Decahydroquinoline-Based Anti-Cholinergic Agents
- Technology Benefits
- Convergence speed is faster than the one obtained through conventional technologies
- Technology Application
- Optical flow estimation This technology is available for licensing.
- Detailed Technology Description
- Researchers at the University of California, Santa Barbara have developed compounds with anticholinergic activity useful for modulating cholinergic function in mammals. These compounds may exist in and be isolated in optically active and racemic forms. Some compounds may exhibit polymorphism.
- Supplementary Information
- Patent Number: US5929087A
Application Number: US1997826830A
Inventor: Efange, S. Mbua Ngale | Parsons, Stanley M.
Priority Date: 8 Apr 1997
Priority Number: US5929087A
Application Date: 8 Apr 1997
Publication Date: 27 Jul 1999
IPC Current: C07D040104
US Class: 514314 | 514278 | 546017 | 546154 | 546158 | 546164
Assignee Applicant: Regents of the University of Minnesotanneapolis
Title: Decahydroquinoline-based anti-cholinergic agents
Usefulness: Decahydroquinoline-based anti-cholinergic agents
Summary: (I) and (II) are useful for inhibiting cholinergic function by inhibiting vesicular acetylcholine transporter in the treatment of cardiac arrhythmia, for inhibiting the release of acetylcholine in a mammal exposed to a chemical agent (chemical weapon) that inhibits acetylcholinesterase, before or after exposure to the chemical agent (claimed). (I) and (II) may also be used as imaging agents for mapping cholinergic innervation in the brain.
Novelty: New decahydroquinoline derivatives are anticholinergic agents, useful for the treatment of cardiac arrhythmia and chemical weapon poisoning
- Industry
- Chemical/Material
- Sub Category
- Chemical/Material Application
- Application No.
- 5929087
- Others
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Background
Vesamicol is a well-known lipophilic analogue of the choline precursor deanol. In small to moderate doses, vesamicol induces respiratory paralysis and death in laboratory animals. Investigations of the mechanism underlying the actions of vesamicol led to the identification of a vesicular acetylcholine transporter (VAChT). VAChT is a protein complex which transports acetylcholine (ACh) from its site of synthesis in the cytosol into the synaptic vesicle. Vesamicol has no effect on pre-loaded vesicles, and vesamicol-mediated anti-cholinergic effects are frequency-dependent (reflecting the depletion of a pre-loaded vesicle pool). The identification of the VAChT provides another point for potential regulation of cholinergic function. Moreover, the availability of vesamicol, a prototypical antagonist for the VAChT, provides an alternative method for modulating cholinergic function in the central and peripheral nervous system. There is a need for novel, potent, and selective VAChT antagonists and agonists of moderate lipophilicity, which display enhanced penetration into the central nervous system.
Additional Technologies by these Inventors
Tech ID/UC Case
22783/1997-278-0
Related Cases
1997-278-0
- *Abstract
-
Compounds with anticholinergic activity useful for modulating cholinergic function in mammals.
- *Applications
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- Optical flow estimation
- *IP Issue Date
- Jul 27, 1999
- *Principal Investigator
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Name: Simon M.N. Efange
Department:
Name: Stanley Parsons
Department:
- Country/Region
- USA
