PET and SPECT exploration of central monoaminergic transporters for the development of new drugs and treatments in brain disorders : Capabilities of PET and SPECT in pre-clinical and clinical research
Identifieur interne : 003130 ( Main/Merge ); précédent : 003129; suivant : 003131PET and SPECT exploration of central monoaminergic transporters for the development of new drugs and treatments in brain disorders : Capabilities of PET and SPECT in pre-clinical and clinical research
Auteurs : D. Guilloteau [France] ; S. Chalon [France]Source :
- Current pharmaceutical design [ 1381-6128 ] ; 2005.
Descripteurs français
- Pascal (Inist)
- Physiopathologie, Tomoscintigraphie émission monophotonique, Tomographie émission positon, Médicament, Protéine transport, Recherche développement, Chimiothérapie, Toxicité, Trouble attention, Hyperactivité, Autisme, Etat dépressif, Dépression, Dopamine, Parkinson maladie, Site action, Mécanisme action, Traitement, Trouble de l'attention avec hyperactivité, Imagerie moléculaire, Transporteur sérotonine.
- Wicri :
- topic : Médicament.
English descriptors
- KwdEn :
- Attention disorder with hyperactivity, Attentional disorder, Autism, Carrier protein, Chemotherapy, Depression, Depressions, Dopamine, Drug, Hyperactivity, Mechanism of action, Molecular imaging, Parkinson disease, Pathophysiology, Positron emission tomography, Research and development, Serotonin transporter, Single photon emission tomography, Site of action, Toxicity, Treatment.
Abstract
Membrane and vesicular monoaminergic transporters, responsible for the homeostasis of neurotransmitter pools at nerve endings, are very involved in the physiology and diseases of central nervous system. Recent progresses of cerebral molecular imaging using SPECT and PET methods allow the extend of in vivo exploration of these transporters. For this aim, an increasing number of radiopharmaceuticals labelled with [123I], [99mTc], [11C] or [18F] have been developed such as cocaine derivatives for the DAT, compounds from the diphenyl sulfide family for the SERT, and dihydrotetrabenazine derivatives for the VMAT2. These functional imaging methods can be very useful in several neurological and psychiatric disorders which involve the monoaminergic neurotransmission systems such as Parkinson's disease, ADHD, depression and autism. For example, the DAT is a specific index of the density of dopaminergic endings which progressively degenerate in Parkinson's disease. In vivo exploration of this transporter can therefore be a relevant way (i) to realize an early detection of the loss of dopaminergic neurons, (ii) to assess the progression of the disease, (iii) to validate and improve the efficacy of new therapeutic strategies such as neuroprotection and neuroreparation. In all, the extend of in vivo exploration of monoamine transporters will allow great progress for (1) knowledge of physiopathological mechanisms of brain disorders, (2) early diagnosis of cerebral dysfunctions, allowing early use of new therapies, (3) selection of homogenous classes of subjects for therapeutic assays, (4) objectiveness of drug-molecular target interaction, (5) follow-up of disease evolution and treatment.
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Pascal:05-0423247Le document en format XML
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<term>Depression</term>
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<term>Pathophysiology</term>
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<term>Research and development</term>
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<term>Site of action</term>
<term>Toxicity</term>
<term>Treatment</term>
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<term>Tomoscintigraphie émission monophotonique</term>
<term>Tomographie émission positon</term>
<term>Médicament</term>
<term>Protéine transport</term>
<term>Recherche développement</term>
<term>Chimiothérapie</term>
<term>Toxicité</term>
<term>Trouble attention</term>
<term>Hyperactivité</term>
<term>Autisme</term>
<term>Etat dépressif</term>
<term>Dépression</term>
<term>Dopamine</term>
<term>Parkinson maladie</term>
<term>Site action</term>
<term>Mécanisme action</term>
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<front><div type="abstract" xml:lang="en">Membrane and vesicular monoaminergic transporters, responsible for the homeostasis of neurotransmitter pools at nerve endings, are very involved in the physiology and diseases of central nervous system. Recent progresses of cerebral molecular imaging using SPECT and PET methods allow the extend of in vivo exploration of these transporters. For this aim, an increasing number of radiopharmaceuticals labelled with [<sup>123</sup>
I], [<sup>99m</sup>
Tc], [<sup>11</sup>
C] or [<sup>18</sup>
F] have been developed such as cocaine derivatives for the DAT, compounds from the diphenyl sulfide family for the SERT, and dihydrotetrabenazine derivatives for the VMAT<sub>2</sub>
. These functional imaging methods can be very useful in several neurological and psychiatric disorders which involve the monoaminergic neurotransmission systems such as Parkinson's disease, ADHD, depression and autism. For example, the DAT is a specific index of the density of dopaminergic endings which progressively degenerate in Parkinson's disease. In vivo exploration of this transporter can therefore be a relevant way (i) to realize an early detection of the loss of dopaminergic neurons, (ii) to assess the progression of the disease, (iii) to validate and improve the efficacy of new therapeutic strategies such as neuroprotection and neuroreparation. In all, the extend of in vivo exploration of monoamine transporters will allow great progress for (1) knowledge of physiopathological mechanisms of brain disorders, (2) early diagnosis of cerebral dysfunctions, allowing early use of new therapies, (3) selection of homogenous classes of subjects for therapeutic assays, (4) objectiveness of drug-molecular target interaction, (5) follow-up of disease evolution and treatment.</div>
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