Abstract: The invention relates to methods for the treatment of central nervous system disorders, neurological disorders, gastrointestinal disorders, drug abuse, angina, migraine, hypertension and depression by administering a pharmaceutical composition comprising an effective amount of certain sigma receptor ligands to a patient in need of such treatment. The invention further relates to novel sigma receptor ligands having high binding to the sigma receptor and pharmaceutical compositions thereof.

Abstract: The invention relates to a method of treating alcoholism and alcohol dependence in a mammal comprising administering to the mammal a therapeutically effective amount of a synergistic combination of: (i) at least one opioid antagonist, and (ii) at least one selective serotonin reuptake inhibitor. The invention also relates to compositions and kits containing the same.

Abstract: A method of treating atherosclerosis, independent of lipid lowering, in mammals, induding humans, in need of treatment by inhibiting progression of an atherogenic lesion or by stabilizing plaque. Such lesion progression inhibition or plaque stabilization is preferably achieved by directly inhibiting chemokine expression leading to excessive inflammatory cell recruitment by administering certain estrogen agonist/antagonists.

Abstract: The present invention provides a method for producing a potentiating effect on a therapeutic action of an agent which is selected from a serotonin re-uptake inhibitor, a norepinephrine re-uptake inhibitors, both a serotonin and norepinephrine re-uptake inhibitor, and an atypical antidepressant in a warm blooded mammal, which comprises administering to said mammal an effective amount of moxonidine, or a pharmaceutically acceptable salt thereof.

Abstract: Methods are provided for conducting surgical procedures in a patient wherein, during the surgical procedure, autonomous ventricular electrical conductivity and escape beats are reversibly and transiently suppressed to facilitate the surgical procedure. Also provided are compositions which are capable of inducing ventricular asystole in a patient. The compositions may include an AV node blocker. In one embodiment, compositions including an atrioventricular (AV) node blocker and a .beta.-blocker are provided, wherein the .beta.-blocker is present in an amount sufficient to substantially reduce the amount of AV node blocker required to induce ventricular asystole in the patient. The compositions and methods may be used for inducing temporary ventricular asystole in a beating heart, and to facilitate the performance of a variety of surgical techniques, including minimally invasive microsurgical techniques.

Abstract: The invention relates to methods for the treatment of central nervous system disorders, gastrointestinal disorders, drug abuse, angina, migraine, hypertension and depression by administering a pharmaceutical composition comprising an effective amount of certain sigma receptor ligands to a patient in need of such treatment. The invention further relates to novel sigma receptor ligands having high binding to the sigma receptor and pharmaceutical compositions thereof. Unexpectedly, certain of the sigma receptor ligands of the present invention have selectivity for the sigma receptor over the DA, PCP and 5-HT.sub.1A receptors.

Abstract: This invention relates to compounds that are antagonists of dopamine D4 receptors, and to methods of treating psychosis and schizophrenia using a compound that is an antagonist of dopamine D4 receptors.

Abstract: Disclosed herein is a method for treating depression associated with alcoholism in a patient comprising administering to the patient a pharmacologically effective dose of an opioid antagonist, and a pharmacologically effective dose of at least one drug compound selected from the group consisting of a tricyclic antidepressant, an a-typical antidepressant, and lithium.

Abstract: Norepinephrine reuptake inhibitors are used to treat oppositional defiant disorder.

Abstract: The present invention features calcilytic compounds. "Calcilytic compounds" refer to compounds able to inhibit calcium receptor activity. Also described are the use of calcilytic compounds to inhibit calcium receptor activity and/or achieve a beneficial effect in a patient; and techniques which can be used to obtain additional calcilytic compounds.

Abstract: Method and compositions for treating a patient having a neurological disease or disorder, such as stroke, head trauma, spinal cord injury, spinal cord ischemia, ischemia- or hypoxia-induced nerve cell damage, epilepsy, anxiety, neuropsychiatric or cognitive deficits due to ischemia or hypoxia such as those that frequently occur as a consequence of cardiac surgery under cardiopulmonary bypass, or neurodegenerative diseases such as Alzheimer's Disease, Huntington's Disease, Parkinson's Disease, or amyotrophic lateral sclerosis (ALS).

Abstract: The present invention describes certain alkyloxyamino-substituted fluorenones which inhibit protein kinase C, as well as pharmaceutical compositions including these compounds and methods of using these compounds to control protein kinase C activity in mammals, including humans. More specifically, the present compounds are useful for the treatment of neoplastic disease states, disorders associated with abnormal blood flow (including hypertension, ischemia, atherosclerosis, coagulation disorders), and inflammatory diseases (including immune disorders, asthma, lung fibrosis, and psoriasis).

