36 results about "NA - Noradrenaline" patented technology

The present invention provides a method of treating fibromyalgia syndrome (FMS), chronic fatigue syndrome (CFS), and pain in an animal subject comprising administering a therapeutically effective amount of a dual serotonin norepinephrine reuptake inhibitor compound or a pharmaceutically acceptable salt thereof, wherein said dual serotonin norepinephrine reuptake inhibitor compound is characterized by a non-tricyclic structure and a greater inhibition of norepinephrine reuptake than serotonin reuptake, and wherein said compound is not administered adjunctively with phenylalanine or tyrosine. In particular, the use of milnacipran to treat FMS, CFS, and pain is disclosed.

The present invention relates to methods and compositions for reducing Distress Dysfunction by restoring and maintaining homeostatic balance in the neurotransmitter systems underlying the Stress Response and the experience of distress and hedonic tone. Distress Dysfunction refers to the experience of dysfunctional emotional and physical distress that interferes with the individual's quality of life and functioning. A novel understanding of the bimodal opioid modulation of pain, and its impact, through serotonergic, dopaminergic, epinephrinergic, and norepinephrinergic processes, on hedonic tone, leads directly to new generation pharmaceutical formulations that are remarkably safe and effective for the treatment of a wide variety of Distress Dysfunctions, including anxiety, depression, anger, insomnia, mood disorders, eating disorders, sexual problems, pain, substance and behavioral addictions, gastrointestinal disorders, autistic spectrum disorders, attention-deficit and hyperactivity disorders, and other emotional and physical distress disorders. The foundation of this discovery is the power of Receptor Switchers, such as ultra-low-dose and very-low-dose opioid antagonists and GM1 ganglioside attenuators, in blocking acute and protracted excitatory opioid receptor signaling. Co-administration of Receptor Switchers with Endorphin Enhancers, such as specific cAMP PDE inhibitors and excitatory amino acids, is an excellent formulation for restoring healthy homeostatic balance to the endogenous opioid system, using the body's endorphins to reduce emotional and physical distress, and through synergistic and homeostatic processes, restoring positive hedonic tone. The addition of Synergistic Enhancers, such as amino acids, SSRI and SNRI agents, and non-opioid analgesics, as well as Exogenous Opioids, enhances and prolongs these therapeutic benefits. The novel principles discovered by this invention also teach a new generation of safe and effective formulations for the treatment of respiratory conditions, neuropathy, and nociceptive pain.

The invention relates to novel cyclohexylamine derivatives and their use in the treatment and / or prevention of central nervous system (CNS) disorders, such as depression, anxiety, schizophrenia and sleep disorder as well as methods for their synthesis. The invention also relates to pharmaceutical compositions containing the compounds of the invention, as well as methods of inhibiting reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine from the synaptic cleft and methods of modulating one or more monoamine transporter.

It has been found that the treatment of depression using known serotonin reuptake inhibitors (SRIs) and noradrenaline reuptake inhibitors (NRIs) may be improved by the administration therewith of folic acid or a precursor which produces folate in the patient. The daily dose of NRI or SRI is as prescribed for treatment of depression in the usual way. The daily dose of the folic acid or precursor should be such as to provide a folate dosage of 300-5000 micrograms / day.

Phenyl-substituted cyclohexylamine derivatives and method for their synthesis and characterization are disclosed. Use of these compounds to treat / prevent neurological disorders as well as methods for their synthesis are set forth herein. Exemplary compounds of the invention inhibit reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine (e.g., from the synaptic cleft) and modulate one or more monoamine transporter. Pharmaceutical formulations incorporating compounds of the invention are also provided.

The present invention generally relates to the use of drugs for the treatment of neurobehavioral disorders or symptoms of a neurobehavioral disorder associated with dysfunction of the trimonoamine modulating system (TMMS). More specifically, the invention describes methods for the treatment of a neurobehavioral disorder and / or treatment or prevention of symptoms of a neurobehavioral disorder by administering suitable Isoindole derivatives alone or in combination with other agents so as to provide relatively equal inhibitory effect on serotonin, dopamine and norepinephrine transporters.

The invention relates to a method of treating at least one symptom of a lower urinary tract disorder in a subject in need of treatment wherein the symptom is selected from the group consisting of urinary frequency, urinary urgency, urinary urge incontinence, nocturia and enuresis. The method comprises administering to a subject in need of treatment a therapeutically effective amount of a compound that has 5-HT3 receptor antagonist activity and NorAdrenaline Reuptake Inhibitor (NARI) activity. The invention further relates to a method of treating at least one symptom of a lower urinary tract disorder in a subject in need of treatment wherein the symptom is selected from the group consisting of urinary frequency, urinary urgency, urinary urge incontinence, nocturia and enuresis, comprising coadministering to said subject a first amount of a 5-HT3 antagonist and a second amount of a NARI, wherein the first and second amounts together comprise a therapeutically effective amount or are each present in a therapeutically effective amount.

