12 results about "Amine receptor" patented technology

[Problem] To provide a substance having an activity of antagonizing the binding of histamine to histamine-H3 receptor, or having an activity of inhibiting the homeostatic activity of histamine-H3 receptor. [Means for Solution] A compound of the following formula (I) is provided: [wherein X, Y, Z and W each independently represent a methine group optionally having 1 or 2 substituents, or a nitrogen atom (provided that a case where all of X, Y, Z and W are an optionallysubstituted methine group); A, B and D represent C(0)-, etc.; Q represents a methine group or a nitrogen atom; R represents an optionallysubstituted group of the following formula (II-1): (wherein R7 and R8 each independently represent a lower alkyl group, etc.)].

The present disclosure aims to provide an exercise effect-mimicking agent capable of producing effects similar to those of exercise without actually exercising. An exercise effect-mimicking agent containing at least one compound selected from the group consisting of (A) an α-adrenergic antagonist, (B) a flavonoid, (C) a dopamine D2 receptor antagonist, and (D) an NF-κB signaling pathway inhibitor.

The invention belongs to the technical field of pharmaceutical chemicals, and provides a dopamine D3 receptor radioactive tracer and a preparation method and application thereof. According to the dopamine D3 receptor radiotracer (11C-YQA14) disclosed by the invention, a structure as shown in a formula 1 is used as a precursor compound, and gaseous 11C-CH3I is introduced under a closed condition to obtain the 11C-YQA14. The dopamine D3 receptor radioactive tracer has ideal affinity to a dopamine D3 receptor and has low affinity to a dopamine D2 receptor, so that the dopamine D3 receptor radioactive tracer can selectively recognize the dopamine D3 receptor and has low recognizability to the dopamine D2 receptor.

This invention provides a method for treating postoperative nausea and vomiting using buccal acupuncture combined with a triple antiemetic regimen. The method employs a combined intervention of buccal acupuncture and a triple antiemetic regimen. The triple regimen consists of a 5-HT3 receptor antagonist, a glucocorticoid, and a dopamine receptor antagonist, administered intravenously in two separate doses. The buccal acupuncture uses CA-2 (upper jiao), CA-3 (middle jiao), and CA-4 (lower jiao) as core acupoints, with auxiliary and reinforcing acupoints added based on the surgical site and high-risk groups. A standardized procedure of pecking stimulation is applied, along with a corresponding postoperative remedial antiemetic medication regimen. This invention organically combines multi-target drug blockade with buccal acupuncture's visceral regulation, synergistically enhancing the antiemetic effect, reducing the incidence of nausea and vomiting, and decreasing the need for remedial medication. The regimen is highly standardized, widely adaptable, and can meet the postoperative nausea and vomiting control needs of various surgeries and high-risk groups. It exhibits good safety, strong repeatability, and high clinical application value.

The invention relates to the technical field of biological medicine, in particular to application of vanillyl alcohol in preparation of a dopamine receptor D2 antagonist, and the application proves that the vanillyl alcohol can be specifically combined with a D2 receptor with micromole-level affinity through micro-thermophoresis and biological layer interference technologies. Cell experiments show that vanillyl alcohol can antagonize D2 receptor mediated ERK signal pathway activation in a concentration-dependent manner, and has no agonist activity. In a PCPA-induced insomnia mouse model, vanillyl alcohol can shorten the sleep latency and prolong the total sleep time in a dose-dependent manner. After a D2 receptor is knocked down in nucleus septum, the sleep promoting effect of vanillyl alcohol disappears, and it is confirmed that the drug effect of vanillyl alcohol has target dependence. As a low-toxicity natural small molecule, vanillyl alcohol provides a new choice for developing a novel insomnia treatment medicine.

