200 results about "NMDA receptor" patented technology

Topical compositions and methods for treating pain. The invention provides oil-in-water emulsions comprising an antidepressant; an NMDA-receptor antagonists; a lipophilic component; water; and a surfactant. The compositions induce a local-anesthetic effect when topically administered to intact skin thereby treating or preventing pain, for example, neuropathic pain.

The invention relates to a morphinan-derivative that targets NMDA receptors on pancreatic islets and has the general formula (I)whereinR1 is selected from —OH, —CO2H, —R0, —OR0, —OC(═O)R0, —OC(═O)OR0 or —OC(═O)NHR0; and R2 is selected from —H, —R0, —C(═O)R0, —C(═O)OR0, —C(═O)NHR0 or —C(═NH)—NH—C(═NH)—NH2; wherein R0 is in each case independently selected from —C1-C6-alkyl, -aryl, -heteroaryl, —C1-C6-alkyl-aryl or —C1-C6-alkyl-heteroaryl, in each case independently unsubstituted or substituted;or its physiologically acceptable salt and / or stereoisomer, including mixtures thereof in all ratios, for use in the treatment of a disease or condition, where the disease or condition is insulin-dependent diabetes mellitus, non-insulin-dependent diabetes mellitus, obesity, and / or diabetic nephropathy.

A method is presented for the preparation of topically applied compositions used for the treatment of regional pain, especially sympathetically mediated pain. NMDA receptor antagonists, such as ketamine or dextromethorphan, and one or more tricyclic antidepressants, such as amitriptyline, in combination, are employed.

Coupling of excitation to neurogenesis in proliferating post-natal NPCs is demonstrated in vitro and in vivo. Neurogenesis is potently enhanced by excitatory stimuli, and involves Cav1.2 / 1.3 channels and NMDA receptors. These Ca2+ influx pathways are located on the proliferating NPCs, allowing them to directly sense and process excitatory stimuli. Excitation increases the fraction of NPC progeny that are neurons, and increases total neuron number. Signaling in this pathway leads to rapid induction of a proneural gene expression pattern involving the bHLH genes HES1, Id2, and NeuroD, and the resulting cells become fully functional neurons defined by neuronal morphology, expression of neuronal structural proteins, expression of neuronal TTX-sensitive voltage gated Na+ channels, and synaptic incorporation into active neural circuits.

Improved treatments of joint diseases, such as, e.g. osteoarthritis and rheumatoid arthritis, and pain, wherein a strontium-containing compound is administered alone or in combination with one or more second therapeutically and / or prophylactically active substances, selected from the group consisting of bisphosphonates, glucosamine, pallitative agents, analgesic agents, disease modifying anti-rheumatic compounds (DMARDs), selective estrogen receptor modulators (SERMs), aromatase inhibitors, non-steroidal anti-inflammatory agents (NSAIDs), COX-2 inhibitors, COX-3 inhibitors, opioids, inhibitors / antagonists of IL-1, inhibitors / antagonists of TNF-alpha, inhibitors of matrix metallo-proteinases (MMPs), cathepsin K inhibitors, inhibitors / antagonists of RANK-ligand, statins, glucocorticoids, chondroitin sulphate, NMDA receptor antagonists, inhibitors of interleukin-I converting enzyme, Calcitonin gene related peptide antagonists, glycine antagonists, vanilloid receptor antagonists, inhibitors of inducible nitric oxide synthetase (iNOS), N-acetylcholine receptor agonists, neurokinin antagonists, neuroleptic agents, PAR2 receptor antagonists and anabolic growth factors acting on joint tissue components. Pharmaceutical compositions comprising a strontium-containing compound and a second therapeutically and / or prophylactically active substance as defined above.

A methods, kits and compositions for diagnosing a central nervous system disorder, particularly transient ischemic attack or stroke, comprising measuring the level of NR2A and / or NR2B NMDA receptor or fragment thereof, in a biological sample from a human subject, and optionally measuring other biomarkers such as homocysteine and glutamate. The method is particularly useful for identifying individuals that are at risk for stroke, and for diagnosing stroke in an emergency room setting.

