157 results about "Adrenoceptor agonist" patented technology

Methods and compositions for the treatment of pain and other conditions in a mammal using a composition which directly or indirectly stimulates alpha 2 adrenoreceptor agonist activity with a minimum of sedation or other side effects.

The present invention is directed to the treatment of skin erythema as exhibited in rosacea and other conditions characterized by increased erythema (redness) of the skin. These conditions exhibit dilation of blood vessels due to a cutaneous vascular hyper-reactivity. In particular, the present invention is directed to a novel composition and method for the treatment of skin erythema using α1-adrenergic receptor (α1-adrenoceptor) agonists incorporated into cosmetic, pharmacological or dermatological compositions for topical application to the skin.

The invention provides novel β2 adrenergic receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with β2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.

The present study demonstrates that brimonidine tartrate, an alpha-2 adrenergic receptor agonist, can prevent photoreceptor cell degeneration and the associated Muller cell degenerative signs in an in vitro model of retinal degeneration and retinal detachment (separation of the neuroretina from the retinal pigment epithelium). Similar to control conditions, brimonidine allowed for the formation of highly structured photoreceptor outer segments, prevented the expression of stress markers in Müller cells and preserved the expression patterns of Muller cell markers of proper cell-cell contact and differentiation. Ultrastructural studies also indicated that brimonidine favored the formation of cell-cell junctions between photoreceptor cells and Müller cells, indicating that this phenomenon is associated with the exertion of the neuroprotective effect. The results suggest that brimonidine compounds may be utilized as an effective therapeutic agent for early and late onset retinal degenerations caused by defects in photoreceptor cells, Müller cells or both, and as an adjuvant to therapeutic success in retinal detachment surgery or macular translocation surgery for age-related macular degeneration.

Combination therapies of an alpha-2 adrenergic receptor agonist and an alpha-2 adrenergic receptor antagonist at a concentration effective to potentiate but not antagonize a therapeutic effect of the alpha-2 adrenergic receptor agonist are provided. Also provided are methods for use of these combination therapies in potentiating the therapeutic effects of alpha-2 adrenergic receptor agonists, inhibiting development of acute and / or chronic tolerance to alpha-2 adrenergic receptor agonists and treating conditions treatable by alpha-2 adrenergic receptor agonist therapy in a subject. In addition, a method for reversing alpha-2 adrenergic receptor agonist tolerance and / or restoring therapeutic effect of an alpha-2 adrenergic receptor agonist in a subject via administration of an alpha-2 adrenergic receptor antagonist at a concentration effective to potentiate, but not antagonize, the therapeutic effect of the alpha-2 adrenergic receptor agonist is provided.

This invention involves compounds having the following structure: wherein: a) R1 is hydrogen; or alkyl; bond (a) is a single or a double bond; b) R2 and R3 are each independently selected from hydrogen; unsubstituted C1-C3 alkanyl, alkenyl or alkynyl; cycloalkanyl, cycloalkenyl; unsubstituted C1-C3 alkylthio or alkoxy; hydroxy; thio; nitro; cyano; amino; C1-C3 alkylamino or C1-C3 dialkylamino and halo; c) R4, R5 and R6 are each independently selected from hydrogen; unsubstituted C1-C3 alkanyl, alkenyl or alkynyl; cycloalkanyl, cycloalkenyl; unsubstituted C1-C3 alkylthio or alkoxy; hydroxy; thio; nitro; cyano; amino; C1-C3 alkylamino or C1-C3 dialkylamino; halo; and 2-imidazolinylamino; and wherein one and only one of R4, R5 and R6 is 2-imidazolinylamino; d) R7 is selected from hydrogen; unsubstituted C1-C3 alkanyl, alkenyl or alkynyl; cycloalkanyl, cycloalkenyl; unsubstituted C1-C3 alkylthio or alkoxy; hydroxy; thio; nitro; cyano; amino; C1-C3 alkylamino or C1-C3 dialkylamino and halo; e) the compound is not 4-(2-imidazolinylamino)indole; enantiomers, optical isomers, stereoisomers, diastereomers, tautomers, addition salts, biohydrolyzable amides and esters thereof, and pharmaceutical compositions comprising such novel compounds. The invention also relates to the use of such compounds for treating disorders modulated by alpha-2 adrenoceptors.

This invention describes the use of beta-3-adrenoceptor agonists for the treatment of disorders associated with the prostate. These include disorders like those occurring in a prostatitis, where attributable to inflammatory processes or chronic irritation, or disorders like those associated with benign changes of the prostate. The invention is particularly suitable for the treatment of benign prostatic hyperplasia (BPH).

This invention describes a new combination for the treatment of functional bladder disorders which comprises a beta-3-adrenoceptor agonist and an active substance which influences prostaglandin metabolism.

The invention provides novel β2 adrenergic receptor agonist compounds of formula (I): wherein R1-R13 and w have any of the values described in the specification. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with β2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.

This invention describes a new combination for the treatment of functional bladder disorders which comprises an alpha antagonist and / or 5-alpha-reductase inhibitor and a beta-3-adrenoceptor agonist.

