36 results about "Prostaglandin F2alpha" patented technology

A method of treating age-related macular degeneration in an eye is described, comprising contacting the eye with a therapeutic amount of a prostaglandin F2alpha derivative. The preferred prostaglandin F2alpha derivative is latanoprost, and the preferred dosage is between about 1.5 mug and about 4.5 mug per day per eye.

An ophthalmic formulation for the treatment of glaucoma and intraocular pressure with a prostaglandin compound of the F-series (PGF), and particularly a prodrug form of a PGF2α analog, such as an ester, amide, or internal lactone, wherein preservative is an antimicrobial peptide, such as lactoferrin. In particularly preferred embodiments, the prostaglandin compound is a macrocyclic internal 1,15-lactone, such as the 16-aryloxy prostaglandin analogs, illustratively fluprostenol or cloprstenol.

The present invention relates to a new class of G protein-coupled receptor agonist or antagonist, which specifically binds to the receptor protein structural elements, thus altering signal transmission and subsequent physiological effects. Described herein are peptide sequences derived from the G protein-coupled receptor protein, produced by chemical methods as selective inhibitors of signal transduction associated with stimulation of the receptor by its ligand. Such peptides or molecules derived from their primary, secondary or tertiary structures may be used as effective tocolytics for the prevention of premature labor or be used for the treatment of dysmenorrhea.

The present invention provides a new and effective process for the synthesis of 17-phenyl-18,19,20-trinor-PGF2 alpha and its derivatives, including the anti-glaucoma drugs Bimatoprost and Latanoprost. The benefit of the present invention rises inter alia from the fact that a major intermediate involved in the synthesis of the above compounds may be isolated from a mixture containing also an undesired isomer, by crystallization. In addition, the undesired isomer may be oxidized to give the starting compound, which is then recycled.

The invention relates to compositions which are useful for inhibiting prostaglandin F2αreceptor. The compositions include, but are not limited to, linear peptides, peptide analogs, and peptidomimetics. Methods of using the compositions of the invention to treat preterm labor and dysmenorrhea are disclosed.

An object of the present invention is to find a new pharmaceutical application of a prostaglandin F2α derivative. It was found that the prostaglandin F2α derivative inhibits glutamate-induced retinal neuronal cell death in a concentration-dependent manner in rat fetal retinal neuronal cells, in other words, the prostaglandin F2α derivative acts directly on the retinal neuronal cells and exhibits a protective effect. Accordingly, the prostaglandin F2α derivative is useful for the prevention or treatment of an eye disease associated with retinal neuronal cell damage.

The invention provides a method for fixed-time inseminating of anestrus and non-pregnant sows. The method is characterized in that 1, pre-treatment: applying prostaglandin F2alpha or cloprostenol sodium for long-time anestrus multiparous sows, long-time anestrus replacement sows and non-pregnant sows, and not performing pre-treatment on the anestrus sows within seven days after weaning; 2, promoting of synchronizing of follicular development and estrus induction of the sows: applying a medicine for promoting the follicular development and estrus induction; 3, promoting of synchronizing of sow ovulation: applying a medicine for promoting the follicle final maturing and ovulation; 4, fixed-time inseminating: applying a medicine for promoting ovulation for the obvious estrus, standing reaction, un-estrum or anestrus or inobvious estrus sows, and performing fixed-time inseminating. The method has the advantages that the breeding and delivering rate is effectively improved, the sow resources are sufficiently utilized, the elimination rate of the multiparous sows is reduced, and the utilization rate of the replacement sows is improved.

