Use Of A Compound Modulating At Least One Receiver Selected In A Group Comprising An Interleukin 8 Type B Receptor And Pacap-1 Receptor For Porparing A Pharmaceutical Composition For Rosacea Treatment

Abstract

The invention relates to the use of a modulator of at least one receptor chosen from the group comprising the IL-8RB receptor and the PAC-1 receptor for the preparation of a pharmaceutical composition for treating rosacea.

Description

EXAMPLE 1

Measurement of the Binding to the IL-8RB and PAC-1 Receptors

1) Protocol:

The test of binding to the PAC-1 receptor was performed according to the protocol described by Cauvin et al., 1991, Regul Peptides, vol. 35, pages 161-173.

The test of binding to the IL-8RB receptor was performed according to the protocol described by White et al., 1998, J Biol Chem, vol. 273, pages 10095-10098.

2) Experimental Conditions:

The binding of metronidazole to each receptor was determined by competitive experiments. The receptor, human recombinant protein, was incubated for times indicated in Table 1 below, with a simple concentration of radiolabelled specific ligand, in the presence of 10 μM metronidazole. The bound radioactivity was measured by scintillation counting.

TABLE 1
	Radiolabelled		Incubation
Receptor	specific ligand	Non-specific ligand	conditions
IL-8RB	[125I]IL-8	IL-8(0.3 μM)	60 min/22° C.
	(0.2 nM)
OAC-1	[125I]PACAP1-27	PACAP1-27	30 min/37° C.
	(0.2 nM)	(0.1 μM)

3) Analysis and Expression of the Results:

The specific binding of the ligand to the receptor is defined as the difference between the total binding and the non-specific binding determined in the presence of an excess of unlabelled ligand.

The results are expressed in Table 2 below as a percentage of control specific binding and as a percentage of inhibition of the control specific binding obtained in the presence of metronidazole.

	TABLE 2
			% of control specific
	Receptor	Metronidazole (μM)	binding (±SD)
	IL-8RB	10	120.8 +/− 0.7
	PAC-1	10	133.2 +/− 13.2

Metronidazole thus induces the binding of the ligand to its IL-8RB receptor and to the PCA-1 receptor.

Claims

1: A pharmaceutical composition for treating rosacea, comprising a rosacea treating effective amount of a compound that increases the binding of at least one natural ligand to a receptor chosen from the group comprising the IL-8RB receptor and the PAC-1 receptor, with the proviso that the compound is not metronidazole.

2: The composition according to claim 1, wherein said compound increases the binding of a natural ligand to the IL-8RB receptor and of a natural ligand to the PAC-1 receptor.

3: The composition according to claim 1, wherein said pharmaceutical composition is a dermatological composition for topical application.

4: The composition according to claim 1, wherein the composition is for treating at least one stage of rosacea.

5: The composition according to claim 1, wherein the composition is for treating the first stage of rosacea.

6: The composition according to claim 1, wherein the composition is for treating the second stage of rosacea.

7: The composition according to claim 1, wherein the composition is for treating the third stage of rosacea.

8: The composition according to claim 1, wherein the composition is for treating the fourth stage of rosacea.

9: The composition according to claim 1, wherein the composition contains from about 0.0001% to 20% of said modulator.

10: The composition according to claim 1, wherein said composition further comprises another active agent chosen from the group of antibiotics, antibacterial agents, antiviral agents, antiparasitic agents, antifungal agents, anaesthetics, analgesics, antiallergic agents, retinoids, free-radical scavengers, anti-pruriginous agents, kerato-lytic agents, anti-seborrhoeic agents, antihistamines, sulfides, immunosuppressant products and anti-proliferative products.

11: The composition according to claim 1, wherein the composition further comprises an additive chosen from the group of sequestrants, antioxidants, sunscreens, preserving agents, fillers, electrolytes, humectants, dyes, common mineral or organic acids or bases, fragrances, essential oils, cosmetic active agents, moisturizers, vitamins, essential fatty acids, sphingolipids, self-tanning compounds, calmatives and skin-protecting agents, pro-penetrating agents and gelling agents, or a mixture thereof.

12: The composition according to claim 9, wherein the composition contains from 0.1% to 2% by weight of said modulator.

13: The composition according to claim 12, wherein the composition contains from about 0.75% to 1% by weight of said modulator.