37 results about "Dopamine receptor antagonist" patented technology

The present invention provides novel compositions comprising a combination of a 5-HT₃ receptor antagonist and a selective dopamine D₂ receptor antagonist for the treatment of obsessive, impulsive and compulsive behavioral activities and other dopamine pathway-associated disorders or conditions. Preferably, the pharmaceutical compositions of the present invention comprise amounts of the 5-HT₃ receptor antagonist ondansetron and a selective dopamine D₂ receptor antagonist, such as risperidone or olanzapine, that are sufficient to control a subjects obsessive, impulsive and compulsive behavioral activities. Kits comprising the combination of antagonists for the treatment of addictive disorders such as alcohol dependence are also provided.

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.

The present invention provides a domperiodone oral disitegrant tablet preparation. Its composition includes medicine active component, filling agent, corrective, disitegrant, lubricating agent and glidant. Its medicin active component includes dopamine receptor antagonist and gastroprokinetic, and its disitegrant agent is selected from cross-linked polyvinylpyrrolidone, carboxymethyl starch sodium and microcrystal cellulose or their mixture, and corrective is selected from aspartame. Said invention adopts direct addition of disitegrant in theprescription so as to attain the effect of quick disitegration. Its preparation process is simple, and it is convenient for taking in.

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 disclosure provides compounds having formula (I), wherein the substituents are as defined herein. The compounds are useful for modulating the dopamine D₃ receptor and for treating conditions associated therewith, such as addictions, drug dependency, and psychiatric conditions.

The present invention provides a therapeutic solution for effective control of symptoms related to nausea and vomiting. The therapeutic solution is a pharmaceutical composition which combines anti-emetics of different classes. These classes include dopamine receptor antagonists, serotonin receptor antagonists, butyrphenones, and neurokinin receptor antagonists. The combination of different anti-emetics mitigates adverse affects of a single anti-emetic alone while increasing drug efficacy and decreasing cost of administration to the individual patient.

Haloperidol analogs that conforms to the structural formulae:

wherein:

• • • R is H, or —(CH₂)_n—OH, n is an integer from 0 to 2, and
    • A is a heterocyclic bridging group, consisting essentially of carbon and at least one nitrogen atom, which effectively maintains the distance between the moieties connected thereby such that the compound (1) is incapable of metabolizing to BCPP⁺ like species, (2) has an affinity for the D2 receptor subtype of 15<D2<250 and (3) functions as a dopamine receptor antagonist, or the structural formulae:

wherein:

R₁ is H, or —(CH₂)_n—OH, n is an integer from 0 to 2,

• B is an aza- or diaza-bicyclo group, which effectively maintains the distance between the moieties connected thereby such that the compound is incapable of metabolizing to BCPP⁺ like species; and Z is —CH— or N; and pharmaceutically acceptable salts, esters, derivatives, metal complexes, conjugates and prodrugs thereof.

The present invention provides compounds, which, are novel antagonists for D₁ receptors as well as methods for preparing such compounds. In another embodiment, the invention provides pharmaceutical compositions comprising such D₁ receptor antagonists as well as methods of using them to treat CNS disorders, obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.

Belonging to the field of pharmaceutical chemistry, the invention relates to a benzoazepine compound, a preparation method and application thereof, in particular to the benzoazepine compound, its preparation method and application in the field of treatment of nervous system diseases, especially application in the field of drug addiction related to dopamine D1 and D3 receptors. The benzoazepine compound and pharmacologically acceptable inorganic or organic salts thereof have a structure shown as formula (I). Results of drug experiments carried out by the invention show that the benzoazepine compound and its pharmacologically acceptable inorganic or organic salts have high antagonistic activity on dopamine D1 and D3, can be used as drug leads for further development of dopamine receptor antagonists with good selectivity and high activity, and can be used as potential drugs for treatment of drug addiction by dopamine D1, D3 receptor antagonists. (formula (I)).

This invention pertains to the discovery that a dopamine receptor agonist can activate PKA signaling and/or can act synergistically with an adenosine receptor to activate such signaling. In various embodiments, this invention exploits the synergy between the dopamine receptor pathway and an adenosine receptor pathway to provide methods of mitigating one or more symptoms produced by the chronic consumption of a substance of abuse or to mitigate one or more physiological and/or behavioral symptoms associated with cessation of chronic consumption of a substance of abuse. In certain embodiments, the methods involve administering to the mammal an effective amount of an adenosine receptor antagonist; and an effective amount of a dopamine receptor antagonist; where the effective amount of the adenosine receptor antagonist is lower than the effective amount of an adenosine receptor antagonist administered without said dopamine receptor antagonist.