The invention relates to an analysis method of 8-hydroxy deoxyguanosine, 8-hydroxy guanosine and 8-iso-prostaglandin F2alpha in urine of a human body. The analysis method has the characteristics that the method can detect a change in in vivo typical oxidative stress biological marker caused by active oxygen relatively conveniently, rapidly and quantitatively, and can be used for evaluating in vivo oxidative damage and restoring degrees and studying a pathological process of a disease. The method employs AgilentBondEluC18 solid phase extraction column, three compounds of two different mass spectrometric detection modes, i.e., 8-hydroxy deoxyguanosine, 8-hydroxy guanosine (cation mode detection) and 8-iso-prostaglandin F2alpha (anion mode detection), in the urine can be purified simultaneously, and are subjected to liquid chromatography tandem mass spectrometry detection by the same liquid chromatography column and the same mobile phase. The method has simple, convenient and quick pretreatment, and is high in sensitivity, good in repeatability and high in recovery rate.

The invention concerns a new process for the preparation of prostaglandin derivatives, in particular prostaglandin F2α derivatives, for example bimatoprost, latanoprost and travoprost, the new intermediates of said process and their use in the preparation of prostagblandin derivatives.

The invention relates to a composition for use in treating corneal and conjunctival lesions, wherein the composition comprises a prostaglandin F2alpha or analogue, in a therapeutic amount, said composition being in a form suitable for topical application on the ocular surface and is free of deleterious preservative; the invention also relates to a method for treating surface ocular conditions in a patient in need thereof, comprising administering a composition of the invention.

The invention relates to conformation-constrained entirely-synthetic macrocyclic compounds. A conformation-constrained, space-defined 12-30-member macrocyclic system (I) which is as shown in the description comprises three different constitution units: an aromatic template a, a confor1ation regulator b and a spaced part c, which are illustrated in the description and the claims. The macrocyclic compounds (I) can be easily prepared according to a parallel synthesis method or a combinatorial chemistry method, and are designed for realizing interaction with a specific biological target. Particularly, the compounds show agonistic or antagonistic activity to the following matters: a motilin receptor (MR), a 5-hydroxytryptamine receptor (5-HT2B receptor) of a subtype 5-HT2B, and a prostaglandin F2alpha receptor (FP receptor). Thus, the compounds are effectively used for treating gastrointestinal tract hypomotility disorder such as diabetic gastroparesis and constipation-predominant irritable bowel syndrome, CNS-related diseases such as migraine, schizophrenia, psychosis and depression, ocular hypertension such as glaucoma-related ocular hypertension, and premature delivery.

The invention discloses a synthesizing method of trometamol prostaglandin F2alpha. The synthesizing method includes: using a compound (-)-Corey lactone diol as the raw material, performing oxidation reaction to obtain lactone aldehyde, allowing the lactone aldehyde to splice with a lower side chain through Wittig-Horner reaction to obtain olefin, reducing double carbonyl in the olefin to obtain alcohol, allowing the alcohol to have ylide-Wittig reaction with an upper side chain to obtain prostaglandin F2alpha, dissolving the prostaglandin F2alpha into trometamol, and performing crystallization to obtain the trometamol prostaglandin F2alpha. The synthesizing method does not need a precious-metal catalyst and is few in side reaction, high in yield, low in cost, little in pollution and suitable for large-scale industrial production.

The present invention provides a resin container in which an aqueous liquid preparation containing a prostaglandin F2α derivative having at least a fluorine atom in its molecule can be stored stably for a long period of time. By storing the aqueous liquid preparation containing the prostaglandin F2α derivative having at least a fluorine atom in its molecule in the resin container made of a propylene / ethylene copolymer in which the ratio of a propylene component to an ethylene component is in the range of from 94.0 / 6.0 to 99.5 / 0.5 (propylene component / ethylene component), a decrease in the content of the prostaglandin F2α derivative in the aqueous liquid preparation is inhibited.

An embryo that is transferred into the uterus of a recipient female is protected from embryotoxic effects of prostaglandin F2α by exposing the embryo to a prostaglandin antagonist.

The invention discloses an application of hydrogen in preparation of a drug for preventing limb ischemia-reperfusion injury. Experimental results show that hydrogen can remarkably reduce rise of limb ischemia-reperfusion MDA (malondialdehyde) and 8-isoprostanes F2alpha (8-iso-PGF2alpha), protect the activity of SOD (superoxide dismutase) and GSH-Px (glutathione peroxidase), reduce lipid peroxidation, protect histocyte structure and function integrity, effectively protect tissue injury caused by limb ischemia-reperfusion and has great significance for clinical prevention and treatment of the limb ischemia-reperfusion injury.

