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PROTOTYPICAL MOLECULAR PHARMACOLOGIC PROFILE OF FENDILINE AGAINST NEURODEGENERATIVE AND NEURODEVELOPMENTAL DISEASES
专利权人:
Alexandre Vamvakides
发明人:
Alexandre Vamvakides
申请号:
US15381338
公开号:
US20180193289A1
申请日:
2016.12.16
申请国别(地区):
US
年份:
2018
代理人:
摘要:
The present invention concerns the prototypical pharmacologic profile of 3,3-diphenyl-N-(1-phenylethyl) propan-1-amine (Fendiline), its enantiomers and its pharmaceutically acceptable salts characterized by their selective sigma-1 receptor affinity (vs, sigma-2 receptor: 14 to 18 nM vs 730 to 850 nM) and, therefore, prototypical allosteric antagonisms of brain N-methyl-D-aspartate receptors [NMDA(−)], sodium channels [Nav(−)] and discreet desensitization of muscarinic receptors [M(−)]. Of interest is the positive allosteric modulation of the γ-aminobutyric acid A (GABA) (A) and GABA (B) receptors, originating brain pro-GABAergic and anti-glutamatergic activities and also an unique pharmacological profile which antagonize all the components of the vicious circle generated in the brain by Glutamate/GABA imbalance, with protective and preventive action against all the behavioral abnormalities, the cognitive deficits and neurotoxicities, in neurodegenerative (Alzheimers, Parkinsons Huntingtons and Multiple Sclerosis) diseases and neurodevelopmental diseases (Autism spectrum disorders and related syndromes).
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