Norepinephrine reuptake inhibitor

Norepinephrine reuptake inhibitor
Norepinephrine
Epinephrine

A norepinephrine reuptake inhibitor (NRI, NERI) or adrenergic reuptake inhibitor (ARI), is a type of drug which acts as a reuptake inhibitor for the neurotransmitters norepinephrine (noradrenaline) and epinephrine (adrenaline) by blocking the action of the norepinephrine transporter (NET). This in turn leads to increased extracellular concentrations of norepinephrine and epinephrine and therefore an increase in adrenergic neurotransmission.

Contents

Indications

NRIs may be used in the clinical treatment of attention-deficit hyperactivity disorder (ADHD), narcolepsy, and fatigue or lethargy as stimulants, obesity as anorectics or appetite suppressants for weight loss purposes, as well as mood disorders such as major depressive disorder (MDD) as antidepressants, nasal or sinus congestion as decongestants, nocturnal enuresis or "bedwetting", hypotension and/or orthostatic hypotension as vasopressors, and both as augmentations and to offset some of the side effects of certain other drugs like the selective serotonin reuptake inhibitors (SSRIs) such as sexual dysfunction.

Effects

General

NRIs can induce a wide range of psychological and physiological effects, including the following:

Psychological
Physiological
Miscellaneous

It should be noted, however, that many of these properties are dependent on whether the NRI in question is capable of crossing the blood-brain-barrier (BBB). Those that do not will only produce peripheral effects.

Overdose

At very high doses characterized by overdose, a number of symptoms may come to prominence, as well as hypertensive crisis, including the following:

Psychological
Physiological
Miscellaneous

Abuse

In contrast to dopamine reuptake inhibitors (DRIs) such as cocaine and methylphenidate, NRIs without DRI properties which do not affect dopamine are incapable of inducing significant rewarding effects and are not self-administered in rodents, and as a result, they have a negligible abuse potential in comparison.[1][2]

List of NRIs

Pharmaceutical Drugs
Dietary Supplements
  • Ginkgo biloba [3]
  • Adhyperforin (found in Hypericum perforatum (St. John's Wort))
  • Hyperforin (found in Hypericum perforatum (St. John's Wort))
Street Drugs
Research Chemicals
  • Selective Norepinephrine Reuptake Inhibitors (NRIs)
Potent and selective NET ligands

See also

References

  1. ^ Wee S, Woolverton WL (September 2004). "Evaluation of the reinforcing effects of atomoxetine in monkeys: comparison to methylphenidate and desipramine". Drug and Alcohol Dependence 75 (3): 271–6. doi:10.1016/j.drugalcdep.2004.03.010. PMID 15283948. 
  2. ^ Gasior M, Bergman J, Kallman MJ, Paronis CA (April 2005). "Evaluation of the reinforcing effects of monoamine reuptake inhibitors under a concurrent schedule of food and i.v. drug delivery in rhesus monkeys". Neuropsychopharmacology 30 (4): 758–64. doi:10.1038/sj.npp.1300593. PMID 15526000. 
  3. ^ Fehske, CJ; Leuner, K; Müller, WE (2009). "Ginkgo biloba extract (EGb761) influences monoaminergic neurotransmission via inhibition of NE uptake, but not MAO activity after chronic treatment". Pharmacological research : the official journal of the Italian Pharmacological Society 60 (1): 68–73. doi:10.1016/j.phrs.2009.02.012. PMID 19427589. 
  4. ^ O'Neill, DJ; Adedoyin, A; Alfinito, PD; Bray, JA; Cosmi, S; Deecher, DC; Fensome, A; Harrison, J et al. (2010). "Discovery of novel selective norepinephrine reuptake inhibitors: 4-3-aryl-2,2-dioxido-2,1,3-benzothiadiazol-1(3H)-yl-1-(methylamino)butan-2-ols (WYE-103231)". Journal of medicinal chemistry 53 (11): 4511–21. doi:10.1021/jm100053t. PMID 20462211. 
  5. ^ Fensome, A; Goldberg, J; McComas, CC; Trybulski, EJ; Woodworth, RP; Deecher, DC; Whiteside, GT; Zhang, P (2010). "Structure-activity relationships of norepinephrine reuptake inhibitors with benzothiadiazine dioxide or dihydrosulfostyril cores". Bioorganic & medicinal chemistry letters 20 (5): 1555–8. doi:10.1016/j.bmcl.2010.01.056. PMID 20153188. 
  6. ^ Vu, AT; Cohn, ST; Zhang, P; Kim, CY; Mahaney, PE; Bray, JA; Johnston, GH; Koury, EJ et al. (2010). "1-(Indolin-1-yl)-1-phenyl-3-propan-2-olamines as potent and selective norepinephrine reuptake inhibitors". Journal of medicinal chemistry 53 (5): 2051–62. doi:10.1021/jm901559e. PMID 20131864. 
  7. ^ Zhang, P; Terefenko, EA; Bray, J; Deecher, D; Fensome, A; Harrison, J; Kim, C; Koury, E et al. (2009). "1- or 3-(3-Amino-2-hydroxy-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones: Potent, selective, and orally efficacious norepinephrine reuptake inhibitors". Journal of medicinal chemistry 52 (18): 5703–11. doi:10.1021/jm900888c. PMID 19722525. 
  8. ^ Sabatucci, JP; Mahaney, PE; Leiter, J; Johnston, G; Burroughs, K; Cosmi, S; Zhang, Y; Ho, D et al. (2010). "Heterocyclic cycloalkanol ethylamines as norepinephrine reuptake inhibitors". Bioorganic & medicinal chemistry letters 20 (9): 2809–12. doi:10.1016/j.bmcl.2010.03.059. PMID 20378347. 
v · d · eNeuromodulation
Types
Classes
see Enzyme inhibition
Calcium channel blocker (CCB) • Potassium channel blocker (PCB) • Sodium channel blocker (SCB) • Potassium channel opener (PCO)
Adrenergic receptor agonist (α, β (1, 2)) • Adrenergic receptor antagonist (α (1, 2), β) • Adrenergic reuptake inhibitor (ARI)
Serotonin receptor agonist • Serotonin Receptor Antagonist (5-HT3) • Serotonin reuptake inhibitor (SRI) • Serotonin reuptake enhancer (SRE)
GABA receptor agonist • GABA receptor antagonist • GABA reuptake inhibitor (GRI)
Cannabinoid receptor agonist • Cannabinoid receptor antagonist
Other
Adenosine reuptake inhibitor (AdoRI) • Angiotensin II receptor antagonist • Endothelin receptor antagonist • NK1 receptor antagonist • Vasopressin receptor antagonist
Miscellaneous
Cofactor (see Enzyme cofactors) • Precursor (see Amino acids)

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