Molecular cloning and expression of a prostaglandin F2alpha receptor which is linked to the signal transduction pathways via guanine nucleotide binding regulatory (G) proteins and measured by, for example, cAMP, IP3 or intracellular calcium. By constructing cell lines that express a prostaglandin F2alpha receptor, the affinities and efficacies of agonist and antagonist drugs with the receptor can be assessed. A recombinant DNA construct includes a vector and a DNA fragment encoding a prostaglandin F2alpha receptor. A host cell is transformed with a recombinant DNA construct, so that the DNA fragment is expressed and a prostaglandin F2alpha receptor is produced. Suitable host systems include eukaryotic and prokaryotic cells, especially mamalian cells such as rat or human. Additionally, for diagnostic purposes, antibodies to a prostaglandin F2alpha receptor can be prepared by producing all or a portion of the receptor protein and injecting these into various types of mammals. Using the resulting antibodies, expression of an F2alpha receptor cDNA, i.e. receptor protein in tissue and cells can be measured.

The present invention provides a resin-made container which enables long-term stable preservation of aqueous liquid preparations containing prostaglandin F2a derivatives having fluorine atoms in the molecule. An aqueous liquid preparation containing a prostaglandin F2a derivative having a fluorine atom in the molecule is protected from lowering in the prostaglandin F2a derivative content by keeping the preparation in a container made of a propylene / ethylene copolymer having a propylene / ethylene ratio of 94.0 / 6.0 to 99.5 / 0.5.

Provided are methods for determining the level of microglial activation in the brain of a subject by measuring blood Prostaglandin E2 (PGE2), Prostaglandin F2α, or both, and C-Reactive Protein (CRP) concentrations in a sample obtained from a subject, wherein the ratio of [PGE2] / [CRP], [PGF2α] / [CRP], or both, is indicative of the level of microglial activation in the brain of the subject.

The invention relates to a specific monoclonal antibody hybridoma cell strain WXX-2 of antiprostaglandin F2alpha and application thereof and belongs to the technical field of clinical detection. The specific monoclonal antibody hybridoma cell strain WXX-2 of antiprostaglandin F2alpha provided by the invention has been preserved in CGMCC with the preservation number of CGMCC No. 13087. The specific monoclonal antibody of antiprostaglandin F2alpha is secreted by the specific monoclonal antibody hybridoma cell strain WXX-2 of antiprostaglandin F2alpha. The hybridoma cell strain WXX-2 can secrete a monoclonal antibody which has relatively good specificity and relatively high sensitivity on prostaglandin F2alpha, and the 50% inhibition concentration IC50 on the prostaglandin F2alpha is 1.80 [mu]g / L. The specific monoclonal antibody can be used for specific detection of the prostaglandin F2alpha in clinical detection.

The invention relates to compositions which are useful for inhibiting prostaglandin F2α receptor. The compositions include, but are not limited to, linear peptides, peptide analogs, and peptidomimetics. Methods of using the compositions of the invention to treat preterm labor and dysmenorrhea are disclosed.

Cells and cell lines that are genetically modified to express the hCox-2 enzyme, which results in the upregulation of prostaglandin F2 alpha (PGF2a) on the cells have been obtained. Encapsulated cell therapy devices containing such cells or cell lines that are capable of delivering PGF2a, as well as methods of using these devices to deliver PGF2a to the eye and to treat ophthalmic disorders in patients suffering therefrom are also described.

