Dopamine D3 receptor antagonists: The quest for a potentially selective PET ligand. Part 3: Radiosynthesis and in vivo studies

Bennacef, Idriss; Salinas, Cristian; Bonasera, Thomas A.; Gunn, Roger N.; Audrain, Hélène; Jakobsen, Steen; Nabulsi, Nabeel; Weinzimmer, David; Carson, Richard E.; Huang, Yiyun; Holmes, Ian P.; Micheli, Fabrizio; Heidbreder, Christian; Gentile, Gabriella; Rossi, Tino; Laruelle, Marc

doi:10.1016/j.bmcl.2009.07.055

Cited by 23 publications

(13 citation statements)

References 14 publications

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“…The log P value of this compound is 2.9, which means that it should readily cross the blood-brain barrier(Waterhouse, 2003). Unfortunately, in vivo imaging in rhesus monkeys revealed no specific binding to D 3 receptors (Bennacef et al, 2009). …”

Section: Introductionmentioning

confidence: 99%

Endogenous dopamine (DA) competes with the binding of a radiolabeled D₃ receptor partial agonist in vivo: A positron emission tomography study

Mach

et al. 2011

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A series of microPET imaging studies were conducted in anesthetized rhesus monkeys using the dopamine D3-selective partial agonist, [18F]5. There was variable uptake in regions of brain known to express a high density of D3 receptors under baseline conditions. Pretreatment with lorazepam (1 mg/kg, i.v. 30 min) to reduce endogenous dopamine activity prior to tracer injection resulted in a dramatic increase in uptake in the caudate, putamen, and thalamus, and an increase in the binding potential (BP) values, a measure of D3 receptor binding in vivo. These data indicate that there is a high level of competition between [18F]5 and endogenous dopamine for D3 receptors in vivo.

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Section: Introductionmentioning

confidence: 99%

Endogenous dopamine (DA) competes with the binding of a radiolabeled D₃ receptor partial agonist in vivo: A positron emission tomography study

Mach

et al. 2011

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“…Several attempts have been made in the past to develop D 3 probes (see for e.g. Bennacef et al, 2009;Hocke et al, 2014;Sovago et al, 2005;Xu et al, 2009), but currently the only available probe is [ 11 C]-( + )-PHNO.…”

Section: Development Of a Pet Probe To Investigate D 3 Receptors In Hmentioning

confidence: 99%

Imaging the D3 dopamine receptor across behavioral and drug addictions: Positron emission tomography studies with [11C]-(+)-PHNO

Boileau

Nakajima

Payer

2015

European Neuropsychopharmacology

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“…40). Unfortunately, and quite unexpectedly, despite a high pK i value in pig native tissue and other preclinical species, [110] no specific PET signal could be detected in vivo (in pig) for compound 44. In 2008, Hocke et al [105] reported the synthesis of close analogues of FAUC 346 and BP 879 (1), such as compounds 41.…”

Section: Introductionmentioning

confidence: 96%

Recent Advances in the Development of Dopamine D₃Receptor Antagonists: a Medicinal Chemistry Perspective

Micheli

2011

ChemMedChem

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Dopamine (DA) D(3) receptor antagonism might play a significant role in different therapeutic areas. A high number of preclinical studies on DA D(3) receptor antagonists have shown efficacy in animal models of Parkinson's disease, schizophrenia and drug dependence. This Review covers the activities of medicinal chemists in this field over the last ten years towards the identification of truly selective compounds. Both primary and patent literature is reviewed here. Since the original discoveries, a clear trend towards the optimization of the developability properties of the new scaffold has clearly emerged with time, from both academic and industrial researchers. Examples of advanced leads from academia and industry are described. The latest potential therapeutic applications are reported too.

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Dopamine D3 receptor antagonists: The quest for a potentially selective PET ligand. Part 3: Radiosynthesis and in vivo studies

Cited by 23 publications

References 14 publications

Endogenous dopamine (DA) competes with the binding of a radiolabeled D₃ receptor partial agonist in vivo: A positron emission tomography study

Endogenous dopamine (DA) competes with the binding of a radiolabeled D₃ receptor partial agonist in vivo: A positron emission tomography study

Imaging the D3 dopamine receptor across behavioral and drug addictions: Positron emission tomography studies with [11C]-(+)-PHNO

Recent Advances in the Development of Dopamine D₃Receptor Antagonists: a Medicinal Chemistry Perspective

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Dopamine D3 receptor antagonists: The quest for a potentially selective PET ligand. Part 3: Radiosynthesis and in vivo studies

Cited by 23 publications

References 14 publications

Endogenous dopamine (DA) competes with the binding of a radiolabeled D3 receptor partial agonist in vivo: A positron emission tomography study

Endogenous dopamine (DA) competes with the binding of a radiolabeled D3 receptor partial agonist in vivo: A positron emission tomography study

Imaging the D3 dopamine receptor across behavioral and drug addictions: Positron emission tomography studies with [11C]-(+)-PHNO

Recent Advances in the Development of Dopamine D3Receptor Antagonists: a Medicinal Chemistry Perspective

Contact Info

Product

Resources

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Endogenous dopamine (DA) competes with the binding of a radiolabeled D₃ receptor partial agonist in vivo: A positron emission tomography study

Endogenous dopamine (DA) competes with the binding of a radiolabeled D₃ receptor partial agonist in vivo: A positron emission tomography study

Recent Advances in the Development of Dopamine D₃Receptor Antagonists: a Medicinal Chemistry Perspective