The invention relates to a method of decreasing intestinal motility in a subject in need of treatment. The method comprises administering to the subject a therapeutically effective amount of a compound that has 5-HT3 receptor antagonist activity and NorAdrenaline Reuptake Inhibitor (NARI) activity. The invention further relates to a method of decreasing intestinal motility in a subject in need thereof, comprising coadministering to said subject a first amount of a 5-HT3 antagonist and a second amount of a NARI, wherein the first and second amounts together comprise a therapeutically effective amount or are each present in a therapeutically effective amount. In addition, the method of the invention comprises administering a NARI alone. In certain embodiments, the subject is a subject with a functional bowel disorder, such as IBS, functional abdominal bloating, or functional diarrhea.

Therapeutic uses of 4-[2-(4-methylphenylsulfanyl)phenyl]piperidine and therapeutically acceptable salts thereof are provided.

The invention relates to the observation that the p38 mitogen-activated protein kinase pathway is an important regulator of biogenic amine transporter (BAT) function. By using modulator of p38 MAPK, one can alter BAT function in a specific manner. This recognition of the pathway and its interaction with the serotonin transporter (SERT) and the norepinephrine transporter (NET), along with the PPA, PKG and PDE pathways, also provides the opportunity to identify polymorphisms that will impact the efficacy of drugs that act though on these enzymes or their pathways.

The invention relates to a method of treating functional bowel disorders in a subject in need of treatment. The method comprises administering to a subject in need of treatment a therapeutically effective amount of a compound that has 5-HT3 receptor antagonist activity and NorAdrenaline Reuptake Inhibitor (NARI) activity. The invention further relates to a method of treating a functional bowel disorder in a subject in need thereof, comprising coadministering to said subject a first amount of a 5-HT3 antagonist and a second amount of a NARI, wherein the first and second amounts together comprise a therapeutically effective amount or are each present in a therapeutically effective amount. In addition, the method of the invention comprises administering a NARI alone. The functional bowel disorders which can be treated according to the method of the invention include IBS, functional abdominal bloating, functional constipation and functional diarrhea.

The present invention provides a method of treating fibromyalgia syndrome (FMS), chronic fatigue syndrome (CFS), and pain in an animal subject comprising administering a therapeutically effective amount of a dual serotonin norepinephrine reuptake inhibitor compound or a pharmaceutically acceptable salt thereof, wherein said dual serotonin norepinephrine reuptake inhibitor compound is characterized by a non-tricyclic structure and a greater inhibition of norepinephrine reuptake than serotonin reuptake, and wherein said compound is not administered adjunctively with phenylalanine or tyrosine. In particular, the use of milnacipran to treat FMS, CFS, and pain is disclosed.

Various compounds, compositions, and methods for binding to β-amyloid plaque and norepinephrine transporters are presented. Especially preferred compounds include those with a PET-detectable label.

Host cells that are engineered to produce benzylisoquinoline alkaloid (BIAs) precursors, such as norcoclaurine (NC) and norlaudanosoline (NL), are provided. The host cells may have one or more engineered modifications selected from: a feedback inhibition alleviating mutation in a enzyme gene; a transcriptional modulation modification of a biosynthetic enzyme gene; an inactivating mutation in an enzyme; and a heterologous coding sequence. Also provided are methods of producing a BIA of interest or a precursor thereof using the host cells and compositions, e.g., kits, systems etc., that find use in methods of the invention.

Host cells that are engineered to produce benzylisoquinoline alkaloid (BIAs) precursors, such as norcodaurine (NC) and norlaudanosoline (NL), are provided. The host cells may have one or more engineered modifications selected from: a feedback inhibition alleviating mutation in a enzyme gene; a transcriptional modulation modification of a biosynthetic enzyme gene; an inactivating mutation in an enzyme; and a heterologous coding sequence. Also provided are methods of producing a BIA of interest or a precursor thereof using the host cells and compositions, e.g., kits, systems etc., that find use in methods of the invention.

The invention discloses new medicinal application of 3,6'-disinapoyl sucrose (DISS), in particular the application of the 3,6'-disinapoyl sucrose (DISS) in preparing a product for treating tristimania. The 3,6'-disinapoyl sucrose (DISS) has better therapeutic effect on treating the tristimania caused by various reasons and obvious anti-depression activity to a pharmacological depression model, and the anti-depression activity of the 3,6'-disinapoyl sucrose is relative to the enhancement of the functions of 5-hydroxytryptamine (5-HT) and noradrenergic (NE) nerves. The DISS has no central excitation or inhibitive action within the range of an effective dosage of anti-depression.

The present invention relates to novel 3-phenyl-azetidine derivatives, useful for modulating extracellular levels of catecholamines, dopamine and norepinephrine, in cerebral cortical areas of the mammalian brain, and more specifically for the treatment of central nervous system disorders. In other aspects the invention relates to pharmaceutical compositions comprising the 3-phenyl-azetidine derivatives of the invention and to the use of these compounds for therapeutic applications.

Provided herein are compounds and prodrugs and methods of preparation of compounds and prodrugs that are capable of functioning as releasers and / or uptake inhibitors of one or more monoamine neurotransmitters, including dopamine, serotonin, and norepinephrine. Also provided are pharmaceutical compositions comprising one or more of these compounds or prodrugs, which may further comprise one or more additional therapeutic agents. Also provided are methods of treatment of various conditions that may be responsive to modification of monoamine neutrotransmitter levels, such as pre-obesity, obesity, addiction, and depression.