The invention discloses an application of citrus fruit volatile oil in preparation of food and medicine that regulate a human endocrine system and are used to relieve or neutralize effect of alcohol.The development of the citrus volatile oil food and medicine can make full use of the peel of citrus fruits and avoid waste of resources. In addition, the current drugs for relieving or neutralizing effect can only inhibit the development of the disease and have side effects, and cannot achieve the purpose of relieving or neutralizing effect as well as sobering up. The citrus fruit volatile oil incitrus plant volatile oil food and medicine can achieve the purpose of sobering up by inhibiting the secretion of prostaglandin F2alpha, increasing the secretion of prostaglandin E2, reducing the expression level of inflammatory factors, improving the body's antioxidant capacity, adjusting the human endocrine system, and stimulating the hormone secretion of the glands in the body to return to normal levels.

The invention belongs to the field of weight loss and beautification, and particularly relates to a composition for eliminating subcutaneous fat deposition and application of the composition. The composition comprises prostaglandin F2 alpha (PGF2 alpha) receptor stimulants and skin care active components. A mass ratio of the prostaglandin F2 alpha receptor stimulants to the skin care active components in the composition is 0.1-10:1-100, and the preferable mass ratio of the prostaglandin F2 alpha receptor stimulants to the skin care active components is 0.1-1:1-100. The composition and the application have the advantages that the composition can be locally applied to skin surfaces, accordingly, effects of eliminating the subcutaneous fat deposition can be realized, and skin can be whitenedand tightened; the composition is convenient to use, high in safety and free of side effects.

Provided are methods for determining the level of microglial activation in the brain of a subject by measuring blood Prostaglandin E2 (PGE2), Prostaglandin F2α, or both, and C-Reactive Protein (CRP) concentrations in a sample obtained from a subject, wherein the ratio of [PGE2] / [CRP], [PGF2α] / [CRP], or both, is indicative of the level of microglial activation in the brain of the subject.

A convergent synthesis of the prostaglandin F2α analogues, travoprost and bimatoprost, was developed employing Julia-Lythgoe olefination of the structurally advanced phenylsulfone with an enantiomerically pure aldehyde ω-chain synthon. The novel convergent strategy allows the synthesis of a whole series of prostaglandin analogues of high purity from a common and structurally advanced prostaglandin intermediate.

The invention discloses an application of citrus fruit volatile oil in preparation of food and medicine that regulate a human endocrine system and are used to treat hemorrhoid. The functional hemorrhoid can be treated by inhibiting the secretion of prostaglandin F2alpha, increasing the secretion of prostaglandin E2, reducing the expression level of inflammatory factors, improving the body's antioxidant capacity, adjusting the human endocrine system, and stimulating the hormone secretion of glands in the body to return to normal levels The product makes full use of the peel of citrus fruits, avoids waste of resources, and can effectively treat hemorrhoid without temporary eating a laxative to improve hemorrhoid.

The present invention relates to compositions for treating glaucoma and elevated ocular pressure. The compositions comprise a nitric oxide releasing isomannide derivative and a prostaglandin F2[alpha] analog.

The invention relates to conformation-constrained entirely-synthetic macrocyclic compounds. A conformation-constrained, space-defined 12-30-member macrocyclic system (I) which is as shown in the description comprises three different constitution units: an aromatic template a, a confor1ation regulator b and a spaced part c, which are illustrated in the description and the claims. The macrocyclic compounds (I) can be easily prepared according to a parallel synthesis method or a combinatorial chemistry method, and are designed for realizing interaction with a specific biological target. Particularly, the compounds show agonistic or antagonistic activity to the following matters: a motilin receptor (MR), a 5-hydroxytryptamine receptor (5-HT2B receptor) of a subtype 5-HT2B, and a prostaglandin F2alpha receptor (FP receptor). Thus, the compounds are effectively used for treating gastrointestinal tract hypomotility disorder such as diabetic gastroparesis and constipation-predominant irritable bowel syndrome, CNS-related diseases such as migraine, schizophrenia, psychosis and depression, ocular hypertension such as glaucoma-related ocular hypertension, and premature delivery.

A method of protecting a retinal neuronal cell by administering an effective amount of a prostaglandin F2α derivative to a patient. A method of preventing or treating an eye disease associated with retinal neuronal cell damage by administering a therapeutically effective amount of a prostaglandin F2α derivative to a patient.