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Laboratoires Debat

Subsidiary Company|France

Last update 08 May 2025

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Translational Medicine

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100 Clinical Results associated with Laboratoires Debat

0 Patents (Medical) associated with Laboratoires Debat

Literatures (Medical) associated with Laboratoires Debat

01 Mar 1991·Biochemical PharmacologyQ2 · MEDICINE

Non-adrenergic binding sites for the “α2-antagonist” [3h]idazoxan in the rabbit urethral smooth muscle pharmacological and biochemical characterization

Q2 · MEDICINE

Article

Author: Dausse, J. P. ; Yablonsky, F.

In the present study, pharmacological and biochemical binding characteristics of [3H]idazoxan, an originally thought alpha 2-adrenoceptor antagonist, have been determined in smooth muscle of rabbit urethra. It is shown that [3H]idazoxan labels with high affinity non-adrenergic binding sites. Specific binding of [3H]idazoxan is inhibited by compounds possessing an imidazoline or a guanidinium moiety whereas phenylethanolamines and classical alpha 2-antagonists are ineffective competitors which suggests an imidazoline-preferring binding site. However, imidazolidines such as clonidine and paminoclonidine are poorly effective, which differs considerably from pharmacological characteristics of imidazoline binding sites previously reported in the central nervous system. In addition, it is shown that K+ and Mn2+ inhibit [3H]idazoxan binding in a competitive and non-competitive manner, respectively. Other cations such as Na+, Li+ and Mg2+ have no significant effect. It is shown that K+ accelerates the dissociation of [3H]idazoxan binding while Mn2+ does not produce any modification. These results suggest that K+ may bind to an allosteric site, while Mn2+ may bind with a membrane component susceptible to alter [3H]idazoxan binding sites.

01 Jan 1991·Journal of Receptor Research

Non-Adrenergic Binding Sites for the “α-Antagonist” [³H] Idazoxan in Rabbit Urethral Smooth Muscle

Article

Author: Lacolle, J. Y. ; Yablonsky, F. ; Dausse, J. P.

In the present study, we have provided evidence that [3H] rauwolscine and [3H] idazoxan bind to different sites in rabbit urethra. The [3H] idazoxan capacity and affinity was 215 +/- 14 fmol/mg protein and 1.59 +/- 0.16 nM while [3H] rauwolscine binding parameters were 45.9 +/- 3.4 fmol/mg protein and 2.39 +/- 0.27 nM. [3H] idazoxan specific binding was inhibited only by compounds possessing an imidazoli(di)ne or a guanidinium moiety, while [3H] rauwolscine specific binding was inhibited by phenylethanolamines and classical alpha 2-antagonists. [3H] idazoxan was inhibited by KCl in a competitive and by MnCl2 in a non-competitive way, while other cations such as Na+, Li+ and Mg2+ did not inhibit [3H] idazoxan binding. Moreover, we investigated the regional distribution of [3H] idazoxan and [3H] rauwolscine along the rabbit urethra using quantitative autoradiography. Analysis of the films revealed a different distribution of these two binding sites on the urethral sections.

01 Jan 1991·Neurourology and Urodynamics

Autoradiographic localization of α₁‐adrenoceptors in the dog prostate and urethra with ³H‐prazosin

Author: Feuerstein, C. ; Yablonsky, F. ; Manier, M. ; Savasta, M. ; Lacolle, J. Y. ; Poirier, M.

AbstractThe regional distribution of α1‐adrenoceptors in the dog urethra has been studied by quantitative autoradiography using the specific α1‐antagonist 3H‐prazosin as a ligand. The binding of 3H‐prazosin to urethral tissue sections was saturable, reversible, and of high affinity (Kd = 0.7 nM); it occurred at a single population of sites and possessed the pharmacological features of the α1‐adrenoceptor. The binding parameters of 3H‐prazosin on urethral tissue sections were found similar to those obtained on urethral membranes. Autoradiographic results revealed that the α1‐adrenoceptors are heterogeneously distributed along the dog urethral axis. The highest densities of 3H‐prazosin binding sites were found in the preprostatic urethra. Comparison between autoradiographic and histological slides revealed that the 3H‐prazosin binding sites were only localized on the smooth muscle fibres of the dog urethra.

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100 Translational Medicine associated with Laboratoires Debat

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