12 results about "Receptor selectivity" patented technology

The invention provides a heteroaromatic ring compound as well as a pharmaceutical composition and application thereof. Specifically, the invention provides a compound shown as a formula (I), a pharmaceutically acceptable salt of the compound, a solvate of the compound or a solvate of the pharmaceutically acceptable salt of the compound. The heteroaromatic ring compound provided by the invention has one or more of the following advantages: good 5-HT4 receptor selective excitation activity and relatively weak hERG inhibitory activity.

Compound I as defined, having high S1P5 receptor-selective agonist activity on the S1P1 receptor, and the crystal forms of Compound I, the salts of Compound I, and the crystal forms of salts thereof are provided as drug substances of pharmaceuticals.

The present invention relates to a morphinan-type compound, a preparation method therefor, a composition thereof and the use thereof. Specifically disclosed is a compound I or a pharmaceutically acceptable salt thereof. The morphinan-type compound of the present invention has one or more of the following effect advantages: (1) a relatively high binding affinity for an opioid receptor; (2) a significant agonistic effect on KOR and MOR; (3) good selectivity for a κ receptor; and (4) a good therapeutic effect on inflammatory pain (for example, rapid onset of action or significant analgesic effect).

The present application relates to oxytocin receptor selective cyclic peptide molecules and their use in the preparation of anti neuropathic pain drugs. The present application provides an oxytocin receptor (OXTR) selective cyclic peptide molecule, the OXTR selective cyclic peptide molecule comprises an amino acid sequence as shown in formula I and salts thereof: formula I: [CYIX1NC]X2X3G-NH2. The OXTR selective polypeptide provided by the present application, by establishing a bioluminescence resonance energy transfer high-throughput screening system for OXTR, detecting the G alpha q protein decoupling triggered after the polypeptide ligand activates OXTR, in order to screen out candidate molecules that can selectively agonize OXTR and play an anti neuropathic pain, and is expected to realize the discovery of anti neuropathic pain new drugs.

A method for selective extraction of lithium halide from a solid phase into an organic phase, using a receptor that selectively binds lithium cations and halide anions, wherein the receptor is dissolved in an organic solvent or a mixture of organic solvents, in contact with the solid phase, which receptor reversibly binds a lithium halide ion pair to form a complex that is soluble in the organic solvent or the mixture of organic solvents, wherein lithium halide is isolated by a back- extraction of a lithium halide ion pair into an aqueous phase, resulting in the dissociation of the complex and the transfer of the lithium halide to the aqueous phase while the free receptor remains in the organic phase or precipitates. The solid extraction product, containing the lithium halide is isolated after separation of the aqueous phase from the organic phase and evaporation of water from the aqueous solution thus obtained, or by precipitation in the form of a poorly soluble salt.

The invention relates to a morphinan type compound as well as a preparation method, a composition and application thereof. Specifically disclosed is a compound I or a pharmaceutically acceptable salt thereof. The morphinan type compound provided by the invention has one or more of the following effects and advantages: (1) the morphinan type compound is relatively high in binding affinity with an opioid receptor; (2) the compound has an obvious agonistic effect on KOR and MOR; (3) the selectivity to a kappa receptor is good; and (4) the ointment has a good treatment effect on inflammatory pain (for example, the ointment takes effect quickly or has an obvious pain effect).

An object of the present invention is to provide a formulation capable of effectively suppressing post-operative delirium. A post-operative delirium suppressant according to the present invention contains a GABA-A receptor-selective positive allosteric modulator as an active ingredient.

To provide novel functionalized lactams as modulators of the 5-hydroxytryptamine receptor 7 and methods of using the same.SOLUTION: Described herein are new, selective modulators of the 5-HT7 receptor. These selective compounds may be useful for the treatment of CNS and non-CNS indications. The compounds described herein may be selective in targeting 5-HT7 receptors as compared to other receptors and / or by selectively targeting 5-HT7 receptors expressed in certain tissues or organs, thereby providing effective selectivity through a particular partitioning profile of the 5-HT7 modulator.SELECTED DRAWING: None

This invention reports rational design, synthesis, and characterization of a series of a delta opioid receptor (DOR)-selective bitopic ligands targeting a conserved sodium site in DOR. The design is based on modifications in a selective DOR ligand, Naltrindole, and related indole-to-quinoline derivatives. The discovered compounds are analgesics that are free of addiction and seizure liabilities. Accordingly, a compound of the technology described herein is represented by Formula I:

The application prepares a hyaluronic acid-encapsulated dexmedetomidine microneedle system, which is verified by multidimensional characterization, and the microneedle system has excellent forming property, mechanical property, transdermal and drug release performance, has the characteristics of rapid effect (0.5h cumulative release 43.3%) and long-term delivery (4h cumulative release 86.5%), and has good biocompatibility, and the behavior and electrophysiology experiments confirm that the anti-haze and anti-vomiting effect is remarkable, and because the alpha 2 receptor selectivity is higher, the effect is better than that of clonidine.

The present disclosure provides compounds 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 39, 38, 39 JPEG2026500166000038.jpg48165 or a pharmaceutically acceptable salt thereof. The unit dosage forms described herein are suitable for oral administration. There remains a need for anti-estrogen agents that can completely inhibit estrogen receptors, including those encoded by both wild-type and mutant forms (e.g., those containing activating mutations) of the genes encoding estrogen receptor alpha (ERα) and estrogen receptor 1 (ESR1). Selective estrogen receptor modulators (SERMs) or degraders (SERDs) are particularly useful or promising tools for such treatment.

The present invention relates to selective GLP1R agonists. In particular, the present invention relates to the finding that the secretin (SCT) may be converted into highly potent and selective GLP1R agonists.