Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as alpha 1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.

Abstract: This invention provides an isolated nucleic acid encoding a mammalian galanin receptor, an isolated galanin receptor protein, vectors comprising isolated nucleic acid encoding a mammalian galanin receptor, cells comprising such vectors, antibodies directed to a mammalian galanin receptor, nucleic acid probes useful for detecting nucleic acid encoding a mammalian galanin receptor, antisense oligonucleotides complementary to unique sequences of nucleic acid encoding a mammalian galanin receptor, nonhuman transgenic animals which express DNA encoding a normal or a mutant mammalian galanin receptor, as well as methods of determining binding of compounds to mammalian galanin receptors.

Abstract: This invention is directed to morpholinone and morpholine derivatives which are selective antagonists for human &agr;1a receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia, sympathetic mediated pain, migraine, and for the treatment of any disease where the antagonism of the &agr;1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

Abstract: This invention is directed to novel imidazole and imidazoline derivatives which are selective agonists for cloned human &agr;2 adrenergic receptors. This invention is also related to the use of these compounds for the treatment of any disease where modulation of the &agr;2 receptors may be useful. The invention further provides for a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

Abstract: This invention is directed to dihydropyrimidine compounds which are selective antagonists for human &agr;1A receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia and for the treatment of any disease where the antagonism of the &agr;1A receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

Abstract: This invention is directed to triazine derivatives which are selective antagonists for a NPY (Y5) receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier.

Abstract: The present invention provides a process for identifying a chemical compound which specifically binds to a rat or human 5-HT4 receptor. The invention also provides a process involving competitive binding for identifying a chemical compound which specifically binds to a rat or human 5-HT4 receptor. The invention provides for a process for determining whether a chemical compound specifically binds to and activates a rat or human 5-HT4 receptor. The invention additionally provides for a process for determining whether a chemical compound specifically binds to and inhibits activation of a rat or human 5-HT4 receptor.

Abstract: This invention provides an isolated nucleic acid encoding a mammalian galanin receptor, an isolated galanin receptor protein, vectors comprising isolated nucleic acid encoding a mammalian galanin receptor, cells comprising such vectors, antibodies directed to a mammalian galanin receptor, nucleic acid probes useful for detecting nucleic acid encoding a mammalian galanin receptor, antisense oligonucleotides complementary to unique sequences of nucleic acid encoding a mammalian galanin receptor, nonhuman transgenic animals which express DNA encoding a normal or a mutant mammalian galanin receptor, as well as methods of determining binding of compounds to mammalian galanin receptors.

Abstract: Photoelectron spectroscopy apparatus are disclosed that comprise a photoelectron detector and that exhibit improved performance of the photoelectron detector and thus more reliable and accurate analysis of photoelectron energy. In performing energy analysis of photoelectrons, the photoelectron detector measures the time distribution at which photoelectrons emitted from a specimen surface traverse a flight tube when the specimen is irradiated with X-rays from a pulse X-ray source. A magnetic field generator is situated near the specimen to collect and collimate photoelectrons emitted from the specimen surface and form a photoelectron flux inside a flight tube.

Abstract: This invention provides methods of modifying feeding behavior, including increasing or decreasing food consumption, e.g., in connection with treating obesity, bulimia or anorexia. These methods involve administration of compounds are selective agonists or antagonists or the Y5 receptor. One such compound has the structure: In addition, this invention provides an isolated nucleic acid molecule encoding a Y5 receptor, an isolated Y5 receptor protein, vectors comprising an isolated nucleic acid molecule encoding a Y5 receptor, cells comprising such acid probes useful for detecting nucleic acid encoding Y5 receptors, antisense oligonucleotides complementary to any unique sequences of a nucleic acid molecule which encodes a Y5 receptor, and nonhuman transgenic animals which express DNA a normal or a mutant Y5 receptor.

Abstract: This invention provides compounds having the structure: wherein each of R1, R2, R3 and R9 is independently H; straight chain or branched, substituted or unsubstituted C1-C7 alkyl, C2-C7 alkenyl or alkynyl; C3-C7 cycloalkyl or cycloalkenyl; acyl, phenyl, substituted phenyl, or heteroaryl; wherein each dashed line represents a single or a double bond as described herein; wherein each of R4, R5 and R6 is independently H, F, Cl, Br, I; straight chain or branched, substituted or unsubstituted C1-C7 alkyl, C2-C7 alkenyl or alkynyl; C3-C7 cycloalkyl or cycloalkenyl; phenyl, substituted phenyl, heteroaryl, —OH, —OR7, —CN, —COR7, —CO2R7, —CON (R7)2,—OCOR7, —SR7,—N(R7)2—NR7COR7, —(CH2)nOR7, —(CH2)n(R7)2, —(CH2)nNR7COR7, wherein n is an integer from 1 to 4; and wherein each of R7 and R8 is independently H; straight chain or branched, substituted or unsubstituted C1-C7 alkyl, C2-C7 alkenyl or alkynyl; phenyl or substituted phe

