Effects of two-carbon bridge region methoxylation of benztropine: discovery of novel chiral ligands for the dopamine transporter.

Author: BaruchelloR, BianchiC, BoreaP A, CavalliniS, GessiS, InvidiataF P, MarinoS, MerighiS, RobertiM, RondaninR, RossiM, SimoniD, SiniscalchiA, VaraniK

Paper Details 
Original Abstract of the Article :
6-Methoxylated and 8-oxygenated benztropines were prepared and evaluated for their DAT and SERT activity (binding and uptake inhibition). Methoxylation at the two-carbon bridge of benztropine produced a novel class of potent and selective DAT ligands. An interesting enantioselectivity was also obser...See full text at original site
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引用元:
https://doi.org/10.1016/s0960-894x(01)00068-3

データ提供:米国国立医学図書館(NLM)

A Novel Class of Chiral Benztropines: Exploring New Pathways for Dopamine Transporter Modulation

The study of [dopamine transporter (DAT)] ligands is like a fascinating exploration of a vast and complex desert, where each molecule holds the potential for unlocking new therapeutic possibilities. This research investigates the effects of [methoxylation] at specific positions within the [benztropine] molecule, seeking to develop novel and potent DAT ligands.

Methoxylation Unveils Potent and Selective DAT Ligands

The researchers discovered that [methoxylation] at the two-carbon bridge region of benztropine yielded a new class of potent and selective DAT ligands. These findings suggest that strategically modifying the benztropine structure can lead to the development of new drugs with targeted activity at the DAT. This discovery opens up exciting avenues for further research and exploration of these novel ligands.

A New Frontier in DAT Ligand Design

This research is a testament to the power of molecular modification in drug development. The authors' work highlights the importance of exploring different structural modifications to design potent and selective DAT ligands. The findings pave the way for further research into the therapeutic potential of these novel benztropine derivatives, potentially leading to the development of new treatments for conditions related to dopamine signaling.

Dr.Camel's Conclusion

This research is like a treasure hunt in the desert, where the authors have uncovered a new and promising class of DAT ligands. The findings demonstrate the importance of creative and innovative approaches to drug design, seeking to unlock the potential of molecules for therapeutic benefit. These novel benztropines hold promise for future research and development, potentially leading to new treatments for a range of neurological and psychiatric conditions.

Date :
  1. Date Completed 2001-06-28
  2. Date Revised 2019-08-19
Further Info :

Pubmed ID

11277529

DOI: Digital Object Identifier

10.1016/s0960-894x(01)00068-3

Related Literature

SNS
PICO Info
in preparation
Languages

English

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