The application provides a compound with histamine H3 receptor protein degradation activity and a preparation method and application thereof, and belongs to the field of medicines. The application provides a compound shown in formula I, the compound has obvious degradation effect on HRH3 protein, the compound can be used for preparing a histamine H3 receptor degrading agent, and is used for treating diseases related to the activity of HRH3 protein. The application further proves through experiments that the compound has the effects of significantly improving cognition, learning and memory and attention, and has a wide application prospect. A-L-B formula I.

An orally disintegrating pharmaceutical tablet comprising: between 0.1 and 21 wt % of cariprazine or its pharmaceutically acceptable salts, between 0.1 and 15 wt % of a disintegrant, between 0.1 and 5 wt % of colloidal silicon dioxide, between 0.1 and 10 wt % of a taste masking agent, between 0.1 and 5 wt % of a lubricant, and up to 100 wt % of a diluent, the percentage being expressed with regard to the total weight of the pharmaceutical tablet. Said composition for use in the treatment and / or prevention of pathological conditions which require the modulation of dopamine receptors, selected from the group of psychoses, drug abuse, cognitive impairment accompanying schizophrenia, mild-to-moderate cognitive deficits, dementia, psychotic states associated with dementia, eating disorders, attention deficit disorders, hyperactivity disorders in children, psychotic depression, bipolar disorder, paranoid and delusional disorders, dyskinetic disorders, anxiety, sexual dysfunction, sleep disorders, emesis, aggression and autism.

The present disclosure relates to a pharmaceutical composition for preventing or treating a brain disease, comprising a stem cell-derived exosome surface-modified with a compound capable of binding to dopamine receptors or L-amino acid transporters as an active ingredient. The stem cell-derived exosome according to the present disclosure selectively binds to dopamine receptors (D2) overexpressed as autoreceptors in dopaminergic neurons in the substantia nigra through surface modification. Thereby, local accumulation in dopaminergic neurons is possible. In addition, it was identified that the stem cell-derived exosome exhibited an excellent neuron protective effect and neuron death inhibitory effect. Accordingly, the surface-modified stem cell-derived exosome according to the present disclosure is expected to be usefully used as a composition for preventing or treating a brain disease including Parkinson's disease and Alzheimer's disease.

This disclosure presents an advanced oral cannabinoid formulation in drop form for fast-acting relief of multiple sclerosis (MS), utilizing absorption through the oral mucosa to enhance bioavailability. The formulation includes cannabinoids like CBD, CBG, and THC, combined with Hericium erinaceus extract and Vitamin D to boost therapeutic efficacy. It targets various MS subtypes, including relapsing-remitting (RRMS), secondary progressive (SPMS), primary progressive (PPMS), and progressive-relapsing (PRMS), addressing symptoms such as fatigue, motor issues, spasticity, cognitive impairments, and mood disorders. The cannabinoids activate CB1 and CB2 receptors, reducing excitatory signaling, muscle spasticity, and neuroinflammation. CBD and CBG further enhance neuroprotection by modulating dopamine receptor expression and uptake, promoting synaptic health. Hericium erinaceus and Vitamin D complement these effects, reducing neural and immune damage and improving mental well-being, providing a comprehensive therapeutic strategy for managing MS.

The present invention relates to the use of a combination of two or more of a D2 agonist, an adenosine A2A receptor antagonist, a histamine H3 antagonist or inverse agonist, a mGluR5 receptor antagonist, or a nicotinic α4-β2 and / or α7 receptor agonist to increase D2 dopaminergic molecular signaling in the striatum for the treatment of psychiatric or neurological disorders in which anhedonia or motivation-related dysfunction exists (such as major depressive disorder, bipolar I or II disorder, post-traumatic stress disorder, addiction, anhedonia or motivation-related aspects of schizophrenia (e.g. negative symptoms) and Parkinson's disease (e.g. non-motor features such as depression and apathy)).

The invention relates to particular substituted deuterated heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and / or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) and / or pathways involving dopamine D1 / D2 receptor signaling systems, and / or the treatment of residual symptoms.