27 results about "Dopamine receptor" patented technology

The present invention relates to novel dopamine D2 receptor ligands. The invention further relates to functionally-biased dopamine D2 receptor ligands and the use of these compounds for treating or preventing central nervous system and systemic disorders associated with dysregulation of dopaminergic activity.

The present application relates to azapeptide compounds of formula (I) derived from melanocyte-stimulating hormone release-inhibiting factor-1. A method to obtain compounds of formula (I) is also described herein. The compounds of formula (I) have been shown to be suitable for the treatment of dopamine-related disorders of the central nervous system. These compounds showed enhanced potency as positive allosteric modulators of the dopamine D2 receptors in comparison with the melanocyte-stimulating hormone release- inhibiting factor-1 and, in general, do not exhibit meaningful cytotoxicity.

The present disclosure generally relates to binding agents that are capable of targeting tumor cells and immune cells. The binding agents of the present disclosure are multispecific and comprise antigen binding domains that are capable of binding to Dopamine Receptor D2 (DR2), to Programmed Cell Death Protein 1 (PD-1) and / or to Cluster of Differentiation 47 (CD47). The multispecific binding agents of the present disclosure may be used to treat subjects in need thereof.

Disclosed in the present invention are an aza-ergoline derivative, a pharmaceutical composition thereof and the use thereof. Provided in the present invention is a compound as shown in formula I, a pharmaceutically acceptable salt thereof, a solvate thereof, or a solvate of the pharmaceutically acceptable salt thereof. The compound of the present invention has good affinity and agonistic activity to dopamine receptor D2 or D3.

The invention relates to a targeted dopamine D3 receptor molecular probe as well as a preparation method and application thereof, 7-methoxy-2-(N-propyl) amino tetrahydronaphthalene is taken as a raw material, acylation, deprotection, substitution and hydroxyl protection reaction are carried out, then a precursor is marked by utilizing a nucleophilic substitution reaction of < 18 > F, and a drug [< 18 > F] standard substance of a dopamine D3 receptor is obtained. The drug has good in-vitro stability, low radioactive uptake in skull, stability of more than 90% after incubation in normal saline for 5 h, good in-vivo stability, and negligible defluorination [< 18 > F] effect; the antibody has specific binding to a dopamine D3 receptor at an animal level; the logP value is 1.97, and the dopamine D3 can penetrate through a blood brain barrier to enter the brain, so that a dopamine D3 receptor in the brain is subjected to tracing imaging, and the imaging effect is good. The molecular probe targeting the dopamine D3 receptor has a great prospect in clinical application of diagnosis, treatment and curative effect monitoring of diseases related to the dopamine D3 receptor.

The invention relates to the technical field of fluorescent molecular materials for biological imaging, in particular to an N-phenylpiperazine fluorescent probe molecule as well as a preparation method and application thereof. The probe molecule is a fluorescent ligand receptor combined type fluorescent sensor, takes N-(2-methoxyphenyl) piperazine as a targeting group and 4-dimethylamino-1, 8-naphthalimide as a fluorescent reporter group, has specific recognition capability on a dopamine D3 receptor, and is excellent in fluorescence performance, low in cytotoxicity, fast in cell uptake (10s) and remarkable in fluorescence enhancement; the method can be used for cell imaging of mouse hippocampal nerve HT-22 cells, achieves the purpose of visualization, and has potential development value and good application prospects. The fluorescent probe is short in synthesis route, simple and easy to operate and suitable for industrial popularization and application.

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.

Disclosed are novel C4-carboxylic acid-substituted tryptamine derivative compounds and pharmaceutical and recreational drug formulations containing the same. The pharmaceutical formulations may be used to treat brain neurological disorders through the modulation of various receptors, such as 5-HT1A receptor, a 5-HT2A receptor, a 5-HT1B receptor, a 5-HT2B receptor, a 5-HT3A receptor, an ADRA1 A receptor, an ADRA2A receptor, CHRM1 receptor, a CHRM2 receptor, a CNR1 receptor, a DRD1 receptor, a DRD2S receptor, or an OPRD1 receptor.

The invention belongs to the technical field of neurobiology, and particularly relates to application of a dopamine D2 receptor G protein antagonist in preparation of a drug for treating drug addiction. Researches show that the dopamine D2 receptor G protein antagonist can inhibit recurrence after drug addiction fading induced by ignition of small-dose drugs. A mouse cocaine self-administration addiction model is adopted, a small dose of cocaine is given after model mice are subjected to regression training, and the recurrence behavior of the mouse cocaine addiction after regression is induced. A signal channel dependent on dopamine D2 receptor downstream G protein is inhibited before addiction recurrence is induced by a small dose of cocaine, and recurrence after drug-induced cocaine fading can be inhibited; however, the signal pathway for inhibiting the dependence of beta-arretin on the downstream of the dopamine D2 receptor cannot inhibit the recurrence after drug-induced cocaine fading. The invention discloses the effect of the G protein biased antagonist of the dopamine D2 receptor in treatment of drug addiction, and provides a new thought and a drug intervention target for treatment of drug addiction of cocaine and the like.