Abstract: The invention provides a method of treating benign prostatic hyperplasia in a subject which comprises administering to the subject a therapeutically effective amount of a compound having the structure: wherein Y is —(CH2)n—, where n is 1, 2, 3, 4 or 5; —(CH2)h—O—(CH2)k—, where h and k are independently the same or different and are 2, 3 or 4; —(CH2)h—CH═CH—(CH2)k—; or —(CH2)h—C≡C—(CH2)k—, where h and k are independently the same or different and are 1, 2, 3 or 4; wherein Z is O, NH, or CH2; wherein R1 is a linear or branched chain alkyl, alkoxyalkyl or arylalkyl group; wherein R2 and R4 are independently the same or different and are H, or it linear or branched chain alkyl group; wherein R3 is H, a linear or branched chain alkyl, alkoxy, alkoxyalkyl or acyl group; and wherein R5 and R6 are independently the same or different and are H, OH, Cl, Br, F, NO2, CN, CF3, or NH2, or a linear or branched ch

Abstract: This invention is directed to indole and benzothiazole compounds which are selective for cloned human alpha 2 receptors. This invention is also related to uses of these compounds for any indication where use of an alpha 2 agonist may be appropriate. Specifically, this includes use as analgesic, sedative and anaesthetic agents. In addition, this invention includes using such compounds for lowering intraocular pressure, presbyopia, treating migraine, hypertension, alcohol withdrawal, drug addiction, rheumatoid arthritis, ischemic pain, spasticity, diarrhea, nasal decongestion, urinary incontinence as well as for use as cognition enhancers and ocular vasoconstriction agents. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

Abstract: This invention provides an isolated nucleic acid molecule encoding a mammalian 5-HT4B receptor and an isolated nucleic acid molecule encoding a human 5-HT4B receptor, an isolated protein which is mammalian 5-HT4B receptor, vectors comprising an isolated nucleic acid molecule encoding a mammalian 5-HT4B receptor, vectors comprising an isolated nucleic acid molecule encoding a human 5-HT4B receptor, mammalian cells comprising such vectors, antibodies directed to the 5-HT4B receptor, nucleic acid probes useful for detecting nucleic acid encoding a mammalian or human 5-HT4B receptor, antisense oligonucleotides complementary to any sequences of a nucleic acid molecule which encodes a mammalian or human 5-HT4B receptor, pharmaceutical compounds related to the human 5-HT4B receptor. This invention further provides methods for determining ligand binding, detecting expression, drug screening, and treatments for alleviating abnormalities associated with a human 5-HT4B receptor.

Abstract: This invention is directed to novel imidazole and imidazoline derivatives which are selective agonists for cloned human &agr;2 adrenergic receptors. This invention is also related to the use of these compounds for the treatment of any disease where modulation of the &agr;2 receptors may be useful. The invention further provides for a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

Abstract: This invention provides isolated nucleic acids encoding a mammalian GABABR2 polypeptide, an isolated GABABR2 protein, vectors comprising isolated nucleic acid encoding mammalian GABABR2 polypeptides, cells expressing mammalian GABABR1/R2 receptors, antibodies directed to an epitope on mammalian GABABR2 polypeptides or mammalian GABABR1/R2 receptors, nucleic acid probes useful for detecting nucleic acids encoding mammalian GABABR2 polypeptides, antisense oligonucleotides complementary to unique sequences of nucleic acids encoding mammalian GABABR2 polypeptides, nonhuman transgenic animals which express DNA encoding normal or mutant mammalian GABABR1/R2 receptors, as well as methods of screening compounds acting as agonists or antagonists of mammalian GABABR1/R2 receptors.

Abstract: This invention provides an isolated nucleic acid encoding a human MCH1 receptor, a purified human MCH1 receptor, vectors comprising isolated nucleic acid encoding a human MCH1 receptor, cells comprising such vectors, antibodies directed to a human MCH1 receptor, nucleic acid probes useful for detecting nucleic acid encoding human MCH1 receptors, antisense oligonucleotides complementary to unique sequences of nucleic acid encoding human MCH1 receptors, transgenic, nonhuman animals which express DNA encoding a normal or mutant human MCH1 receptor, methods of isolating a human MCH1 receptor, methods of treating an abnormality that is linked to the activity of a human MCH1 receptor, as well as methods of determining binding of compounds to mammalian MCH1 receptors.

Abstract: This invention provides an isolated nucleic acid encoding a mammalian galanin receptor, an isolated galanin receptor protein, vectors comprising isolated nucleic acid encoding a mammalian galanin receptor, cells comprising such vectors, antibodies directed to a mammalian galanin receptor, nucleic acid probes useful for detecting nucleic acid encoding a mammalian galanin receptor, antisense oligonucleotides complementary to unique sequences of nucleic acid encoding a mammalian galanin receptor, nonhuman transgenic animals which express DNA encoding a normal or a mutant mammalian galanin receptor, as well as methods of determining binding of compounds to mammalian galanin receptors.

Abstract: This invention is directed to dihydropyrimidines which are selective antagonists for human &agr;1a receptors. This invention is also related to uses of these compounds for relaxing lower urinary tract tissue, treating benign prostatic hyperplasia and for the treatment of any disease where the antagonism of the &agr;1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

Abstract: This invention is directed to dihydropyrimidine compounds of the following formula: which are selective antagonists for human &agr;1C receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotence, cardiac arrhythmia and for the treatment of any disease where antagonism of the &agr;1C receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.