摘要:
New analgesic compounds, which are prepared by the hydrolysis of N-acylated 4-hydroxyphenylamine derivatives, their synthesis and pharmaceutical compositions containing them are disclosed. These compounds surprisingly possess high analgesic activity with little hepatotoxic effect, making them more useful than conventional non-steroidal anti-inflammatory drugs (NSAIDs) in the treatment of chronic pain.
摘要:
The present invention is based, in part, on our discovery that certain types of therapeutic agents can be used in combination to treat a variety of neuropsychiatric and related disorders, including addiction (e.g., to a substance or to an activity) as well as to alleviate some of the symptoms experienced during menopause or associated with the menstrual cycle. Regardless of the precise formulation, the compositions of the invention can include at least one active ingredient that targets the hypothalamo- pituitary-adrenal (HPA) axis and at least one active ingredient that targets the prefrontal cortex. Either or both of these types of agents can be combined with an agent that inhibits activity in the sympathetic nervous system. Thus, the compositions or combination pharmacotherapies can also include an agent that inhibits a beta-adrenergic receptor or that otherwise acts as an anti-hypertensive or anxiolytic agent.
摘要:
Boron-containing porphyrin compounds are disclosed that may be used for boron neutron capture therapy of tumors, radiotherapy of tumors, and photodynamic therapy of tumors.
摘要:
The present invention encompasses methods and compositions for treating a bone condition. The isolated adipose tissue-derived stromal cell of the invention and products related thereto have a plethora of uses, including but not limited to research, diagnostic, and therapeutic applications such as in spinal fusion procedures.
摘要:
A non-invasive in vivo technique is disclosed, useful for example in detecting cancers and micrometastases. The technique may be used to selectively deliver drugs to target cells such as tumors, metastases, micrometastases, and individual malignant cells. Ligands with specificity for a target cell receptor, and optionally drug molecules as well, are covalently bound to magnetic nanoparticles, either directly or through a spacer molecule. The ligand precludes the need for a separate coating layer. For example, human breast cancer cells express receptors both for luteinizing hormone/chorionic gonadotropin (LH/CG), and for luteinizing hormone releasing hormone (LHRH). These cells can be specifically targeted by iron oxide nanoparticles covalently linked to LH/CG or LHRH. The nanoparticles are incorporated into the cancer cells through receptor-mediated endocytosis. The specific accumulation in targeted cancer cells enhances resolution for imaging, therapy, or both. The ligand may, for example, be a hormone, receptor, or antibody, or a fragment thereof.
摘要:
The topical administration of a combination of nerve growth factor (NGF) and docosahexaenoic acid (DHA) has been discovered to synergistically increase the effects of NGF in re-innervating the cornea. This enhancement in corneal nerve re-growth will yield a faster anatomical and functional recovery after PRK or LASIK surgeries. Using rabbits, the application of NGF and DHA resulted in increased corneal nerve surface area, increased epithelial proliferation, and decreased rose bengal staining as compared with NGF, DHA, or vehicle control individually. The topical application of NGF plus DHA in accelerating the re-innervation after PRK or LASIK, will help avoid or alleviate the symptoms of dry eye or other neurotrophic keratopathies due to corneal injuries. The topical application can be by using a corneal shield or lens. This treatment will also be useful in other corneal abnormalities including those caused by chemical burn, congenital corneal neuropathy, or acquired corneal neuropathy.
摘要:
The present invention relates generally to analgesic compounds having a mu opioid receptor agonist linked to a delta opioid receptor antagonist, and to methods for producing analgesia using such compounds. As compared to opioids such as morphine, these compounds can cause less tolerance, physical dependence, and/or constitpation. These compounds are also more potent than morphine and are able to cross the blood brain barrier, thereby allowing for peripheral (e.g., IV) administration.
摘要:
The present invention relates to a method of treating a warm-blooded animal, especially a human, having hyperparathyroidism comprising administering to said animal a therapeutically effective amount of an epothilone derivative of formula (I) or a pharmaceutically acceptable salt thereof.
摘要:
Two genes have been discovered that show single nucleotide polymorphisms that are differentially expressed in patients with inflammatory bowel disease (IBD) as compared to unaffected controls. These two genes, FLJ21425 and CSF1R (colony stimulating factor 1 receptor), are located close together on chromosome 5q33 which was known to have other IBD susceptibility genes. Moreover, expression of the CSF1R gene was shown in the intestinal epithelium. These two genes can be used to test for the presence of the allele associated with IBD for an early diagnosis of susceptibility to IBD. Early identification of subjects with susceptibility to IBD will enable early treatment with known methods. Additionally, the two genes can be used to target treatment, e.g., drugs known to affect CSF1R expression. Based on gene expression data, chromosomal location and biological function, the colony stimulating factor 1 receptor gene was shown to contribute to Crohn's disease susceptibility.
摘要:
A unique DHA product, 10, 17S-docosatriene ('Neuroprotectin D1' or 'NPD1'), was found to provide surprisingly effective neuroprotection when administered right after an experimental stroke. Moreover, both nerve cells and retinal pigment epithelial (RPE) cells were found to synthesize 10,175-docosatriene (NPD 1) from DHA. NPD 1 also potently counteracted H2O2/TNFα oxidative stress-mediated cell apoptotic damage. Under the same oxidative-stress conditions, NPDI up-regulated the anti-apoptotic Bcl-2 proteins, Bcl-2 and Bcl-xL, and decreased expression of the pro-apoptotic proteins, Bad and Bax. Moreover, in RPE cells NPD1 inhibited oxidative stress-induced caspase-3 activation, IL-lß-stimulated human COX-2 promoter expression, and apoptosis due to N-retinylidene-N-retinylethanolamine (A2E). Overall, NPD1 protected both nerve and retinal pigment epithelial cells from cellular apoptosis and damage due to oxidative stress. NPD1 concentration in the brain of Alzheimer's patients was found to be significantly decreased from that of controls. In cultured human brain cells, NPD1 synthesis was up-regulated by neuroprotective soluble ß amyloid, and NPD 1 was found to inhibit secretion of toxic ß amyloid peptides.