The present invention belongs to the field of pharmaceutical chemistry. Specifically disclosed are a N-substituted quinolinone compound, a preparation method therefor and pharmaceutical use thereof. The compound of the present invention has a structure represented by formula (I), has excellent oil solubility, has a multi-target effect on the 5-HT2A receptor, the dopamine D2 / 3 receptor, the 5-HT1A receptor and the 5-HT transporter, helps adjust the balance of intracerebral neurotransmitters, has relatively good efficacy on various diseases of the central nervous system, has few toxic and side effects, is very safe and tolerable, has good general druggability, and has good clinical application prospects.

This invention relates to the application of a melanin-catalase nanocomposite (MAC) targeting intestinal mucosal neutrophils in the preparation of drugs for treating inflammatory bowel disease, belonging to the field of novel applications of nanomedicine. It addresses the challenges of catalase oral delivery being easily degraded and inactivated by gastrointestinal proteases and difficult to precisely target neutrophils. This invention is the first to discover a MAC prepared by in-situ polymerization of dopamine on the surface of catalase, which can be used for the treatment of inflammatory bowel disease. This nanocomposite, through oral delivery, precisely targets intestinal mucosal infiltrating neutrophils and maintains structural stability in the gastrointestinal fluid environment, effectively protecting catalase activity. It actively targets intestinal mucosal infiltrating neutrophils through the high affinity of melanin for dopamine D2 receptors, synergistically exerting a triple effect of hydrogen peroxide decomposition, hypochlorous acid scavenging, and iron ion chelation, effectively inhibiting the formation of extracellular traps in neutrophils.

A pharmaceutical composition for treating obsessive-compulsive disorder is provided. The present invention relates to (1) a pharmaceutical composition comprising a dopamine D1 receptor agonist as an effective ingredient for treating obsessive-compulsive disorder, and / or (2) a pharmaceutical composition comprising a dopamine D1 and D2 receptor stimulator, which is administered in combination with a dopamine D2 receptor inhibitor for the purpose of stimulating the dopamine D1 receptor in the striatum, and / or (3) a pharmaceutical composition comprising a dopamine D2 receptor inhibitor, which is administered in combination with a dopamine D1 and D2 receptor stimulator.

The application discloses benzamide phenylpiperazine radioactive compounds and a preparation method and application thereof, and belongs to the field of radioactive drugs. 18 The F-labeled compound is simple in preparation method. The benzamide phenylpiperazine radioactive compound can be used as a dopamine D3 receptor targeted radioactive probe, and has the characteristics of excellent biological performance, high chemical purity and high specific activity.

The present invention discloses a 2-amino-5-hydroxytetralin derivative containing a hydroxypyridone side chain, as well as its preparation and application. The target compound is obtained by using 2-amino-5-hydroxytetralin as the parent nucleus, and performing one-step condensation of a specific linker with a benzyl-protected hydroxypyridone and subsequent deprotection. Experiments have shown that at the cellular level, it has a significant anti-ferroptosis effect on RSL-3 or Erastin-induced related tumor cells (human fibrosarcoma cells HT-1080), and has a good protective effect on MPP+-induced damage-related nerve cells (human neuroblastoma cells SH-SY5Y). It also has a strong agonist effect on dopamine D2 receptors (HEK 293 cells stably transfected with human dopamine D2 receptors), and can be used to prepare corresponding anti-Parkinson's drugs. The structural formula I or II of the 2-amino-5-hydroxytetralin derivative containing a hydroxypyridone side chain is as follows: #imgabs0#

This invention belongs to the field of medicinal chemistry, specifically disclosing a thienopyrimidine compound and its application as an allosteric antagonist of the dopamine D2 receptor (D2R). The target compounds of this invention contain a thieno[3,2-d]pyrimidine ring skeleton, the structural formula of which is shown in Formula 1. This invention uses GloSensor cAMP accumulation experiments to test the functional activity of the target compounds for D2R and to elucidate the allosteric mechanism of action of the new compounds on D2R. Pharmacological results show that all target compounds in this invention can negatively allosterically regulate the functional activity of the D2R endogenous ligand dopamine, i.e., all target compounds are negative allosteric modulators or allosteric antagonists of D2R.

