Monoamine uptake inhibitors

Transporters for dopamine (DAT), serotonin (SERT) and norepinephrine (NET) are the initial targets for psychomotor stimulants. By interacting with these transporters (Chs 12 and 13), psychomotor stimulants increase extracellular levels of monoamine neurotransmitters. Cocaine is a monoamine uptake inhibitor. The reinforcing effects of cocaine correlate best with its binding potency at the DAT. However, experiments with monoamine transporter-deficient mice suggest that cocaine actions at... 

Hilakivi LA, Taira T, Hilakivi I, Loikas P. Neonatal treatment with monoamine uptake inhibitors alters later response in behavioural despair test to beta and GABA-B receptor agonists. Pharm Toxicol 1988 63 57-61. 

Assignee The Trustees of The University of Pennsylvania Utility Preparation of Monoamine Uptake Inhibitors and Radiolabeled... 

DB 2182 Leo 640) is one of the tricyclic class of monoamine UPTAKE INHIBITORS. It has been used as an ANTIDEPRESSANT, lofexidine [ban, inn] is an imidazoline with properties similar to clonidine. It is an (oj) a-ADRENOCEPTOR AGONIST that can be used as an antihypertensive. It can also be used to alleviate opioid withdrawal symptoms. The (R)- om is a more active isomer. 

Protopam chloride" pralidoxime. protriptyline [ban. inn] (protriptyline hydrochloride [usan] Concordin Vivactil" ) is one of the tricyclic class of monoamine uptake inhibitors, and is used as an oral ANTIDEPRESSANT. 

ICI 58834) is an oxazine chemically distinct from the tricyclics and tetracyclics monoamine uptake inhibitors, and has been used as an oral ANTIDEPRESSANT, viloxazine hydrochloride viloxazine, viminol [inn] is a pyrrole, and is a nsaid analgesic and... 

Ortiz J, Artigas F. Effects of monoamine uptake inhibitors on extracellular and platelet 5-hydroxytryptamine in rat blood different effects of clomipramine and fluoxetine. Br J Pharmacol 1992 105 941-6. 

Marek, G.J. Vosmer, G. and Seiden, L.S. The effects of monoamine uptake inhibitors and methamphetamine on neostriatal 6-hydroxy-dopamine (6-OHDA) formation, short-term monoamine depletions and locomotor activity in the rat. Brain Res 516 1-7, 19906. 

The hypothesis that serotonin dysfunction may play an important role in depression and the fact that tricyclic antidepressants are monoamine uptake inhibitors but also have a considerable affinity as antagonists for cholinergic, histaminergic and adrenergic receptors and thus may cause unwanted severe side-effects initiated the search for and development of selective serotonin uptake inhibitors. 

Fluvoxamine and clovoxamine are nontricyclic monoamine uptake inhibitors structurally related to the tricyclic smtidepressant noxiptiline (fig. 3). Both fluvoxamine and dovoxamine are trans isomers. Clovoxamine is a potent but nonselective inhibitor of the 5-HT and NE transporter in a synaptosomal preparation of the rat brain frontal cortex (Kj=5.9 and 7.0 nM respectively) and a weak (KjS 720 nM) inhibitor of the DA transporter in synaptosomes of the corpus striatum [26]. 

Recently Cheetham et al. [66] extended the series and investigated a wide range of monoamine uptake inhibitors. Again a very good and highly significant correlation (r=0.946, p<0.001) was found between the potencies in inhibition of H-paroxetine binding and inhibition of 5-HT uptake in synaptosomal preparations of rat fi ontal cortex. 

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