The effect of a series of organic cations upon the plasmalemmal serotonin transporter, SERT

Keating, Elisa; Lemos, Clara; Monteiro, Rosário; Azevedo, Isabel; Martel, Fátima

doi:10.1016/j.lfs.2004.08.007

Cited by 22 publications

(15 citation statements)

References 55 publications

(52 reference statements)

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“…On platelets of [207] African-American smokers, a decreased paroxetine binding has been found [202]. It is unlikely that this was caused by a direct interaction of nicotine with the SERT, because it only exerts inhibitory effects at concentrations much higher than found in the blood of smokers [301]. Other studies indicate a possible genetic link related to the above mentioned polymorphism in the 5' promoter region of the SERT.…”

Section: Substance Abusementioning

confidence: 99%

Neuroimaging of the Serotonin Transporter: Possibilities and Pitfalls

Brust¹,

Hesse²,

Müller³

et al. 2006

CPSR

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Nuclear medicine imaging techniques like positron emission tomography (PET) and single-photon emission computed tomography (SPECT) apply radiolabeled drugs that bind selectively to specific neurotransmitter receptors and transporters such as the serotonin transporter (SERT) in the living human brain. They can help overcome certain limitations of postmortem, platelet and genetic studies of the SERT. This review compares the outcome of those studies with recent neuroimaging findings. The first part of this review deals with the choice of radioligands used to quantify SERT distribution in the human brain. The second part summarizes studies performed to understand the normal physiology of the serotonergic system. Selective serotonin reuptake inhibitors (SSRIs), used to treat a wide range of neuropsychiatric disorders with emotional instability and behavioral control deficits, compete with SERT radioligands and have been investigated in pharmacological PET and SPECT studies in healthy volunteers and patients. Part three reviews SERT imaging studies in patients, which have meanwhile been performed in most disorders that benefit from SSRI treatment. It is hypothesized that serotonin deficits and neuropsychiatric symptoms are linked by the inhibition of involuntary emotional reactions to external and internal stimuli. This could explain, why the consistency of many SERT neuroimaging findings is low, and may help develop individual treatment strategies in therapy-nonresponsive cases and to engineer new drugs for the therapy of neuropsychiatric disorders.

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Section: Substance Abusementioning

confidence: 99%

Neuroimaging of the Serotonin Transporter: Possibilities and Pitfalls

Brust¹,

Hesse²,

Müller³

et al. 2006

CPSR

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show abstract

“…Compounds such as N-butylscopolamine, isobutyl-methyl-xanthine, nicotinamide, L-phenylalanine, L-tyrosine, tyramine, dopamine, noradrenaline, L-tryptophan, L-histidine, metformine, and Clonidine uptake was also not affected by agmatine and serotonin. Intestinal transport that is inhibited by clonidine has been reported for both drugs, (19,20). Because clonidine affects many transport systems for organic solutes or inorganic ions directly or indirectly, inhibition of such transporters by clonidine does not at all allow the conclusion of substrate inhibition.…”

mentioning

confidence: 99%

Substrate Specificity and Mechanism of the Intestinal Clonidine Uptake by Caco-2 Cells

et al. 2006

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Clonidine is transported by a carrier-mediated process. Substrate specificity and mechanism are very similar to the transport described in blood-brain barrier endothelial cells. The transport characteristics do not correspond to carriers for organic cations of the SLC22 family or the choline transporters CHT1 and CLT1. The system might be identical to the H+/tertiary amine antiporter. It interacts with a large number of both hydrophilic and lipophilic cationic drugs, and also, interestingly, with opiates.

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“…In addition, thiamine (1-3000 µM) reduced 3 H-5-HT uptake to 83% of the controls in human placental choriocarcinoma cells. These cells are the only cell line of human origin expressed in the 5-HT transporter [70]. Lurcher mutant mice are characterized by considerable atrophy in the cerebellum, which is secondary to a massive loss of cerebellar Purkinje cells, granule cells, and neurons from the inferior olivary nucleus; a therapeutic combination of amantadine, thiamine, and L-tryptophan increased SERT densities to 98% in Lurcher mutant mice, which is higher than those of wild-type mice [71].…”

Section: Neurotransmitter Systemmentioning

confidence: 99%

The Role of Thiamine in Autism

Lương¹

2013

AJPN

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Autism spectrum disorders are a group of neuro-developmental conditions characterized by varying degrees of language impairment, including verbal and non-verbal communication, impaired social skill, and repetitive behaviors. In this paper, we review the evidence for an association between autism and thiamine. A relationship between thiamine status and the development of autism has been established, with thiamine supplementation exhibiting a beneficial clinical effect on children with autism. Thiamine may involve in autism via apoptotic factors (transcription factor p53, Bcl-2, and caspase-3), neurotransmitter systems (serotonin, acetylcholine, and glutamate), and oxidative stress (prostaglandins, cyclooxygenase-2, reactive oxygen species, nitric oxide synthase, the reduced form of nicotinamide adenine dinucleotide phosphate, and mitochondrial dysfunction). In addition, thiamine has also been implicated in autism via its effects on basic myelin protein, glycogen synthetase kinase-3β, alpha-1 antitrypsin, and glyoxalase 1. Thiamine may play a role in children with autism. Additional investigation of thiamine in children with autism is needed.

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The effect of a series of organic cations upon the plasmalemmal serotonin transporter, SERT

Cited by 22 publications

References 55 publications

Neuroimaging of the Serotonin Transporter: Possibilities and Pitfalls

Neuroimaging of the Serotonin Transporter: Possibilities and Pitfalls

Substrate Specificity and Mechanism of the Intestinal Clonidine Uptake by Caco-2 Cells

The Role of Thiamine in Autism

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