The invention belongs to the technical field of biomedicine and particularly relates to a novel pharmaceutical use of a dopamine receptor 1 antagonist, and to a novel use of the dopamine receptor 1 antagonist in preparing drugs for the treatment of ketamine-induced schizoid symptoms in mice. The dopamine receptor 1 antagonist is selected from SCH23390 having a molecular formula of C17H18ClNO.HCl,and is one or only one effective ingredient to the drugs. A drug for the treatment of ketamine-induced schizoid symptoms in mice comprises the dopamine receptor 1 antagonist having the effective amount (5 mg/kg). The dopamine receptor 1 antagonist is used as one means to treat ketamine-induced schizoid behaviors of mice, and scientific basis is provided for the research and development of a methodto effectively relieve schizoid symptoms in mice.

The present invention provides a combination medicine for treatment of depression, comprising a combination of (A1) an antidepressant and either (B1) a dopamine D1 receptor agonist or (C1) a dopamine D1 receptor antagonist; and a method for screening for an antidepressant that in combination with a dopamine D1 receptor agonist provides an improvement in treatment of depression, the method comprising the steps of: administering, to a mammal, (A2) a compound having an antidepressant action and (B1) a dopamine D1 receptor agonist, and detecting a greater increase in depression-related gene expression, dopamine D1 receptor expression and/or dopamine D1 receptor signaling in comparison with the case where (A2) the compound having an antidepressant action or (B1) the dopamine D1 receptor agonist is administered.

The invention discloses an application of a dopamine receptor antagonist chlorprothixene in treatment of acute myeloid leukemia, develops a new application of the dopamine receptor antagonist chlorprothixene as a drug, also provides a new way for treating acute myeloid leukemia, and uses the action mechanism between different fusion proteins and the existing APL theoretical model as support. Related in-vitro cell experiments and in-vivo animal experiments prove that: the chlorprothixene can induce cell apoptosis and autophagy pathways to promote death of AML cells, and can induce the decreaseof the expression quantity of fusion proteins PML-RARA and AML1-ETO, so that the chlorprothixene is a potential drug for inducing AML cell death, and provides a new visual angle for exploring alternative strategies of various AML subtype treatments.

Methods for treating a patient having neurological, psychotic, and psychiatric disorders are described comprising the steps of administering to the patient an effective amount of a partial and/or full dopamine D₁ receptor agonist, and administering to the patient an effective amount of a dopamine D₂ receptor antagonist. Pharmaceutical compositions comprising a dopamine D₁ receptor agonist and a dopamine D₂ receptor antagonist are also described. The D₁ dopamine receptor agonist and the D₂ dopamine receptor antagonist can be administered to the patient in the same or in a different composition or compositions.

The invention provides a dopamine D1 receptor antagonist and an application thereof, and relates to the field of medicinal chemistry. The invention relates to the field of medicine, in particular to adopamine D1 receptor antagonist shown in a structural formula (I), pharmaceutically acceptable salt of the dopamine D1 receptor antagonist, a pharmaceutical composition containing the dopamine D1 receptor antagonist, and an application of a compound medicine to preparation of medicines for treating or preventing related diseases or symptoms caused by high expression or over-high activity of a dopamine D1 receptor.

The invention discloses a dopamine receptor antagonist and an application thereof. The dopamine receptor antagonist includes 2,9,10-trimethoxy-6,8,13,13a-tetrahydro-5H-isoquinolino[2,1-b]isoquinolin-3-ol and a pharmaceutically acceptable salt or precursor compound. The dopamine receptor antagonist can antagonize a calcium influx caused by activation of a dopamine receptor, widen the application range of analgesia for a ligand of the dopamine receptor, and find a novel idea for development of a novel drug. Animal experiments provided by the invention prove that the 2,9,10-trimethoxy-6,8,13,13a-tetrahydro-5H-isoquinolino[2,1-b]isoquinolin-3-ol has a good analgesic effect on acute pain, inflammatory pain and bone cancer pain as the dopamine receptor antagonist.

The disclosure is directed to novel dopamine D3 receptor antagonists, processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, including treating drug dependency and psychosis.