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Effects of chloro, methoxy and trifluoromethyl substituents in the aromatic ring of cycloalkanol ethylamine scaffold were tested. The results showed that the strongest electron-withdrawing m-trifluoromethyl analogue exhibited the most potent inhibitory effect of norepinephrine and the most selectivity over serotonin uptake. [36]
Norepinephrine Epinephrine. A norepinephrine reuptake inhibitor (NRI, NERI) or noradrenaline reuptake inhibitor or adrenergic reuptake inhibitor (ARI), is a type of drug that acts as a reuptake inhibitor for the neurotransmitters norepinephrine (noradrenaline) and epinephrine (adrenaline) by blocking the action of the norepinephrine transporter (NET).
The general function of norepinephrine is to mobilize the brain and body for action. Norepinephrine release is lowest during sleep, rises during wakefulness, and reaches much higher levels during situations of stress or danger, in the so-called fight-or-flight response. In the brain, norepinephrine increases arousal and alertness, promotes ...
The connection was made shortly after the discovery of catecholamines having effects on emotion, relating to depression, and was of wide interest. Discovery was made on the decreased levels of certain neurotransmitters, catecholamines such as norepinephrine, dopamine and serotonin, and their role in the pathogenesis of depression. [28]
In men, the side effects of antidepressants result in reduced drive (low libido) or lowered desire, delayed climax, and difficulties with developing and maintaining arousal.
Desipramine, sold under the brand name Norpramin among others, is a tricyclic antidepressant (TCA) used in the treatment of depression. [8] It acts as a relatively selective norepinephrine reuptake inhibitor, though it does also have other activities such as weak serotonin reuptake inhibitory, α 1-blocking, antihistamine, and anticholinergic effects.
3-Methoxy-4-hydroxyphenylglycol (MHPG, MOPEG) is a metabolite of norepinephrine degradation.In the brain, it is the principal norepinephrine metabolite. It is released into the blood and cerebrospinal fluid, [1] and a blood sample of it may therefore be an indication of recent sympathetic nervous system activity.
The majority of TCAs exert greater effect on norepinephrine, which leads to side effects like drowsiness and memory loss. [ citation needed ] In order to be more effective on serotonin agonism and avoid anticholinergic and antihistaminergic side effects, selective serotonin reuptake inhibitors (SSRI) were researched and introduced to treat ...