Abstract: The present invention concerns the prototypical pharmacologic profile of GABA-stearamide, GABA-palmitamide, GABA-linoleamide and Progabide characterized by their interesting positive modulation of at least one ?-aminobutyric acid A receptor being GABA (A) and GABA (B), which are principally extrasynaptic, for treating a neurodegenerative or neurodevelopmental disease. The present invention further 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 the Glutamate/GABA imbalance, with protective and preventive action against all the behavioral abnormalities, the cognitive deficits and neurotoxicities, in neurodegenerative (Alzheimer's, Parkinson's Huntington's and Multiple Sclerosis) diseases and neurodevelopmental diseases (Autism spectrum desorders and related syndroms).

Abstract: 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(?)].

Abstract: This invention concerns a dosage form comprising a therapeutically neuroprotective amount of A2-73 and a neuroprotective amount of at least one cooperating acetylcholinesterase inhibitor selected from the group consisting of donepezil, galantamine, rivastigmine, or memantine and method of use.

Abstract: This invention concerns a dosage form comprising a therapeutically neuroprotective amount of A2-73 and a neuroprotective amount of at least one cooperating acetylcholinesterase inhibitor selected from the group consisting of donepezil, galantamine, rivastigmine, or memantine and method of use.

Abstract: The present invention involves new and original sigma receptors ligands: (Mono-or di-alkylaminoalkyl)-?-butyrolactones, their analogues aminotetrahydrofuranes, the (1-adamantyl) phenyl(s) alkylamines, the N,N Dialkyl ?-[(adamantyl-l)benzyloxy-2] alkylamines and the 3-cyclopentyl adamantyl-amines or alkylamines or alkyl phenylamines, their enantiomers or diastereoisomers and their pharmaceutically acceptable salts, with pro-apoptotic and/or anti-apoptotic properties over cellular biochemical mechanisms, with anti-cancer, anti-metastatic, anti-(chronic) inflammatory, neuro-protective, anticonvulsive, antidepressive and nooanaleptic or sedative action.

Abstract: The present invention discloses the prototypical profile of 3,3-diphenyl-N-(1-phenylethyl) propan-1-amine (fendiline) against the anticancer drugs induced neuropathic pain (ADINP). Indeed, fendiline exhibited high analgesic activity against the Paclitaxel induced neuropathic sensitization (PINS), in mice, and also inducing decrease of brain dopamine (DA) turnover, in rats and mice, i.e., the exactly opposite effects of those induced by the ?-opioid receptor agonists (?-ORAs). Thus, the above properties of fendiline allow the beneficial synergy of fendiline and ?-ORAs, with fendiline reinforcing the analgesic properties of ?-ORAs and protecting against the opioid dependence and the neurotoxicity of ?-ORAs, coming from the increase of the brain DA turnover induced by the ?-ORAs.

Abstract: The present invention discloses the prototypical profile of N-Stearyl dopamine (NS-DA) against the anticancer drugs induced neuropathic pain (ADINP). Indeed, NS-DA exhibited high analgesic activity against the Paclitaxel induced neuropathic sensitization (PINS), in mice, and also decrease of brain dopamine (DA) turnover and of motility, in rats and mice, i.e., the exactly opposite effects of those induced by the ?-opioid receptor agonists (?-ORAs). Thus, the above properties of NS-DA allow the beneficial synergy of NS-DA and ?-ORAS, with NS-DA reinforcing the analgesic properties of ?-ORAs and protecting against the opioid dependence and the neurotoxicity of ?-ORAs, coming from the increase of the brain DA turnover induced by the ?-ORAs.

Abstract: Tetrahydro-N-methyl-2,2-diphenyl-3-furanomethanamine (AE37Met) is a highly selective ligand of the extrasynaptic NMDA receptors, of the M2 muscarinic autoreceptors and of the sigma-1 (?1) receptors, with prototypical brain, preventive and therapeutical, protective activity. This invention concerns the prototypical profile of AE37Met and its pharmaceutically acceptable salts, with cytoprotective activity, more specifically for brain glial cells and neurons, against the neuro-degenerative diseases (e.g. Alzheimer's, Huntington's and Parkinson's diseases, depression, brain ischemia/hypoxia, traumatic brain injury and epilepsy), by the highly selective antagonisms, exerced by AE37Met, on the extrasynaptic NMDA glutamatergic receptors [eNMDA(?)] and on the M2 muscarinic cholinergic autoreceptors [M2(?)], associated with a highly selective sigma-1 agonism [?1(+)]. The above prototypical profile was observed only with AE37Met between the other family members (AE14, AE37 and their enantiomers).

