179 results about "D2 dopamine receptors" patented technology

A method for administration of a substance into the dermis of a mammal is disclosed. The method involves administration into the dermis by injection which results in improved systemic absorption relative to that obtained upon subcutaneous administration of the substance. The substance administered may be a growth hormone, a low molecular weight heparin or a dopamine receptor agonist.

Methods and compositions are provided for diagnosing and treating pathological conditions related to a dopamine receptor abnormality. The methods comprise administering to a patient having such a pathological condition a plasmid encoding an oligonucleotide, antisense to one or more RNA molecules encoding one of the several dopamine receptors, thereby selectively controlling expression of one or more dopamine receptor subtypes, and alleviating the pathological conditions related to their expression. The vectors are targeted to specific regions of the brain via complexation with antibody studded liposomes.

A composition for intranasal administration comprising a full or partial D1-agonist of the dopamine receptor.

The invention relates to a long acting sustained-release formulation containing dopamine-receptor stimulant medicine, which comprises 5-5- wt% of effective dose of dopaminergic acceptor medicaments, and 50-95 wt% of medicinal macromolecular auxiliary materials.

An orally deliverable pharmaceutical composition comprises a therapeutically effective amount of pramipexole or a pharmaceutically acceptable salt thereof and at least one pharmaceutically acceptable excipient, said composition exhibiting at least one of (a) an in vitro release profile wherein on average no more than about 20% of the pramipexole is dissolved within 2 hours after placement of the composition in a standard dissolution test; and (b) an in vivo pramipexole absorption profile following single dose administration to healthy adult humans wherein the time to reach a mean of 20% absorption is greater than about 2 hours and/or the time to reach a mean of 40% absorption is greater than about 4 hours. The composition is useful for oral administration, not more than once daily, to a subject having a condition or disorder for which a dopamine receptor agonist is indicated.

Provided is a method of treating or preventing age-related macular degeneration (AMD) in a patient subject to, or symptomatic of the disease, wherein the method comprises restoring normal lysosomal pH (pH_L), or acidifying an abnormally elevated pH_L, thus decreasing or preventing a damaging accumulation of lipofuscin or waste products in the retinal pigment epithelium (RPE) cells of the eye of the patient. Further, this method is achieved by elevating cAMP by administering or stimulating receptors coupled to a Gs protein in an amount sufficient to decrease the elevated pH_L or restore acidity of said lysosomes, specifically by administering or stimulating receptors comprising D1-like dopamine receptors by the use of D1-like dopamine receptor agonists. Methods for selecting and quantifying the effectiveness of drugs to restore pH_L and determine outer segment clearance rates is also provided using a high through-put screening protocol.

The side effect of decrease in body weight caused by the alkylphosphocholines such as miltefosine can be antagonized by certain acetylcholine receptor antagonists such as domperidone and pimozide. The combination of alkylphosphocholine plus the antagonist does not have any effect on the anti-tumor action of the alkylphosphocholine. The combination also caused no new side effects in the animals.

Disclosed herein is the use of N-desmethylclozapine (NDMC) and related compounds to treat a variety of neuropsychiatric diseases including psychosis. It is shown that NDMC and related compounds are agonists or partial agonists at D2 and D3 dopamine receptors and thus may be effective as a dopamine stabilizing agent, allowing it to be used to treat or provide reduced incidence of Extrapyramidal symptoms (EPS) and/or tardive dyskinesias (TD). Also disclosed is administering NDMC and related compounds in combination with other anti-psychotic agents.

The present invention provides, inter alia, compositions containing enantiomerically pure (R)(+)-amisulpride or enantiomerically pure (R)(+)-sulpiride, optionally with dopamine receptor modulators. The present invention also provides compositions containing racemic (RS)-amisulpride or (RS)-sulpiride in combination with dopamine receptor modulators. Methods for preventing, treating, or ameliorating the effects of a metabolic disorder or key element thereof, for modulating blood glucose levels, and for preventing, treating, or ameliorating the effects of diabetes in a subject are also provided. Additionally, the present invention provides methods for counter-acting the dopamine antagonist activity of (S)-amisulpride in racemic (RS)-amisulpride, or the dopamine antagonist activity of (S)-sulpiride in racemic (RS)-sulpiride, administered to a subject to prevent, treat, or ameliorate the effects of a metabolic disorder.

