Small molecule antagonists of the tachykinin NK 2 receptor. 2004

Daniela Fattori, and Maria Altamura, and Carlo Alberto Maggi
Chemistry Department, Menarini Ricerche S.p.A, via Tito Speri 10, 00040 Pomezia, Rome, Italy. dfattori@menarini-ricerche.it

The NK(2) receptor (member of the tachykinin receptor family) is mainly located in the smooth muscle of the urinary, respiratory and gastrointestinal tracts, with limited presence in the CNS. This has raised interest in tachykinin NK(2) receptor antagonists for the treatment of urological disorders, asthma. This review outlines progress done after 1998 in the field of NK(2) small molecule antagonists, both acting on the NK(1)/NK(2), NK(2)/NK(3), NK(1)/NK(2)/NK(3) receptors and selective for the NK(2) one.

UI MeSH Term Description Entries
D008024 Ligands A molecule that binds to another molecule, used especially to refer to a small molecule that binds specifically to a larger molecule, e.g., an antigen binding to an antibody, a hormone or neurotransmitter binding to a receptor, or a substrate or allosteric effector binding to an enzyme. Ligands are also molecules that donate or accept a pair of electrons to form a coordinate covalent bond with the central metal atom of a coordination complex. (From Dorland, 27th ed) Ligand
D009130 Muscle, Smooth Unstriated and unstriped muscle, one of the muscles of the internal organs, blood vessels, hair follicles, etc. Contractile elements are elongated, usually spindle-shaped cells with centrally located nuclei. Smooth muscle fibers are bound together into sheets or bundles by reticular fibers and frequently elastic nets are also abundant. (From Stedman, 25th ed) Muscle, Involuntary,Smooth Muscle,Involuntary Muscle,Involuntary Muscles,Muscles, Involuntary,Muscles, Smooth,Smooth Muscles
D012140 Respiratory Tract Diseases Diseases involving the RESPIRATORY SYSTEM. Respiratory Diseases,Respiratory System Diseases,Disease, Respiratory System,Disease, Respiratory Tract,Respiratory System Disease,Respiratory Tract Disease
D005767 Gastrointestinal Diseases Diseases in any segment of the GASTROINTESTINAL TRACT from ESOPHAGUS to RECTUM. Cholera Infantum,Gastrointestinal Disorders,Functional Gastrointestinal Disorders,Gastrointestinal Disorders, Functional,Disease, Gastrointestinal,Diseases, Gastrointestinal,Functional Gastrointestinal Disorder,Gastrointestinal Disease,Gastrointestinal Disorder,Gastrointestinal Disorder, Functional
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D013329 Structure-Activity Relationship The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups. Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships
D014570 Urologic Diseases Pathological processes of the URINARY TRACT in both males and females. Urinary Tract Diseases,Urological Diseases,Disease, Urinary Tract,Disease, Urologic,Disease, Urological,Diseases, Urinary Tract,Diseases, Urologic,Diseases, Urological,Urinary Tract Disease,Urologic Disease,Urological Disease
D015195 Drug Design The molecular designing of drugs for specific purposes (such as DNA-binding, enzyme inhibition, anti-cancer efficacy, etc.) based on knowledge of molecular properties such as activity of functional groups, molecular geometry, and electronic structure, and also on information cataloged on analogous molecules. Drug design is generally computer-assisted molecular modeling and does not include PHARMACOKINETICS, dosage analysis, or drug administration analysis. Computer-Aided Drug Design,Computerized Drug Design,Drug Modeling,Pharmaceutical Design,Computer Aided Drug Design,Computer-Aided Drug Designs,Computerized Drug Designs,Design, Pharmaceutical,Drug Design, Computer-Aided,Drug Design, Computerized,Drug Designs,Drug Modelings,Pharmaceutical Designs
D015394 Molecular Structure The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds. Structure, Molecular,Molecular Structures,Structures, Molecular

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