Dopamine transporter binding without cocaine-like behavioral effects: synthesis and evaluation of benztropine analogs alone and in combination with cocaine in rodents.

Author: AgostonG E, AllingK L, ForsterM J, KatzJ L, KlineR H, KopajticT A, NewmanA H, WoolvertonW L

Paper Details 
Original Abstract of the Article :
Previous SAR studies demonstrated that small halogen substitutions on the diphenylether system of benztropine (BZT), such as a para-Cl group, retained high affinity at the cocaine binding site on the dopamine transporter. Despite this high affinity, the compounds generally had behavioral effects dif...See full text at original site
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引用元:
https://doi.org/10.1007/s002130000667

データ提供:米国国立医学図書館(NLM)

Exploring the Dopamine Transporter: A Journey Through Molecular Interactions

The intricate world of molecular interactions fascinates Dr. Camel. This research delves into the fascinating dance between molecules, specifically focusing on the dopamine transporter and its interaction with various compounds. The study explores the binding affinity of benztropine analogs to the cocaine binding site on the dopamine transporter, revealing intriguing insights into their potential effects.

The authors investigated a series of benztropine analogs, modifying their chemical structure to understand their binding affinity and behavioral effects. They observed that small halogen substitutions on the diphenylether system of benztropine, particularly a para-Cl group, retained high affinity at the cocaine binding site. However, these compounds exhibited behavioral effects distinct from cocaine. In contrast, compounds with meta-Cl substitutions displayed effects more akin to cocaine, suggesting a crucial role for molecular structure in influencing these interactions.

A Delicate Balance of Molecular Interactions

The research reveals the delicate balance of molecular interactions that govern the effects of drugs. Slight modifications to the molecular structure of benztropine analogs can significantly impact their binding affinity and ultimately their behavioral effects. This finding underscores the importance of understanding these interactions for developing drugs with targeted therapeutic effects.

Navigating the Desert of Drug Discovery with Precision

Dr. Camel finds this research inspiring. It's like navigating a vast desert, meticulously mapping out the intricate pathways of molecular interactions. Understanding these pathways allows researchers to develop drugs with precise therapeutic effects, minimizing unintended consequences. This research highlights the power of molecular design in drug discovery, paving the way for more effective and targeted therapies.

Dr. Camel's Conclusion

This study takes us on a fascinating journey through the complex world of molecular interactions, demonstrating the profound impact of chemical structure on drug effects. The findings provide valuable insights into the design of drugs that target specific molecular pathways, paving the way for more effective and targeted therapies.

Date :
  1. Date Completed 2001-09-13
  2. Date Revised 2019-12-10
Further Info :

Pubmed ID

11349389

DOI: Digital Object Identifier

10.1007/s002130000667

Related Literature

SNS
PICO Info
in preparation
Languages

English

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