A method for treating pain in painful diabetic neuropathy comprises administering in combination a first agent that comprises a compound as defined herein, illustratively lacosamide, and a second agent effective to provide enhanced treatment of pain, by comparison with the first agent alone. The second agent illustratively comprises an analgesic, an anticonvulsant, an antidepressant or an NMDA receptor antagonist.

The present embodiments relate to topically delivered medication (compounded) for treatment of pain, inflammation, muscle fatigue, spasms, and / or other ailments. A transdermal cream may provide the effective topical administration of multiple medications simultaneously. The transdermal cream may include a salt load of approximately 30% or greater. The transdermal cream may include a unique base composition such that the transdermal cream may be able to remain stable and avoid degradation for six months or more and capable of effective delivery of active ingredient concentrations exceeding approximately 40% or more of the total formulation weight. The active ingredients may include a nerve depressant, NSAID, muscle relaxant, opiate agonist, local anesthetic, NMDA receptor antagonist, and a tricyclic antidepressant. In one embodiment, the transdermal cream may comprise ketamine HCL, gabapentin, clonidine HCL and baclofen. The transdermal cream may deliver an enhanced topical delivery flux of ketamine via a single transdermal application.

Coupling of excitation to neurogenesis in proliferating post-natal NPCs is demonstrated in vitro and in vivo. Neurogenesis is potently enhanced by excitatory stimuli, and involves Cav1.2 / 1.3 channels and NMDA receptors. These Ca2+ influx pathways are located on the proliferating NPCs, allowing them to directly sense and process excitatory stimuli. Excitation increases the fraction of NPC progeny that are neurons, and increases total neuron number. Signaling in this pathway leads to rapid induction of a proneural gene expression pattern involving the bHLH genes HES1, Id2, and NeuroD, and the resulting cells become fully functional neurons defined by neuronal morphology, expression of neuronal structural proteins, expression of neuronal TTX-sensitive voltage gated Na+ channels, and synaptic incorporation into active neural circuits.

A methods, kits and compositions for diagnosing a central nervous system disorder, particularly transient ischemic attack or stroke, comprising measuring the level of NR2A and / or NR2B NMDA receptor or fragment thereof, in a biological sample from a human subject, and optionally measuring other biomarkers such as homocysteine and glutamate. The method is particularly useful for identifying individuals that are at risk for stroke, and for diagnosing stroke in an emergency room setting.

A methods, kits and compositions for diagnosing a central nervous system disorder, particularly transient ischemic attack or stroke, comprising measuring the level of NR2A and / or NR2B NMDA receptor or fragment thereof, in a biological sample from a human subject, and optionally measuring other biomarkers such as homocysteine and glutamate. The method is particularly useful for identifying individuals that are at risk for stroke, and for diagnosing stroke in an emergency room setting.

A method for treating autism comprising the step of administering an effective amount of a medicament characterized as a NMDA-receptor antagonist or a pharmaceutically acceptable salt thereof.

The present embodiments relate to topically delivered compounded medications. A transdermal cream may provide the effective topical administration of multiple medications simultaneously; may include low concentrations of local anesthetics, a NSAID, an anticonvulsant, and / or other active ingredients; and may include lidocaine, prilocaine, meloxicam, and lamotrigine and / or topiramate. Alternatively, the transdermal cream may include a lidocaine / prilocaine base cream to which is added a fine powder of one or more ground up medications to form a compounded medication. The compounded medication in powder form may be generated from grinding up tablets of NSAIDs, anticonvulsants, nerve depressants, antidepressants, muscle relaxants, NMDA receptor antagonists, opiate or opioid agonists, and / or other agents. The compounded medication in powder form may include meloxicam, lamotrigine, topiramate, other active ingredients, and DMSO or Sterile Water for Irrigation. In another aspect, the present embodiments relate to methods of compounding medications and transdermal creams or gels.