Abstract: Disclosed are dopamine agonist and opioidergic compositions and methods for their use in the treatment of alcoholism. The invention discloses compounds and therapeutic kits useful in the treatment of alcoholics having the A1 allele of the dopamine receptor D2 gene. Also disclosed are methods of treating alcoholics having the A1/A1 or A1/A2 DRD2 genotype comprising administration of dopamine agonists such as aporphines, ergolines, related compounds, and their analogs, in combination with opioidergic compounds such as naloxone.

Abstract: A class of substituted phenoxy naphthalene compounds of the structure: ##STR1## where n is 2 or 3; R.sup.1 is hydrogen, hydroxy, C.sub.1 -C.sub.4 alkoxy, phenoxycarbonyl, C.sub.1 -C.sub.6 alkoxycarbonyl, or C.sub.2 -C.sub.6 alkoxy-sulfonyl; R.sup.2 is is hydrogen, hydroxy, C.sub.1 -C.sub.4 alkoxy, phenoxycarbonyl, C.sub.1 -C.sub.6 alkoxycarbonyl, or C.sub.2 -C.sub.6 alkoxy-sulfonyl, or halo; and R.sup.3 is 1-piperidinyl, 1-pyrollidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; are useful in the treatment of pathological conditions associated with post-menopause including osteoporosis, endometriosis, uterine fibroid disease, cardiovascular disease (particularly hyperlipidemia), and hormonally-dependent cancers (particularly breast and uterine cancer).

Abstract: The invention provides benzo[b]thiophene compounds, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions including hyperlipidemia and related cardiovascular pathologies.

Abstract: The invention provides a method of treating heart failure. The method comprises administering a positive inotropic agent and a .beta.-adrenergic receptor antagonist in a specific manner.

Abstract: The present invention provides a class of substituted indene compounds and their pharmaceutically acceptable salts which possess selective estrogen receptor modulator (SERM) activity and are thus useful in the treatment of osteoporosis and cardiovascular disease, particularly hyperlipidemia in women. The compounds possess the structure ##STR1## in which R.sup.1 is hydrogen, hydroxy, alkoxy, phenylcarbonyloxy, alkylcarbonyloxy, or alkylsulfonyloxy. R.sup.2 is hydrogen, hydroxy, halo, alkoxy, phenylcarbonyloxy, alkylcarbonyloxy, or alkylsulfonyloxy. R.sup.3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexa-methyleneimino, and n is 2 or 3. The dashed line bond between the carbon atoms at positions 1 and 2 of the indene nucleus represent an optional double bond with the proviso that when the double bond is absent, the parenthetic hydroxy group at position 1 is present and vice versa.

Abstract: The present invention concerns the use of receptor antagonists of the 5HT4 receptor for avoiding, alleviating, suppressing or overcoming the gastrointestinal side-effects of serotonin reuptake inhibitors. The present invention also concerns pharmaceutical formulations comprising 5HT4-receptor antagonists for alleviating, suppressing or overcoming the gastrointestinal side-effects of serotonin reuptake inhibitors, as well as pharmaceutical compositions comprising 5HT4 receptor antagonists and serotonin reuptake inhibitors.

Abstract: Methods of treating painful neuropathies are provided comprising administering compounds comprising the (S)-isomer of chiral compounds having the formula: ##STR1## wherein R1 is C1-C5 hydrocarbyl, R2 and R3 are independently C1-C5 hydrocarbyl or H, R4 is C1-C5 hydrocarbyl, R3 and R4 may optionally be joined together to form a 5, 6 or 7 membered ring system, or a pharmaceutically acceptable salt thereof, substantially free of the (R)-isomer.

Abstract: Preeclampsia and preterm labor in a pregnant female mammal are treated by administering thereto a combination of a progestin and a nitric oxide synthase substrate, a nitric oxide donor or both, optionally in further combination with one or more of a cyclooxygenase inhibitor, a PGI.sub.2 -mimetic, a thromboxane (TXA.sub.2) inhibitor, a compound possessing TXA.sub.2 -agonistic and TXA.sub.2 -inhibiting properties, a compound possessing TXA.sub.2 -antagonistic and PGI.sub.2 -memetic activities, and a TXA.sub.2 antagonist.