The invention discloses a Beta 2-adrenergic receptor stimulant detection method based on microfluidic chip; the detection system adopts laser detection; the detection system takes the microfluidic chip (1) as the core, and the microfluidic chip (1) is sequentially compounded through three-layer structure, including: the upper fluid pathway layer (101), a middle elastic film layer (102) and a lower pneumatic control layer (103); the relationship of the three parts includes that: the upper fluid pathway layer (101) and the lower pneumatic control layer (103) are tightly connected with the elastic film layer (102) through surface tension respectively between the two layers and the elastic film layer. The invention has the advantages of short detection time, low LOD, good repeatability, easy operation, less sample dosage and integration, also has great foreseeable scientific value and economic value.

A pharmaceutical composition useful in the treatment of functional bladder disorders comprising an antimuscarinic agent and a beta-3-adrenoceptor agonist is described.

In its many embodiments, the present invention relates to a novel class of phenylmorpholine and phenylthiomorpholine compounds useful as α2C adrenergic receptor agonists, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the α2C adrenergic receptor agonists using such compounds or pharmaceutical compositions.

The invention discloses an immune colloidal gold detection card for phenylethanolamine A and a preparation method thereof, and relates to the technical field of detection of beta-epinephrine receptor stimulants. A test paper in a shell of a detection card consists of a polyvinyl chloride (PVC) rubber plate, a sample cushion, a colloidal gold combined cushion, a coating membrane and a water sucking cushion, wherein a colloidal gold membrane is a glass cellulose membrane containing a phenylethanolamine A monoclonal antibody; the coating membrane is a nitrocellulose membrane; a line T and a line C are arranged on the coating membrane; the line T coating is provided with a phenylethanolamine A protein conjugate; and the line C is coated with a goat-anti-mouse IgG antibody. The immune colloidal gold detection card is effectively used for rapidly detecting the phenylethanolamine A, so that the detection is convenient and quick, and the detection result is accurate.

This invention involves involves the use of compounds having the following structure:wherein:(a) R is unsubstituted C1-C3 alkanyl or alkenyl; and(b) R' is selected from hydrogen; unsubstituted C1-C3 alkanyl or alkenyl; unsubstituted C1-C3 alkylthio or alkoxy; hydroxy; thiol; cyano; and halo;for preventing or treating of disorders modulated by alpha-2 adrenoceptors.The subject invention also involves novel compounds and compositions.

The invention relates to combinations of an aminosugar and a beta-2-adrenoceptor agonist, such as salbutamol, for the treatment of diseases associated with hypersensivity and inflamation, in particular hypersensivity skin diseases. The aminosugar is preferably a monosaccharide derivative.

It is an objective to produce intermediates of optically active beta-3 adrenaline receptor agonists from readily available raw materials in a safe, efficient and industrially advantageous manner. A substituted acetylpyridine derivative represented by the general formula (9) is reduced by enantioselective reduction to produce an optically active hydroxyethylpyridine derivative represented by the general formula (10) (wherein * represents an asymmetric carbon atom), and it is further derivatized to an intermediate of an optically active beta-3 adrenaline receptor agonist, such as an optically active dihydroxyethylpyridine derivative represented by the general formula (14) or an optically active oxirane derivative represented by the general formula (16).

This invention relates to the use of beta-3-adrenoceptor agonists for the prevention and treatment of kidney damage and / or functional bladder complaints, particularly bladder complaints of neurogenic origin as the result of spinal cord injury.

The invention discloses a potentiometric sensing electrode for testing an adrenergic agonist and a sensor thereof. The sensing electrode comprises an electrode cable, a platinum electrode, an insulating sleeve, an electrode cap, a molecular imprinting membrane and a potential electrode solution; the platinum electrode is arranged in the insulating sleeve, and the electrode cable is drawn out from the upper end portion of the insulating sleeve; an end cap of the electrode cap is in an annular hollow structure, and an inner circle area on the inner side of the end cap is covered with the molecular imprinting membrane provided with a molecular imprinting pore structure; the outer side on the lower end portion of the insulating sleeve is closely sleeved with the electrode cap to fix the molecular imprinting membrane between the electrode cap and the insulating sleeve; and the potential electrode solution immersing at least the lower end of the platinum electrode is poured in the insulating sleeve. According to the potentiometric sensing electrode for detecting the adrenergic agonist and the sensor thereof, the potentiometric sensing electrode uses the molecular imprinting membrane with high peculiarity as a receptor of an electrochemical sensor and has the advantages that the test sensitivity is high, the operation is simple, the sensing electrode is convenient to carry, and the like, and field tests of adrenergic agonists are achieved.

This invention describes a new combination for the treatment of functional bladder disorders which comprises alpha agonists and a beta-3-adrenoceptor agonist.

The invention discloses a zilpaterol immune colloidal gold detection card and a preparation method thereof, and relates to the beta-epinephrine receptor agonist detection technical field. A test strip in an outer shell of the detection card is composed of a PVC rubber plate, a sample pad, a colloidal gold combined pad, a coating film and a water-absorbing pad; a colloidal gold film is a glass cellulose film containing a zilpaterol monoclonal antibody, and the coating film is a nitrocellulose film; a T line and a C line are arranged on the nitrocellulose film, the T line is coated with a zilpaterol-protein conjugate, and the C line is coated with a sheep anti-mouse IgG antibody. The detection card is effectively used for rapid detection of zilpaterol, is convenient and fast, and has accurate results.