-Roptionally occupying the same position on the phenyl group, one to four of R-Rbeing H and the others being selected in the group comprising -0-(CH)&#x2014;COOH; &#x2014;S&#x2014;(CH)&#x2014;COOH; &#x2014;NH&#x2014;(CH)&#x2014;COOH; -0-(CH,R')&#x2014;COOH; &#x2014;O&#x2014;(CH)&#x2014;OH; OR&#x2032;, &#x2014;R&#x2032; being a C-Calkyl radical; &#x2014;OH; &#x2014;COOH; halogen, particularly &#x2014;F, &#x2014;CI, &#x2014;Br, &#x2014;I, &#x2014;CF; &#x2014;OCF; &#x2014;N0; &#x2014;CH&#x2550;CH&#x2014;COOH; &#x2014;(CH)&#x2014;COOH; O&#x2014;(CH)&#x2014;P0H; O&#x2014;(CF)&#x2014;P0H; O&#x2014;(CH)&#x2014;S0H; O&#x2014;(CH)&#x2014;CONHOH; O&#x2014;(CH)-tetrazol; O&#x2014;(CH)-hydroxyisoxazol&#x2014;n=1 to 5, preferably 1-3; said hypophosrous acid derivatives being diastereoisomers or enantiomers. 

Hypophosphorous acid derivatives having antihyperalgic activity and biological applications thereof

A method for identifying and selecting a compound acting as an allosteric regulator of a GPCR-III is described. A method comparing the activity level of a recombinant GPCR-III (GPCR-III-&#x394;), essentially depleted of the extracellular domain of the corresponding native GPCR-III, in the presence of a given compound, with the activity level of the same GPCR-III-&#x394; is described. A method of identifying positive or negative allosteric regulators of GPCRs-III is described.

Method for selecting allosteric regulators of class III G protein-coupled receptors

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Cyril Goudet