Abstract: Stimulating non-amyloidogenic processing by the activation of cell surface serotonin receptors linked to phospholipase and protein kinase C is described. Activation of the cell surface serotonin receptors is accomplished by contacting the cell with an agent which is a serotonin agonist or which increases the intrasynaptic concentration of serotonin. Also described is the activation of cell surface serotonin receptors by dexnorfenfluramine. Agents which cause the activation of cell surface serotonin receptors can be administered to an individual to stimulate non-amyloidogenic processing in the brain of the individual, thereby inhibiting the deposition of amyloid in the brain of the individual.

Abstract: Dysmenorrhea, disfunctional uterine bleeding, preterm labor and postpartum labor in female mammals are treated by inhibiting uterine contractility by administering thereto a nitric oxide synthase substrate, a nitric oxide donor or both, optionally in combination with one or more of a prostaglandin inhibitor, a prostacyclin-mimetic, a progestin, an oxytocin antagonist or a .beta.-agonist in an amount effective to ameliorate the symptoms thereof; and inadequate menses treated and induction of abortion or stimulation of labor in a pregnant female is achieved by uterine contractility stimulation by administering thereto a nitric oxide inhibitor, either alone or optionally in a combination of progesterone antagonist, an oxytocin or oxytocin analogue antagonist or a prostaglandin.

Abstract: The invention relates to a method of treating alcoholism and alcohol dependence in a mammal comprising administering to the mammal a therapeutically effective amount of a synergistic combination of: (i) at least one opioid antagonist, and (ii) at least one selective serotonin reuptake inhibitor. The invention also relates to compositions and kits containing the same.

Abstract: The present invention provides a method for preventing or decreasing diarrhea associated with irinotecan administration comprising the administration of tamoxifen at least two cell cycles prior to irinotecan administration.

Abstract: The present invention provides dihalopropene compounds of the general formula: ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.10 alkyl or the like; L is C(.dbd.O)NH or the like; R.sub.2, R.sub.3 and R.sub.4 are independently halogen or the like; R.sub.5, R.sub.6 and R.sub.7 are independently hydrogen or the like; m is an integer of 0 to 4; n is an integer of 0 to 2; X is chlorine or the like; Y is oxygen or the like; and Z is oxygen or the like, which have excellent insecticidal activity so that they are satisfactorily effective for the control of noxious insects.

Abstract: Dysmenorrhea, disfunctional uterine bleeding, preterm labor and postpartum labor in female mammals are treated by inhibiting uterine contractility by administering thereto a nitric oxide synthase substrate, a nitric oxide donor or both, optionally in combination with one or more of a prostaglandin inhibitor, a prostacyclin-mimetic, a progestin, an oxytocin antagonist or a .beta.-agonist in an amount effective to ameliorate the symptoms thereof; and inadequate menses treated and induction of abortion or stimulation of labor in a pregnant female is achieved by uterine contractility stimulation by administering thereto a nitric oxide inhibitor, either alone or optionally in a combination of progesterone antagonist, an oxytocin or-oxytocin analogue antagonist or a prostaglandin.

Abstract: TGF-beta activators and TGF-beta production stimulators are employed to prevent or treat conditions characterized by inappropriate proliferation of smooth muscle cells, such as the prevention or reduction of restenosis following angioplasty or other vascular trauma. Such TGF-beta activators and production stimulators inhibit abnormal proliferation of smooth muscle cells. TGF-beta activators or production stimulators that are not characterized by an undesirable systemic toxicity profile at a prophylactic dose are also amenable to chronic use for prophylactic purposes with respect to disease states involving proliferation of vascular smooth muscle cells over time. Further provided is a method for upregulating cellular mRNA coding for TGF-beta.

Abstract: A 1,2-ethanediol derivative represented by the general formula ?I! or its salt: ##STR1## has a NGF activity-potentiating effect and is useful as a remedy for various diseases caused by degeneration of central nervous system or peripheral nervous system such as senile dementia of Alzheimer type, Huntington's chorea, various neuropathies, Riley-Day syndrome, traumatic nerve injury, amyotrophic lateral sclerosis (ALS) and the like.

Abstract: A new use of halogenated triphenylethylene derivatives for lowering levels of serum lipid perioxides and for the prevention or treatment of oxidative tissue damage induced by lipid peroxidation is disclosed. The new use includes the prevention or treatment of atherosclerosis, ischemic injury, psoriasis, inflammatory diseases, such as inflammatory bowel disease, or cardiovascular disorders, such as coronary heart disease, cardiac ischemic injury and post-ischemic cardiac arrhythmias, or the treatment of AIDS.

