Fluorescent reporters of monoamine transporter distribution and function

Bagale, Sharanappa M.; Brown, Adrienne S.; Gonzalez, Melissa M. Carballosa; Vitores, Alberto; Micotto, Teresa L.; Kumar, N. S. Saleesh; Hentall, Ian D.; Wilson, James N.

doi:10.1016/j.bmcl.2011.10.007

Cited by 6 publications

(6 citation statements)

References 23 publications

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“…This can be interpreted in three ways: 1) that TPH2 knockout is not complete, but there is little other evidence to suggest this is true; 2) there is another source for 5-HT synthesis (such as TPH1 or phenylalanine hydroxylase) that is revealed upon removal of the primary 5-HT synthetic source in the CNS (TPH2); and 3) it is possible that the 5-HT detected in the brain of the TPH2(Ϫ/Ϫ) mouse is made by TPH1 (located in the periphery), and this 5-HT moves from the periphery to the brain. Bagale et al (2011) reported the use of ethylamine-functionalized fluorophores that can be used to visualize SERT in living tissues. Thus, it remains possible that systemic 5-HT could have effects on blood pressure by binding to 5-HT receptors on CNS neurons, and we have tools to test this idea.…”

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confidence: 99%

Serotonin and Blood Pressure Regulation

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confidence: 99%

Serotonin and Blood Pressure Regulation

et al. 2012

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“…Based on physical and photophysical properties of all final compounds, compound 5 (Figure 4C) was suitable for cellular and in vivo studies and showed accumulation in an MLO‐Y4 (Murine osteocyte) cell line expressing SERT. In the presence of clomipramine, uptake of this FLL was significantly reduced 52 …”

Section: Matsmentioning

confidence: 98%

“…In the presence of clomipramine, uptake of this FLL was significantly reduced. 52 We previously described ASP + (4-(4-(dimethylamino)-styryl)-N-methylpyridinium) (Figure 2A) as a substrate for DAT, although its ability to be transported by SERT is not as efficient. Therefore, Solis et al 54 characterized a series of fluorescent analogues.…”

Section: Sertmentioning

confidence: 99%

“…In a similar approach, the same group reported the synthesis of ethylamine-functionalized fluorescent probes by using naphthalene, anthracene, pyrene and phenothiazine as the fluorophore cores. 52 Based on physical and photophysical properties of all final compounds, compound 5 (Figure 4C) was suitable for cellular and in vivo studies and showed accumulation in an MLO-Y4 (Murine osteocyte) cell line expressing SERT. In the presence of clomipramine, uptake of this FLL was significantly reduced.…”

Section: Sertmentioning

confidence: 99%

“…(A) Compound 1 in Micotto et al 51 ; (B) compound 4, Micotto et al 51 ; (C) compound 5 in Bagale et al 52 ; (D) APP + ; (E) (±)Citalopram; (F) ZP 455 (compound 8 in Zhang et al 53 ); (G) VK2‐83 (compound 14 in Kumar et al 25 )…”

Section: Matsmentioning

confidence: 99%

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Illuminating the monoamine transporters: Fluorescently labelled ligands to study dopamine, serotonin and norepinephrine transporters

Camacho‐Hernandez

Jahan

Newman

2023

Basic Clin Pharma Tox

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Fluorescence microscopy has revolutionized the visualization of physiological processes in live‐cell systems. With the recent innovations in super resolution microscopy, these events can be examined with high precision and accuracy. The development of fluorescently labelled small molecules has provided a significant advance in understanding the physiological relevance of targeted proteins that can now be visualized at the cellular level. One set of physiologically important target proteins are the monoamine transporters (MATs) that play an instrumental role in maintaining monoamine signalling homeostasis. Understanding the mechanisms underlying their regulation and dysregulation is fundamental to treating several neuropsychiatric conditions such as attention deficit hyperactivity disorder (ADHD), anxiety, depression and substance use disorders. Herein, we describe the rationale behind the small molecule design of fluorescently labelled ligands (FLL) either as MAT substrates or inhibitors as well as their applications to advance our understanding of this class of transporters in health and disease.

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Inherited Disorders of Brain Neurotransmitters: Pathogenesis and Diagnostic Approach

Sztefko

Kuśmierska

Demkow

2014

Neurotransmitter Interactions and Cognitive Function

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Neurotransmitters (NTs) play a central role in the efficient communication between neurons necessary for normal functioning of the nervous system. NTs can be divided into two groups: small molecule NTs and larger neuropeptide NTs. Inherited disorders of NTs result from a primary disturbance of NTs metabolism or transport. This group of disorders requires sophisticated diagnostic procedures. In this review we discuss disturbances in the metabolism of tetrahydrobiopterin, biogenic amines, γ-aminobutyric acid, foliate, pyridoxine-dependent enzymes, and also the glycine-dependent encephalopathy. We point to pathologic alterations of proteins involved in synaptic neurotransmission that may cause neurological and psychiatric symptoms. We postulate that synaptic receptors and transporter proteins for neurotransmitters should be investigated in unresolved cases. Patients with inherited neurotransmitters disorders present various clinical presentations such as mental retardation, refractory seizures, pyramidal and extrapyramidal syndromes, impaired locomotor patterns, and progressive encephalopathy. Every patient with suspected inherited neurotransmitter disorder should undergo a structured interview and a careful examination including neurological, biochemical, and imaging.

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Fluorescent reporters of monoamine transporter distribution and function

Cited by 6 publications

References 23 publications

Serotonin and Blood Pressure Regulation

Serotonin and Blood Pressure Regulation

Illuminating the monoamine transporters: Fluorescently labelled ligands to study dopamine, serotonin and norepinephrine transporters

Inherited Disorders of Brain Neurotransmitters: Pathogenesis and Diagnostic Approach

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