Abstract: The present invention involves new and original sigma receptors ligands: (Mono- or dialkylaminoalkyl)-?-butyrolactones, their analogues aminotetrahydroturanes, the (1-adamantyl)benzene alkylamines, the N,N Dialkyl ?-[(adamantyl-1)benzyloxy-2]alkylamines and the 3-cyclopentyl adamantyl-amines or alkylamines or -alkyl phenylamines, their enantiomers or diastereoisomers, their pharmaceutically acceptable salts and Quinacrine Me-thylene blue, Asteinizole and their relative analogues with pro-apoptotic and/or anti-apoptotic properties over cellular biochemical mechanisms, with prototypical anti-cancer, antimetastatic and antiviral activities associated with antagonism of the neuropatic pain and, at very low doses, with cytoprotective and cytoregenerative activity against the cytodegenerative diseases.

Abstract: The present invention involves the selected aminotetrahydrofurans AE37, AE37Met, AE14 and their enantiomers as original mixed sigma-1/muscarinic ligands for the optimization of the anticholinesterasic drugs and more specifically of Donepezil, Galantamine or Rivastigmine. Indeed, these aminotetrahydrofurans exhibited M2 and M3 muscarinic antagonisms against the cholinergic adverse effects of these drugs, which constitute the most limitating factor in the use of these drugs against the symptoms of the Alzheimer's disease (AD). Moreover, by their antagonism of the presynaptic muscarinic M2 cholinergic autoreceptors and their very selective sigma-1 agonism they constitute putative agents for the valorization of the anticholinesterasic drugs and more specifically of Donepezil, Galatamine or Rivastigmine from their present status of drugs acting against the symptoms of AD to the perspective of therapeutic agents against the evolution of AD.

Abstract: This invention concerns a dosage form comprising a therapeutically neuroprotective amount of A2-73 and a neuroprotective amount of at least one cooperating acetylcholinesterase inhibitor selected from the group consisting of donepezil, galantamine, rivastigmine, or memantine and method of use.

Abstract: The present invention involves new and original sigma receptors ligands: (Mono-or dialkylaminoalkyl)-?-butyrolactones, their analogues aminotetrahydroturanes, the (1-adamantyl) benzene alkylamines, the N,N Dialkyl ?-[(adamantyl-1)benzyloxy-2] alkylamines and the 3-cyclopentyl adamantyl-amines or alkylamines or-alkyl phenylamines, their enantiomers or diastereoisomers, their pharmaceutically acceptable salts and Quinacrine Me-thylene blue, Asteinizole and their relative analogues with pro-apoptotic and/or anti-apoptotic properties over cellular biochemical mechanisms, with prototypical anti-cancer, antimetastatic and antiviral activities associated with antagonism of the neuropatic pain and, at very low doses, with cytoprotective and cytoregenerative activity against the cytodegenerative diseases.

Abstract: The present invention involves new and original sigma receptors Ligands: (Mono-or dialkylaminoalkyl)-?-butyro-lactones, their analogues aminotetrahydroturanes, the (1-adamantyl) benzene alkylamines, the N,N Dialkyl ?-[(adamantyl-1)ben-zyloxy-2] alkylamines and the 3-cyclopentyl adamantyl-amines or alkylamines or-alkyl phenylamines, their enantiomers or di-astereoisomers, their pharmaceutically acceptable salts and Quinacrine Me-thylene blue, Astemizole and their relative analogues with pro-apoptotic and/or anti-apoptotic properties over cellular biochemical mechanisms, with prototypical anti-cancer, an-timetastatic and antiviral activities associated with antagonism of the neuropatic pain and, at very low doses, with cytoprotectve and cytoregenerative activity against the cytodegenerative diseases.

Abstract: The present invention involves new and original sigma receptors ligands : (Mono- or di-alkylaminoalkyl)-?-butyrolactones, their analogues aminotetrahydrofuranes, the (1-adamantyl)phenyl(s) alkylamines, the N,N Dialkyl ?-[(adamantyl-1)benzyloxy-2] alkylamines and the 3-cyclopentyl adamantyl-amines or alkylamines or -alkyl phenylamines, their enantiomers or diastereoisomers and their pharmaceutically acceptable salts, with pro-apoptotic and/or anti-apoptotic properties over cellular bio-chemical mechanisms, with anti-cancer, anti-metastatic, anti-(chronic) inflammatory, neuro-protective, anticonvulsive, antidepressive and nooanaleptic or sedative action.