Abstract: A lacrimation accelerating agent containing a ligand of serotonin receptor as an active ingredient. Also provided is a method for preventive and/or therapeutic treatment of a disease caused by a deficiency of lacrimal fluid such as dry eye, which comprises the step of administering to a mammal an effective amount of a ligand of a serotonin receptor such as sarpogrelate hydrochloride.

Abstract: The optically pure R(-) isomer of salmeterol, which is substantially free of the S(+) isomer, is a potent bronchodilator for relieving the symptoms associated with asthma in individuals. A method is disclosed utilizing the optically pure R(-) isomer of salmeterol for treating asthma while minimizing toxicity and other side effects associated with salmeterol.

Abstract: The present invention pertains to the field of pain management in medicine. Methods for treating reflex sympathetic dystrophy (including causalgia) are provided, in which a haloalkylamine a adrenergic blocking agent and a local anesthetic are administered to the affected limb by intravenous regional block. Formulations which can be used in these methods are also provided. In a preferred embodiment, phenoxybenzamine and either lidocaine or procaine are administered to the affected limb using a Bier block procedure.

Abstract: The invention provides naphthofluorene compounds, intermediates, formulations, processes, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, cardiovascular-related pathological conditions, including hyperlipidemia, and estrogen-dependent cancer.

Abstract: The present invention provides novel compounds such as certain aryloxy indanamines which are useful as anti-depressants and as inhibitors of synaptic norepinephrine and serotonin uptake. The present invention also provides an improvement in the treatment of depression which comprises inhibiting synaptic serotonin and epinepherine uptake.

Abstract: Prostate cancer particularly hormone-unresponsive metastatic prostate cancer, is treated by cyclophosphamide or other normally substantially inactive agent. Potentiation of the anti-cancer activity and amelioration of cyclophosphamide-associated toxicity is achieved by an initial intravenous infusion of DPPE over an approximately one hour period prior to cyclophosphamide treatment.

Abstract: Methods are disclosed for increasing the effectiveness of dextromethorphan in treating chronic or intractable pain, for treating tinnitus and for treating sexual dysfunction comprising administering dextromethorphan in combination with a therapeutically effective dosage of a debrisoquin hydroxylase inhibitor. A preferred combination is dextromethorphan and the oxidative inhibitor quinidine.

Abstract: The in vivo chemotherapeutic treatment of cancer cells in a living animal is improved by first administering to the animal, a compound which inhibits normal cell proliferation while promoting malignant cell proliferation, specifically a potent antagonist selective for intracellular histamine receptors, in an amount sufficient to inhibit the binding of intracellular histamine to the receptors in normal and malignant cells. An enhanced toxic effect on the cancer cells from the chemotherapeutic agent is obtained while any adverse effect of the chemotherapeutic agent on normal cells, particularly bone marrow and gastro-intestinal cells, is inhibited. In addition, long term continuous administration of the antagonist following administration of the chemotherapeutic agent results in at least amelioration of adverse side effects of chemotherapy on normal bone marrow and gastro-intestinal cells.

Abstract: TGF-beta activators and TGF-beta production stimulators are employed to maintain or increase vessel lumen diameter in a diseased or injured vessel of a mammal. Conditions such as restenosis following angioplasty, vascular bypass grafts, transplanted organs, atherosclerosis or hypertension are characterized by a reduced vessel lumen diameter. In a preferred embodiment of the invention, TGF-beta activators and production stimulators inhibit abnormal proliferation of smooth muscle cells. TGF-beta activators or production stimulators that are not characterized by an undesirable systemic toxicity profile at a prophylactic dose are also amenable to chronic use for prophylactic purposes with respect to disease states involving proliferation and/or migration of vascular smooth muscle cells over time.

Abstract: The present invention provides a composition of matter for the treatment of non-melanoma cancers, wherein said composition comprises a platinum anti-neoplastic compound and tamoxifen, wherein said platinum anti-neoplastic compound and tamoxifen exert a synergistic anti-tumor effect on said non-melanoma cancer. Also provided are various methods of treating non-melanoma cancers and methods of preventing or overcoming resistance to platinum-containing anti-neoplastic compounds.

Abstract: A method of determining the effects of administering a psychoactive compound, such as a drug, on a patient's brain using imaging techniques with position emission tomography (PET) is disclosed. The method measures cerebral metabolism before and after administering the compound, and employs a behavioral clamp to control behavioral influences on the patient's brain after administration of the compound. The method also includes transportation of image data into standard computer space and statistical procedures for volumetrically determining areas of treatment effects.

