[HTML][HTML] The antidepressant desipramine is an arrestin-biased ligand at the α2A-adrenergic receptor driving receptor down-regulation in vitro and in vivo
C Cottingham, Y Chen, K Jiao, Q Wang - Journal of Biological Chemistry, 2011 - ASBMB
The neurobiological mechanisms of action underlying antidepressant drugs remain poorly
understood. Desipramine (DMI) is an antidepressant classically characterized as an inhibitor
of norepinephrine reuptake. Available evidence, however, suggests a mechanism more
complex than simple reuptake inhibition. In the present study, we have characterized the
direct interaction between DMI and the α 2A-adrenergic receptor (α 2A AR), a key regulator
of noradrenergic neurotransmission with altered expression and function in depression. DMI …
understood. Desipramine (DMI) is an antidepressant classically characterized as an inhibitor
of norepinephrine reuptake. Available evidence, however, suggests a mechanism more
complex than simple reuptake inhibition. In the present study, we have characterized the
direct interaction between DMI and the α 2A-adrenergic receptor (α 2A AR), a key regulator
of noradrenergic neurotransmission with altered expression and function in depression. DMI …