6 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.

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.

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.

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.