The present invention is concerned with deuterium-enriched pyrimidine compounds of formula I, their derivatives, enantiomers, diastereomers, solvates and pharmaceutical salts thereof,

and their uses in the treatment, prevention and modulation of various diseases including chronic liver diseases, liver cirrhosis, liver fibrosis, hepatocellular carcinoma, liver cancer, renal cell carcinoma, kidney cancer, colorectal cancer, brain cancer, breast cancer, blood cancer, lung cancer, thyroid cancer, ovarian cancer, pancreas cancer, prostate cancer, stomach cancer, testicular cancer, uterus cancer, intestinal cancer, skin cancer, and other forms of cancer, carcinoid tumors, teratocarcinoma, tumor progression, metastasis and fibrosis in the neuroendocrine neoplasia, fibrotic processes as well as a disease state modulated directly or indirectly with 5-HT receptors, 5-HT₁, 5-HT_1A, 5-HT₂ receptors, 5-HT_2A and 5-HT_2B receptors, dopamine receptors and multiple kinase pathways.

The present invention relates to the treatment of dopamine-related dysfunction using full D₁ dopamine receptor agonists in an intermittent dosing protocol with a short, but essential, “off-period.” The D₁ agonist concentration is reduced during the “off-period” to obtain a plasma concentration of agonist that suboptimally activates D₁ dopamine receptors for a period of time to prevent induction of tolerance. Specifically, the method comprises the steps of periodically administering to a patient a full D₁ agonist with a half-life of up to about 6 hours at a dose resulting in a first plasma concentration of agonist capable of activating D₁ dopamine receptors to produce a therapeutic effect. The dose is reduced at least once every 24 hours to obtain a second lower plasma concentration of agonist that results in suboptimal activation of D₁ dopamine receptors for a period of time sufficient to prevent induction of tolerance.

A sustained-release pharmaceutical composition in a form of an orally deliverable tablet comprises as active pharmaceutical agent a compound of formula

or a pharmaceutically acceptable salt thereof, wherein R¹, R² and R³ are the same or different and are H, C_1-6 alkyl (optionally phenyl substituted), C_3-5 alkenyl or alkynyl or C_3-10 cycloalkyl, or where R³ is as above and R¹ and R² are cyclized with the attached N atom to form pyrrolidinyl, piperidinyl, morpholinyl, 4-methylpiperazinyl or imidazolyl groups; X is H, F, Cl, Br, I, OH, C_1-6 alkyl or alkoxy, CN, carboxamide, carboxyl or (C_1-6 alkyl)carbonyl; A is CH, CH₂, CHF, CHCl, CHBr, CHI, CHCH₃, C═O, C═S, CSCH₃, C═NH, CNH₂, CNHCH₃, CNHCOOCH₃, CNHCN, SO₂ or N; B is CH, CH₂, CHF, CHCl, CHBr, CHI, C═O, N, NH or NCH₃, and n is 0 or 1; and D is CH, CH₂, CHF, CHCl, CHBr, CHI, C═O, O, N, NH or NCH₃. The agent is. dispersed in a matrix comprising a hydrophilic polymer and a starch having a tensile strength of at least about 0.15 kN cm⁻² at a solid fraction representative of the tablet. The composition exhibits sustained-release properties effective for treatment of Parkinson's disease. The tablet is optionally coated. Tablets of the invention have improved resistance to attrition or erosion during manufacture, packaging and handling.

The invention belongs to the field of pharmacy, and relates to a multi-purpose targeting molecule, and applications of a compound and a drug delivery system modified by the multi-purpose targeting molecule in brain tumor diagnosis and treatment. According to the invention, the multi-purpose targeting molecule RGD-pHA being compatible to brain capillary endothelial cells and crossing the blood-brain barrier, being highly compatible to integrin and crossing the blood-brain tumor barrier, and targeting to the brain tumor cells is prepared by adopting a molecule splicing method; the invention further relates to preparation of fluorescein and a medicine modified by RGD-pHA, and a macromolecular carrier material, and applications of RGD-pHA in construction of the drug delivery system. The experimental result shows that the RGD-pHA can be specifically taken by brain capillary endothelial cells expressing the dopamine receptor for mediating the model drug or the nanometer drug delivery system to enter the brain, so that the model drug or the nanometer drug delivery system is specifically taken by the positive cells and the tumor sphere tissue expressing the integrin, the good brain tumor targeting effect is shown in vitro and vivo, and the efficiency in resisting brain tumor is obviously improved.

