a(MESH:"5-(2-azetidinylmethoxy)-2-chloropyridine") increases act(p(HBP:"alpha-4 beta-2 nAChR"))

PubMed:19721446

The first nicotinic receptor ligand to undergo Phase ii clinical trials for analgesic activity was the potent Abbott compound ABT-594, a nAChR agonist that preferentially targets α4β2 (ReFS 231–235). The compound allowed for the clinical proof of concept, but could not be developed further because of adverse effects such as emesis and nausea236. As these adverse effects seemed to be attributable to the activation of the ganglionic α3β4 nAChR receptors, Abbott undertook a search for more selective α4β2 agonists, independently and in cooperation with Neurosearch.

Related Edges 5

• a(MESH:"5-(2-azetidinylmethoxy)-2-chloropyridine") association path(MESH:Vomiting)
• a(MESH:"5-(2-azetidinylmethoxy)-2-chloropyridine") association path(MESH:Nausea)
• a(MESH:"5-(2-azetidinylmethoxy)-2-chloropyridine") increases act(complex(p(HGNC:CHRNA3), p(HGNC:CHRNB4)))
• path(MESH:Nausea) association a(MESH:"5-(2-azetidinylmethoxy)-2-chloropyridine")
• path(MESH:Vomiting) association a(MESH:"5-(2-azetidinylmethoxy)-2-chloropyridine")

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