The wide variety of drugs in development includes opioid receptor ligands, bradykinin antagonists, mPGES-1 inhibitors, glutamate receptor antagonists, substance P and neurokinin receptor antagonists, norepinephrine transporter
inhibitors,P2X2 neuron receptor antagonists and nitric oxide-based analgesics.
31-35) One potential mechanism involves changes in the norepinephrine transporter
In particular, variations in the gene encoding the norepinephrine transporter
seemed to predispose adolescents toward impulsivity.
In patients with cardiac failure, for example, increased spillover of norepinephrine from the heart into coronary sinus plasma was shown to reflect both increased exocytotic release and decreased efficiency of norepinephrine reuptake via the norepinephrine transporter
dependent and was not observed in the presence of imipramine or desipramine, serotonin (SERT) and norepinephrine transporter
(NET) blockers, indicating it was specific for uptake blocker binding.
Biochemical profiling of AR-13324 has revealed inhibitory activity against Rho kinase (ROCK) and the norepinephrine transporter
Dopamine uptake through the norepinephrine transporter
in brain regions with low levels of the dopamine transporter: evidence from knock-out mouse lines.
It is a strong dopamine-2 and serotonin-2A receptor antagonist, a potent inhibitor of the norepinephrine transporter
, and a moderate antagonist at the serotonin-1A receptor.
They conducted a study to determine whether SSRI efficacy is linked to polymorphisms in the serotonin transporter gene (5-HTT) and whether the efficacy of norepinephrine reuptake inhibitors is linked to polymorphisms in the norepinephrine transporter
A nonstimulant and potent inhibitor of the presynaptic norepinephrine transporter
, atomoxetine improved the symptoms of ADHD for 178 patients as effectively as methylphenidate did for 40 patients in a randomized, open-label study (J.
The drug, which also is being studied in adults with ADHD, is a potent inhibitor of the presynaptic norepinephrine transporter
, "with minimal affinity for other noradrenergic receptors or other neurotransmitter transporters or receptors," according to Lilly.
Tracer kinetic modeling of [18F]LMI1195, a new PET imaging agent targeting cardiac norepinephrine transporter
," Ajay V.