The present invention relates to methods of treating various CNS disorders, e.g., mania, bipolar disorder and schizophrenia, by administering NMDA receptor antagonists, alone or in combination with dopamine receptor antagonists.

Described herein are antipyschotic compounds of formula (I) wherein, A is an optionally benzo-fused five or six member aromatic ring having zero to three hetero atoms independently selected from N, O, and S; Alk is (C_1-4) alkylene optionally substituted with OH, methoxy, ethoxy, or F; Ar is optionally substituted phenyl, naphthyl, monocyclic heteroaromatic, or bicyclic heteroaromatic; R¹ is hydrogen or (C_1-4) alkyl optionally substituted with OH, OR³, or OCH₂CH₂OH, wherein R³ is (C_1-2) alkyl; R² is H, (C_1-6) alkyl, halogen, fluorinated (C_1-6) alkyl, OR⁴, SR⁴, NO₂, CN, COR⁴, CONR⁵R⁶, SO₂NR⁵R⁶, NR⁵R⁶, NR⁵COR⁴, NR⁵SO₂R⁴, or optionally substituted phenyl, wherein R⁴ is hydrogen, (C_1-6) alkyl, fluorinated (C_1-6) alkyl, benzyl, or optionally substituted phenyl, R⁵ and R⁶ are independently hydrogen, (C_1-6) alkyl, or optionally substituted phenyl; Z is one or two substituents independently selected from hydrogen, halogen, (C_1-6) alkyl, fluorinated (C_1-6) alkyl, OR⁷, SR⁷, NO₂, CN, COR⁷, CONR⁸R⁹, SO₂NR⁸R⁹, NR⁸SO₂R⁷, NR⁸R⁹, or optionally substituted phenyl, wherein R⁷ is hydrogen, (C_1-6) alkyl, fluorinated alkyl, benzyl, or optionally substituted phenyl, R⁸ and R⁹ are independently hydrogen, (C_1-6) alkyl, or optionally substituted phenyl; and salts, solvates, and crystal forms thereof. Also described are the use of the compounds of formula (a) as antagonists of the dopamine D₂ receptor and as agents for the treatment of psychosis and bipolar disorders, and pharmaceutical formulations of the compounds of formula (I). Also described are compounds useful as intermediates for the synthesis of the compounds of formula (I).

The present invention relates to combination of one or more SGLT2 inhibitors or pharmaceutically acceptable forms and/or salts thereof and one or more dopamine receptor agonists or pharmaceutically acceptable forms and/or salts thereof, preferably in the treatment and/or prevention of a metabolic disorder of an equine animal, wherein more preferably the metabolic disorder is one or more disorders selected from Equine Metabolic Syndrome (EMS), Equine Pituitary Pars Intermedia Dysfunction (PPID), also known as equine Cushing's syndrome, laminitis, vascular dysfunction, hypertension, hepatic lipidosis, hyperadreeocorticism, glucose intolerance, insulin resistance, hyperinsulinaemia, hirsutism, hyperhidrosis. polyuria, polydipsia, chronic infections, abnormal fat distribution, muscle wasting, abnormal weight loss and/or loss of appetite.

Pharmaceutical composite compositions comprising tetrahydroindolones linked to arylpiperazines and derivatives thereof are disclosed. Specifically, composite compositions useful in treating anti-psychotic disorders are disclosed. The composite compositions disclosed herein can effectively ameliorate symptoms and treat psychotic disorders without causing a decrease in cognitive function. Generally, the composite compounds consist of two moieties, moiety A and B in which a tetrahydroindolone comprises a moiety A linked through a linker L to a moiety B, where B is an arylpiperazinyl moiety. The composite compound provides anti-psychotic actively by interaction with GABA, seratoninne and dopamine receptors. The composite molecules with the combined activities will provide treat psychiatric and neurological diseases without cognitive impairment.