Compositions comprising a ligand of a neuronal nicotinic acetylcholine receptor and an allosteric Modulator of alpha4 beta2

摘要

1.- A composition, comprising: (i) a nicotinic acetylcholine receptor ligand and (ii) a positive allosteric modulator of the nicotinic acetylcholine receptor subtype a4ß2 mixed with at least one pharmaceutically acceptable excipient. 2. The composition of claim 1, wherein the nicotinic acetylcholine receptor ligand is a nicotinic acetylcholine receptor ligand subtype a4ß2 having a Ki value measured by the [3H] -cytisine binding assay (Ki Cyt) between about 0.001 nanomolar and about 100 micromolar. 3. The composition of claim 1,Among them, the ligation of acetylcholine receptor is part of pain or pain to acetylcholine receptor in subtropical zone. 4. - composition required in Item 1, wherein the binding of acetylcholine receptor is a derivative of isocyclic ether, an N-substituted p-phenylene derivative, or an isocyclic substituted aminobenzene compound. 5. - component required in Item 1, the binding of acetylcholine receptor is a compound selected from 5 - [(2R) - azerbaijan-2-ilmerhy] - 2-chloropyridine,(3R) -1-pyridin-3-ylpyrrolidin-3-amine and 2-methyl-3- (2- (S) -pyrrolidinylmethoxy) pyridine; 3- (5,6-dichloro-pyridin-3-yl) -1 (S), 5 (S) -3,6-diazabicyclo [3.2.0] heptane; and (R, R) -1- (pyridin-3-yl) octahydro-pyrrole [3,4.b] pyrrole; or is it a pharmaceutically acceptable salt thereof. 6. The composition of claim 1, wherein the nicotinic acetylcholine receptor ligand is selected from aryl-fused azapolycyclic compounds, aryl-substituted olefinic amine compounds, pyridopyranoazepine derivatives, benzylidene- and cinnamylidene-anabasein compounds and Heterocyclic 3-pyridoxylalkyl ether.