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Titolo:
AMINO-TETRABENAZINE AND AMIDO-TETRABENAZINE DERIVATIVES - SYNTHESIS AND EVALUATION AS POTENTIAL LIGANDS FOR THE VESICULAR MONOAMINE TRANSPORTER
Autore:
CANNEY DJ; KUNG MP; KUNG HF;
Indirizzi:
UNIV PENN,DEPT RADIOL PHILADELPHIA PA 19104 UNIV PENN,DEPT RADIOL PHILADELPHIA PA 19104
Titolo Testata:
Nuclear medicine and biology
fascicolo: 4, volume: 22, anno: 1995,
pagine: 527 - 535
SICI:
0969-8051(1995)22:4<527:AAAD-S>2.0.ZU;2-7
Fonte:
ISI
Lingua:
ENG
Soggetto:
POSITRON EMISSION TOMOGRAPHY; )H-3>DIHYDROTETRABENAZINE BINDING; H-3 DIHYDROTETRABENAZINE; TISSUE DISTRIBUTION; C-11 TETRABENAZINE; RECEPTOR-BINDING; STORAGE-VESICLES; MOUSE-BRAIN; SITES;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
38
Recensione:
Indirizzi per estratti:
Citazione:
D.J. Canney et al., "AMINO-TETRABENAZINE AND AMIDO-TETRABENAZINE DERIVATIVES - SYNTHESIS AND EVALUATION AS POTENTIAL LIGANDS FOR THE VESICULAR MONOAMINE TRANSPORTER", Nuclear medicine and biology, 22(4), 1995, pp. 527-535

Abstract

Tetrabenazine (TBZ) and dihydrotetrabenazine are well known inhibitors of the CNS vesicular monoamine transporter (VMAT), which is responsible for the packaging of monoamine neurotransmitters in presynaptic vesicles. Amino and amido derivatives of tetrabenazine were prepared as potential ligands for the vesicular monoamine transporter. Ultimately,organotin derivatives of promising ligands were prepared for radiolabeling with I-125. The compounds were evaluated for their ability to inhibit the specific binding of a selective radioligand to the transporter in rat striatal homogenates. Of the compounds evaluated, three amine derivatives of TBZ (primary, secondary and tertiary) were found to have modest to high affinity for the transporter, while two amides exhibited low to undectable affinity. The secondary propargyl amine was found to possess the highest affinity (K-i = 7.6 nM) and was chosen for further evaluation. The organotin derivative of this compound was synthesized in order to prepare the corresponding radioiodinated ligand. However, our inability to synthesize and characterize the iodinated amine precluded its evaluation as a potential radioiodinated ligand for the transporter. Alternative approaches for decreasing the lipophilicity of TBZ analogs while maintaining high binding affinity are currentlybeing explored.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 06/04/20 alle ore 02:07:04