Synthesis and Biodistribution of (R,S)-[O-Methyl-11C]-1-[3-(5-Methoxy-1,2,3,4-tetrahydro-1-naphtalenyl)propyl]-4-Phenylpiperazine (PNU-157760), A Putative Radioligand for 5-HT1AReceptors

Matarrese, Mario; Soloviev, D.; Moresco, Rosa María; Ferri, V.; Simonelli, Pasquale; Magni, Fulvio; Colombo, Diego; Todde, Sergio; Carpinelli, A.; Fazio, Ferruccio; Kienle, Marzia Galli

doi:10.1006/bioo.1998.1089

Cited by 11 publications

(2 citation statements)

References 28 publications

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“…Another potent phenylpiperazine agonist PNU-157760 ( K i = 0.5 nM) was radiolabeled through 11 C- O -methylation at a tetrahydronaphthalene moiety to generate [ 11 C]PNU-157760 ([ 11 C] 42 , Figure ). Biodistribution experiments in rats showed that this radiotracer could penetrate the BBB and reached the maximal brain uptake at 30 min postinjection. However, similar to [ 11 C] 39 , [ 11 C] 42 failed to give any receptor-specific signal in vivo, perhaps due to its affinity to α 1 AR (IC 50 = 43 nM) and sigma receptor sites (IC 50 = 198 nM, [ 3 H]DTG assay).…”

Section: Pet Ligands For 5-ht1a Receptorsmentioning

confidence: 99%

Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors

Rong

Chen

et al. 2022

J. Med. Chem.

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Serotonin (5-hydroxytryptamine, 5-HT) and 5-HT receptors (5-HTRs) have crucial roles in various neuropsychiatric disorders and neurodegenerative diseases, making them attractive diagnostic and therapeutic targets. Positron emission tomography (PET) is a noninvasive nuclear molecular imaging technique and is an essential tool in clinical diagnosis and drug discovery. In this context, numerous PET ligands have been developed for "visualizing" 5-HTRs in the brain and translated into human use to study disease mechanisms and/or support drug development. Herein, we present a comprehensive repertoire of 5-HTR PET ligands by focusing on their chemotypes and performance in PET imaging studies. Furthermore, this Perspective summarizes recent 5-HTR-focused drug discovery, including biased agonists and allosteric modulators, which would stimulate the development of more potent and subtype-selective 5-HTR PET ligands and thus further our understanding of 5-HTR biology.

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Section: Pet Ligands For 5-ht1a Receptorsmentioning

confidence: 99%

Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors

Rong

Chen

et al. 2022

J. Med. Chem.

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“…22 5-Hydroxy benzimidazolyl 2-carbaldehyde (10h) was also obtained from the demethylation of 10e using tribromoborane (BBr 3 , 2 eq) in methylene chloride at −78 o C. 23 The curcumin mimic library like 13 and its constitutional isomeric curcumin derivatives such as 14 were obtained from the aldol reaction of 11 and 12 with synthetic benzimidazolyl 2-carbaldehyde compounds (10a-10g), respectively. 8 The instrumental data of curcumin library confirmed through 1 H NMR and…”

mentioning

confidence: 99%