The present invention generally relates to binding agents capable of targeting tumor cells and immune cells. The binding agents of the present invention are multispecific and comprise antigen binding domains capable of binding to dopamine receptor D2 (DR2), binding to programmed cell death protein 1 (PD-1), and / or binding to cluster of differentiation 47 (CD47). The multispecific binding agents of the present invention are useful for treating an individual in need thereof.

Disclosed herein are novel compounds including dopamine D3 receptor agonists, compositions thereof, methods of use thereof, and processes of synthesizing the same. Further disclosed are D3R selective agonist compounds, specifically bitopic ligands comprising chirality.

The invention provides certain (phenyl)-3,4-dihydroisoquinolin-2(1H)-yl)ethan-1-one related compounds of formula I as D1 positive allosteric modulators (PAMs), and pharmaceutical compositions thereof. The invention further provides methods of using a compound of formula I, to treat certain symptoms of dopaminergic CNS disorders including Parkinson's disease, Schizophrenia, ADHD or Alzheimer's disease.

The present application relates to a kind of new isoquinoline alkaloid compound and its preparation method and purposes.The new compound (Corybungine A-L) provided by the present application is extracted and separated from Papaveraceae Corydalis bungeana Turcz., a kind of novel isoquinoline alkaloid with novel structure.Biological activity experiment shows that the alkaloid compound has dopamine D2 receptor antagonistic activity, and can be applied in the preparation of dopamine D2 receptor related pain, schizophrenia, Lesch-Nyhan syndrome and other nervous system diseases.

The invention relates to pharmaceutical compositions comprising substituted heterocycle fused gamma carbolines, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) pathway and / or the dopamine D2 receptor pathway, and methods of treating conditions of the central nervous system therewith.

To provide a method for preventing and / or treating a condition, disease, or disorder associated with the dopamine D1 receptor intracellular pathway, for example, a condition, disease, or disorder characterized by a deficit in attention, cognition, memory, and / or inhibitory processing.SOLUTION: A method comprising administering to a subject in need of prevention and / or treatment a pharmaceutically effective amount of a phosphodiesterase 1 (PDE1) inhibitor (for example, a compound represented by formula V).SELECTED DRAWING: None

The present invention relates to a novel isoquinoline alkaloid compound and a preparation method and use thereof. The novel compound (Corybungine A‑L) provided by the present invention is a novel isoquinoline alkaloid extracted and separated from Corydalis bungeana Turcz. in the genus Corydalis of the family Papaveraceae. Biological activity experiments show that the alkaloid compound has dopamine D2 receptor antagonist activity and can be used in the preparation of drugs for dopamine D2 receptor-related pain, schizophrenia, Lesch‑Nyhan syndrome and other nervous system diseases.

The invention belongs to the field of biological medicine. The invention provides a dopamine D2 receptor compound and application thereof in treatment of erectile dysfunction. The dopamine D2 receptor compound provided by the invention has excellent biological activity, and has important application potential in erectile dysfunction treatment drugs.

The present invention relates to PDE1 inhibitory compounds useful in the treatment of diseases involving disorders of the dopamine D1 receptor intracellular pathway, such as, among others, Parkinson's disease, depression, narcolepsy, psychosis, damage to cognitive function, e.g., in schizophrenia, or disorders that may be ameliorated through enhanced progesterone-signaling pathway, as well as their use as pharmaceuticals and pharmaceutical compositions comprising them. Methods of making and methods of use related to such compounds are further described.

The present invention provides a novel ligand for the dopamine D3 receptor and a preparation method therefor. The compound, and a pharmaceutically acceptable salt and a pharmaceutical composition or a pharmaceutical preparation thereof are used for the treatment and prevention of schizophrenia, neurodegenerative diseases, particularly Parkinson's disease, drug dependence, drug addiction, anxiety, depression, etc. The novel ligand of the dopamine D3 receptor features a high affinity, a high specificity, and a high functional selectivity. The compound and the pharmaceutically acceptable salt and the pharmaceutical composition or the pharmaceutical preparation thereof can be used to study the distribution and function of dopamine D2 subtype receptors and mechanism of diseases associated with dysfunction of dopamine D2-like receptors, and can also be used for the disease modification of hyperprolactinemia, extrapyramidal symptoms, and levodopa-associated movement disorder or dyskinesia.

An aza-ergoline derivative and a preparation method therefor and an application thereof. The derivative has a structure as shown in formula (I). The aza-ergoline derivative has good affinity, agonistic activity or selectivity to a dopamine D2 receptor.

Disclosed are a heterocyclic compound and a use thereof. More specifically, disclosed are a heterocyclic compound acting as a dual modulator for 5-HT2A and dopamine D2 receptors and a use thereof as a therapeutic agent for mental illness.