Abstract: This invention relates to a composition and method for treating depression by administering to a patient a pharmacologically effective dose of an opioid antagonist having a pentacyclic nucleus structurally analogous to naltrexone, and a pharmacologically effective dose of a nontricyclic antidepressant

Abstract: The invention describes a method and composition for treating obesity or related disorders in animals using an anorectic agent and dehydroepiandrosterone (DHEA). The composition effectively diminishes caloric intake, may alter metabolism, weight gain, or a combination thereof.

Abstract: This is a new therapy and method used to treat moderate and severe exogenous obesity by combining generic phentermine with an SSRI (selective serotonin reuptake inhibitor) drug in specific doses for a brief or even a long duration, 12 months or more. The preferred drugs for the combination are fluoxetine hydrochloride(Prozac), sertraline (Zoloft), fluvoxamine maleate (Luvox) and trazodone hydrochloride (Desyrel).

Abstract: Methods of treating Parkinson's disease in a human by administering an effective amount of at least one monoamine oxidase (MAO) A inhibitor by a nasal, intrapulmonary or parenteral routes are disclosed. Reversible or irreversible MAO A inhibitors, or non-selective MAO inhibitors, can be used, and more than one MAO A inhibitor can be administered concurrently. The MAO A inhibitor can be administered in conjunction with other drugs, such as MAO B inhibitors.

Abstract: There is disclosed a method for treating certain psychiatric symptoms including anger, rejection sensitivity and a lack of mental or physical energy with administration of a nontoxic dose of a serotonin re-uptake blocker. Preferably, the serotonin re-uptake blocker is fluoxetine or norfluoxetine.

Abstract: TGF-beta activators and TGF-beta production stimulators are employed to prevent or treat conditions characterized by inappropriate proliferation of smooth muscle cells, such as the prevention or reduction of restenosis following angioplasty or other vascular trauma. Such TGF-beta activators and production stimulators inhibit abnormal proliferation of smooth muscle cells. TGF-beta activators or production stimulators that are not characterized by an undesirable systemic toxicity profile at a prophylactic dose are also amenable to chronic use for prophylactic purposes with respect to disease states involving proliferation of vascular smooth muscle cells over time. Further provided is a method for upregulating cellular mRNA coding for TGF-beta.

Abstract: A method for treating or preventing cardiovascular pathologies by administering a compound of the formula (I): ##STR1## wherein Z is C.dbd.O or a covalent bond; Y is H or O(C.sub.1 -C.sub.4)alkyl, R.sup.1 and R.sup.2 are individually (C.sub.1 -C.sub.4)alkyl or together with N are a saturated heterocyclic group, R.sup.3 is ethyl or chloroethyl, R.sup.4 is H or together with R.sup.3 is --CH.sub.2 --CH.sub.2 -- or --S--, R.sup.5 is I, O(C.sub.1 -C.sub.4)alkyl or H and R.sup.6 is I, O(C.sub.1 -C.sub.4)alkyl or H with the proviso that when R.sup.4, R.sup.5, and R.sup.6 are H, R.sup.3 is not ethyl; or a pharmaceutically acceptable salt thereof, effective to activate or stimulate production of TGF-beta to treat and/or prevent conditions such as atherosclerosis, thrombosis, myocardial infarction, and stroke is provided. Useful compounds include idoxifene and salts thereof. Further provided is a method for identifying a compound that is a TGF-beta activator or production stimulator is provided.

Abstract: The in vivo chemotherapeutic treatment of cancer cells in a living animal is improved by first administering to the animal, a compound which inhibits normal cell proliferation while promoting malignant cell proliferation, specifically a potent antagonist selective for intracellular histamine receptors, in an amount sufficient to inhibit the binding of intracellular histamine to the receptors in normal and malignant cells. An enhanced toxic effect on the cancer cells from the chemotherapeutic agent is obtained while any adverse effect of the chemotherapeutic agent on normal cells, particularly bone marrow and gastro-intestinal cells, is inhibited. In addition, long term continuous administration of the antagonist following administration of the chemotherapeutic agent results in at least amelioration of adverse side effects of chemotherapy on normal bone marrow and gastro-intestinal cells.

Abstract: There is disclosed a method for treating Late Luteal Phase Dysphoric Disorder with administration of a nontoxic dose of a serotonin re-uptake blocker. Preferably, the serotonin re-uptake blocker is fluoxetine or norfluoxetine.

Abstract: Urinary incontinence in humans is treated by administration of venlafaxine or a compound chosen from a series of aryloxy propanamines.