| Title : Discovery of non-peptide, small molecule antagonists of alpha9alpha10 nicotinic acetylcholine receptors as novel analgesics for the treatment of neuropathic and tonic inflammatory pain - Zheng_2011_Bioorg.Med.Chem.Lett_21_2476 |
| Author(s) : Zheng G , Zhang Z , Dowell C , Wala E , Dwoskin LP , Holtman JR , McIntosh JM , Crooks PA |
| Ref : Bioorganic & Medicinal Chemistry Lett , 21 :2476 , 2011 |
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Abstract :
A series of azaaromatic quaternary ammonium analogs has been discovered as potent and selective alpha9alpha10 nicotinic acetylcholine receptor (nAChR) antagonists. The preliminary structure-activity relationships of these analogs suggest that increased rigidity in the linker units results in higher potency in inhibition of alpha9alpha10 nAChRs and greater selectivity over alpha7 nAChRs. These analogs represent a new class of analgesic for the treatment of neuropathic and tonic inflammatory pain. |
| PubMedSearch : Zheng_2011_Bioorg.Med.Chem.Lett_21_2476 |
| PubMedID: 21397497 |
Zheng G, Zhang Z, Dowell C, Wala E, Dwoskin LP, Holtman JR, McIntosh JM, Crooks PA (2011)
Discovery of non-peptide, small molecule antagonists of alpha9alpha10 nicotinic acetylcholine receptors as novel analgesics for the treatment of neuropathic and tonic inflammatory pain
Bioorganic & Medicinal Chemistry Lett
21 :2476
Zheng G, Zhang Z, Dowell C, Wala E, Dwoskin LP, Holtman JR, McIntosh JM, Crooks PA (2011)
Bioorganic & Medicinal Chemistry Lett
21 :2476