摘要:
The present invention relates to novel peptide compounds which are effective in modulating one or more melanocortin receptor types, to the use of the compounds in therapy, to methods of treatment comprising administration of the compounds to patients in need thereof, and to the use of the compounds in the manufacture of medicaments. The compounds of the invention are of particular interest in relation to the treatment of obesity as well as a variety of diseases or conditions associated with obesity.
摘要:
Metallopeptide compositions are provided for treatment of sexual dysfunction in mammals, including male sexual dysfunction, such as erectile dysfunction, and female sexual dysfunction. The metallopeptides include at least one, and preferably two, aromatic amino acid side chain moieties, and are further characterized in that the metallopeptides preferably do not bind or significantly bind to a melanocortin receptor.
摘要:
Cyclic peptides of formula I are potent and selective agonists of melanocortin-4 receptors, and as such are useful research tool for the determination of the physiological roles of the MC-4 receptor, as well as for the diagnoses, treatment or prevention of disorders or diseases mediated through the MC-4 receptor.
摘要:
Disclosed are cyclic peptide analogs that are MC-4 and/or MC-3 receptor ligands, the analogs having a structure according to Formula (I): wherein B, X, E, Z, D, G, M′, W, R, R1, R1′, R11, m, n, p and q are as described in the specification. The peptide analogs are useful in treating diseases that are mediated by the MC-4 and/or the MC-3 receptor. As such, the invention is directed to methods of treating body weight disorders, such as obesity, anorexia, and cachexia. The invention also relates to the treatment of CNS depression, behavior-related disorders, memory-related disorders, cardiovascular function, inflammation, sepsis, septic shock, cardiogenic shock, hypovolemic shock, sexual dysfunction, erectile dysfunction, muscle atrophy, diseases associated with nerve growth and repair, and intrauterine fetal growth. Also disclosed are pharmaceutical compositions comprising the peptide analogs of Formula (I).
摘要:
Peptide antagonists of &agr;-melanocyte stimulating hormone are disclosed, together with methods of inhibiting the effects of &agr;-melanocyte stimulating hormone on cells or tissues sensitive to that hormone. In particular, methods for lightening the pigmentation of skin and for treating malignant melanoma, as well as kits for practicing the invention are also disclosed.
摘要:
The invention provides ligands for melanocortin receptors. For example, the invention provides the melanocortin receptor peptide ligand Ac-Nlc-Gln-His-(p(I)-D-Phe)-Arg-(D-Trp)-Cly-NH2, (SEQ ID NO: 1), where the iodo group is unlabeled or radioactively labeled. The invention additionally provides methods of assaying for melanocortin receptors in a cell or tissue such as brain. The invention also relates to pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a melanocortin receptor ligand and to methods of administering the pharmaceutical composition to a subject. The invention further provides tetrapeptide ligands for melanocortin receptors and methods of altering melanocortin receptor activity.
摘要翻译:本发明提供黑皮质素受体的配体。 例如,本发明提供黑皮质素受体肽配体Ac-Nlc-Gln-His-(p(I)-D-Phe)-Arg-(D-Trp)-Cly-NH 2,(SEQ ID NO:1) 其中碘基团未标记或放射性标记。 本发明另外提供了测定细胞或组织如脑中黑皮质素受体的方法。 本发明还涉及包含药学上可接受的载体和黑皮质素受体配体的药物组合物以及向受试者施用该药物组合物的方法。 本发明还提供了黑皮质素受体的四肽配体和改变黑皮质素受体活性的方法。
摘要:
Cyclic peptides of formula I are potent and selective antagonists of melanocortin-4 receptors, and as such are useful research tool for the determination of the physiological roles of the MC-4 receptor, as well as for the diagnosis, treatment or prevention of disorders or diseases mediated through the MC-4 receptor.