The present invention provides a pharmaceutical composition comprising a selective serotonin reuptake inhibitor (SSRI) and a norepinephrine reuptake inhibitor (NRI), particularly, fluoxetine and reboxetine, for treating obesity. Surprisingly, the inventor of the present invention discovered that use of especially low doses of the active compounds, particularly, at most 6 mg / day of reboxetine and at most 20 mg / day of fluoxetine, wherein the reboxetinerfluoxetine ratio is from about 1:4 to about 1:6, induces an effective weight loss in obese patients. Advantageously, the combinations of the present invention include very low doses of the active ingredients, thereby decreasing possible drug-drug interactions and adverse drug reaction.

The present invention relates to new compounds of formula (I): showing great affinity and activity towards the subunit [alpha]2[delta] of voltage-gated calcium channels (VGCC), especially the [alpha]2[delta]-1subunit of voltage-gated calcium channels or dual activity towards subunit [alpha]2[delta] of voltage-gated calcium channels (VGCC), especially the [alpha]2[delta]-1subunit of voltage-gated calcium channels, and the noradrenaline transporter (NET).

The invention discloses a preparation method and application of a nano enzyme for colorimetric detection of glucose. The preparation method comprises the following steps that HAuCl4, Na2PdCl4 and noradrenaline are : uniformly dispersed in an ethanol solution to obtain a mixed solution; NaBH4 is added into the mixed solution under the stirring condition, reduction is conducted under the water bath condition, then centrifugation, washing and freeze drying are conducted, and the AuPd-NE nano-enzyme is obtained. On the basis, a novel method for detecting the content of glucose in human serum is established by utilizing the catalytic performance of the nano enzyme. Under the optimal condition, the detection range of the method for detecting the glucose is 30-250 muM, and the detection limit is 10 muM. The synthesis method is simple, the selectivity is high, the detection limit is low, and sensitive detection of glucose is realized.

The present invention relates to new compounds of formula (I):showing great affinity and activity towards the subunit α2δ of voltage-gated calcium channels (VGCC), especially the α2δ-1 subunit of voltage-gated calcium channels or dual activity towards the subunit α2δ of voltage-gated calcium channels (VGCC), especially the α2δ-1 subunit of voltage-gated calcium channels, and the noradrenaline transporter (NET).

New compounds that bind to monoamine transporters are described. The compounds of the present invention can be racemic or pure R— or S-enantiomers. Certain preferred compounds of the present invention have a high selectively dopamine transporter versus the serotonin transporter. Preferred monoamine transporters for the practice of the present invention include the dopamine transporter, the serotonin transporter and the norepinephrine transporter.

New tropane analogs that bind to monoamine transporters are described, particularly, 8-aza, 8carbo and 8-oxo tropanes having 6- or 7-hydroxyl or ketone substituents. The compounds of the present invention can be racemic, pure R-enantiomers, or pure S-enantiomers. Certain preferred compounds of the present invention have a high selectivity for the DAT versus the SERT. Also described are pharmaceutical therapeutic compositions comprising the compounds formulated in a pharmaceutically acceptable carrier and a method for inhibiting 5-hydroxy-tryptamine reuptake of a monoamine transporter by contacting the monoamine transporter with a 5-hydroxytryptamine reuptake inhibiting amount of a compound of the present invention. Preferred monoamine transporters for the practice of the present invention include the dopamine transporter, the serotonin transporter and the norepinephrine transporter.

Disclosed are a neuralgia treating medicine composition and application thereof. The neuralgia treating medicine composition is composed of amitriptyline hydrochloride and ZL006 methyl ester at a weight ratio of 1: (3-6). Amitriptyline hydrochloride can block nervous centralis from reuptaking of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) as well as receptor antagonism and sodium channel retardation of N methyl D aspartate (NMDA); ZL006 methyl ester can decouple PSD95-nNOS to avoid generation of too much NO; when applied in an appropriate proportion, amitriptyline hydrochloride and ZL006 methyl ester can achieve enhancement or synergistic effects and accordingly improve the use effects. Under the premise of gaining equal therapeutic effects, the risk of adverse effects can be reduced due to application concentration reduction of amitriptyline hydrochloride.

The present invention relates to (1S,6R)-6-(3,4-dichlorophenyl)-1-[(methyloxy)methyl]-3-azabicyclo[4.1.0]heptane, pharmaceutically acceptable salts, prodrugs or solvates thereof; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as serotonin (5-HT), dopamine (DA) and norepinephrine (NE), re-uptake inhibitors.

The invention discloses an application of the double inhibitor of dopamine transporter (DAT) and norepinephrine transporter in the preparation of medicines for treating central nervous degenerative disease and also discloses a medicine combination of the double inhibitor of dopamine transporter (DAT) and norepinephrine transporter. The invention firstly proposes and proves that the double inhibitor of dopamine transporter (DAT) and norepinephrine transporter can protect dopaminergic neuron and provides a new choice for clinical treatment of the central nervous degenerative disease.