74 results about "Serotonin transporter" patented technology

The invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) and/or pathways involving dopamine D1/D2 receptor signaling systems, and/or the treatment of residual symptoms.

The invention relates to particular substituted deuterated heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) and/or pathways involving dopamine D1/D2 receptor signaling systems, and/or the treatment of residual symptoms.

Certain diaryl-substituted tetrahydroisoquinoline compounds are histamine H₃ receptor and/or serotonin transporter modulators useful in the treatment of histamine H₃ receptor- and/or serotonin-mediated diseases.

The gene (SLC6A4) responsible for encoding the serotonin transporter (SERT) has a functional polymorphism at the 5′-regulatory promoter region, which results in two forms, long (L) and short (S). The LL-genotype is hypothesized to play a key role in the early onset of alcohol use. The present invention discloses the differences in treatment and diagnosis based on the L or short genotypes as well as on a single nucleotide polymorphism of the SERT gene, the 3′ UTR SNP rs1042173. The present invention demonstrates the efficacy of using the drug ondansetron and similar drugs for treatment based on diagnosing variations in the polymorphisms of the SERT gene and expression and activity of the SERT gene, as well as methods for diagnosing susceptibility to abuse of alcohol and other addiction-related diseases and disorders, for monitoring treatment and/or abuse (addictive behavior), and for determining which treatment should be used.

The invention relates to the observation that the p38 mitogen-activated protein kinase pathway is an important regulator of biogenic amine transporter (BAT) function. By using modulator of p38 MAPK, one can alter BAT function in a specific manner. This recognition of the pathway and its interaction with the serotonin transporter (SERT) and the norepinephrine transporter (NET), along with the PPA, PKG and PDE pathways, also provides the opportunity to identify polymorphisms that will impact the efficacy of drugs that act though on these enzymes or their pathways.

The invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) and/or pathways involving dopamine D1/D2 receptor signaling systems, and/or the treatment of residual symptoms.

The present invention relates to the use of adenosine type 3 receptor (A3R) modulators to modulate serotonin transporter (SERT) function in vivo. In particular, antagonists of A3R can be used to inhibit A3R-dependent upregulation of SERT, for example, as antidepressants.

The present invention discloses is a method of selecting a drug based on personal genetic information when prescribing an antidepressant for a depressed patient. According to the invention, either a noradrenaline reuptake inhibitor (NRI) antidepressant or a selective serotonin reuptake inhibitor (SSRI) antidepressant can be selected based on the combination of monoamine transporter gene polymorphisms, that is, NET G1287A polymorphism in a norepinephrine transporter (NET) gene, serotonin transporter gene (5-HTT) promoter polymorphism and 5-HTT gene intron 2 polymorphism. Also, based on the norepinephrine transporter gene NET G1287A polymorphism alone, the noradrenaline reuptake inhibitor (NRI) antidepressant can be selected.

The present invention relates to tropane derivatives having particular use for the in vivo detection of dopamine transporters.These derivatives meet the formulain which R1 is I or Sn (R3)3, R2 is for example the methyl group, and X and Y are various substituents.The derivatives with X=CH3 and Y=H show strong specificity for the dopamine transporter compared with the serotonin transporter (74% inhibition when the transporter is previously saturated with GBR 12909).

The invention provides a conjugate comprising (i) a selectivity agent which binds specifically to one or more neurotransmitter transporters selected from the group consisting of a dopamine transporter (DAT), serotonin transporter (SERT) or a norepinephrine transporter (NET) and (ii) a nucleic acid capable of specifically binding to a target molecule which is expressed in the same cell as the neurotransmitter transporter wherein said target molecule is α-synuclein or the mRNA encoding α-synuclein. The conjugates of the present invention are useful for the delivery of the nucleic acid to a cell of interest and thus, for the treatment of diseases which require a down-regulation of the protein encoded by the target nucleic acid as well as for the delivery of imaging agents to the cells for diagnostic purposes.

Disclosed is a method for determination of a smoking trend in a subject which is useful for the assistance or therapy for smoking cessation, which comprises the steps of detecting one or more polymorphisms occurring on one or more genes selected from the genes (1) to (3) or a genome or in the neighborhood of the genes or the genome and determining the smoking trend based on the results of the detection: (1) nicotinic acetylcholine receptor β2 subunit (CHRNB2) gene; (2) serotonin transporter (SLC6A4(5HTT)) gene; and (3) nicotinic acetylcholine receptor α4 subunit (CHRNA4) gene.

The present invention relates to cis-derivatives of formula

wherein

R¹, R², and R³ are as defined herein

and to pharmaceutically acceptable acid addition salts thereof. The compounds of formula I are good inhibitors of the serotonin transporter (SERT inhibitors). By virtue of their efficacy as SERT inhibitors, the compounds of the present invention are particularly useful for the treatment of CNS disorders and psychotic disorders, in particular in the treatment or prevention of depressive states and/or in the treatment of anxiety.

Radiopharmaceutical compounds are disclosed. A tropane compound is linked through the N atom at the 8-position to a chelating ligand capable of complexing technetium or rhenium to produce a neutral labeled complex that selectively binds to the dopamine transporter over the serotonin transporter with a ratio of 10 or more. These compounds can be prepared as separate diastereoisomers as well as a mixture of diastereoisomers. Also disclosed are radiopharmaceutical kits for preparing the labeled radiopharmaceutical compounds.

There is provided a pharmaceutical agent, food, or beverage for treating or preventing a disease or condition that can be ameliorated by inhibiting serotonin reuptake, comprising a clinically-effective amount of (1S,3S)-1-methyl-1,2,3,4-tetrahydro-β-carboline-3-carboxylic acid.

A system for treating addictions includes genetic testing to determine the presence of allelic variants of genes shown to be associated with impulsive/addictive behaviors and a tailored rehabilitation regimen of specific physical exercise, special diet and particular dietary supplements to optimize the way mood elevation is achieved in the patient. The system further includes individual and group counseling and initial oxygen therapy. The genetic testing assesses the presence of gene polymorphism in at least one of D2 dopamine receptor gene (DRD2), dopamine transporter gene (DAT1), dopamine beta-hydroxylase gene (DBH) and serotonin transporter (SERT) gene. The dietary supplements are tailored to stimulate production of neuromediators or neurotransmitters, depending upon the polymorphism determined. The exercises include static and dynamic routines also tailored to the results of the genetic testing. After completion of the inpatient portion of the system, further therapies include daily exercise and dietary supplement programs tailored for each polymorphism discovered.

The present invention relates to trans-derivatives of formula

wherein R¹, R², R³, and the dotted line are as defined herein and to pharmaceutically acceptable acid addition salts thereof.

The compounds of formula I are good inhibitors of the serotonin transporter (SERT inhibitors) and simultaneously, they have good activity on the NK-1 receptor (dual effect). By virtue of their efficacy as SERT inhibitors, the compounds in the present invention are particularly useful for the treatment of CNS disorders and psychotic disorders, in particular in the treatment or prevention of depressive states and/or in the treatment of anxiety.