Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UNIPROT:P08908 (5-HT1A)
 5,574 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The augmentation of serotonin (5-HT) neurotransmission attenuates alcohol consumption, whereas depletion enhances use. A number of serotonin-specific pharmacological probes appear to be effective in reducing the voluntary consumption of alcohol. The 5-HT1A receptor agonist buspirone is an anxiolytic which has been shown to diminish the desire to consume alcohol in anxious alcoholic patients. Thus, serotonin may represent a common denominator for a spectrum of behavioural disorders including anxiety and alcoholism. Novel serotonin drugs, such as the azapirones, may usefully supplement conventional treatment strategies for substance abuse.
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PMID:Anxiety and alcoholism: a serotonin link. 184 Jul 61

Substance abuse worsens the course of schizophrenia and significantly impairs the relationship between the patient and the health care team. Recent advances in laboratory studies of substance abuse and the pharmacology of schizophrenia open up new possibilities for pharmacotherapy of substance abuse in schizophrenia patients. D1 dopaminergic receptor agonists may directly block the drive for stimulant use. D2 dopaminergic receptor antagonists may indirectly block the drive for stimulant and nicotine use, while opioid antagonists appear to reduce the drive to use alcohol. New generations of neuroleptics with serotonin (5-HT2) receptor antagonism and/or 5-HT1A agonist activity may reduce substance abuse in schizophrenia patients who self-medicate negative symptoms or neuroleptic side effects. Pharmacotherapy efficacy may be enhanced by adding contingency management, social skills training, and other manualized programs. Tables are provided of potentially useful medications. Preliminary results are presented of cocaine-abusing schizophrenia patient treated with desipramine and traditional neuroleptics.
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PMID:Pharmacotherapy of schizophrenia patients with comorbid substance abuse. 916 32

While multiple lines of evidence implicate the 5-HT1A receptor in the pathophysiology of anxiety and depression as well as in the mechanism of action of anxiolytics/antidepressants, its relevance to the therapeutic effectiveness of these drugs has been a matter of considerable debate (for review see Griebel, 1995; Hensler, 2003; Hjorth et al., 2000; Lesch et al., 2003). In the current issue of the International Journal of Neuropsychopharmacology, however, both Serretti et al. (2004) and Lemonde et al. (2004) make a strong argument for contribution of a functional 5-HT1A receptor gene variant in the pharmacogenetics of antidepressant treatment with prototypic tricyclics and selective serotonin reuptake inhibitors (SSRIs). Furthermore, the third study in this series by Huang and associates (2004) reveals an association of allelic variation of 5-HT1A receptor expression in a wide spectrum of psychopathology including schizophrenia, substance abuse, and panic disorder. Not unexpectedly, the failure to detect a consistent effect of this gene variation on 5-HT1A receptor functionality in the mature brain as indicated by both receptor binding in post-mortem brain and in-vivo receptor responsivity further supports a critical role of the 5-HT1A receptor in engineering neurodevelopmental processes which may have the potential to set the stage for the brain's permissiveness for psychopathology in later life. The availability of an increasing number of functional gene variants within the serotonergic pathway together with integration of emerging concepts of developmental genetics of complex traits will provide the groundwork for the molecular dissection of syndromal dimensions and treatment response.
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PMID:Focus on The 5-HT1A receptor: emerging role of a gene regulatory variant in psychopathology and pharmacogenetics. 1545 11

Quetiapine is an atypical antipsychotic approved by the FDA (Food and Drug Administration) for use in the treatment of schizophrenia, acute mania, and bipolar depression. Pharmacologically, it has antagonistic effects on serotonin 5-HT1A and 5-HT2A, dopamine D1 and D2, histamine H1, and adrenergic alpha1 and alpha2 receptors. In addition to reports of its use in schizophrenia and bipolar disorder, many studies have examined the use of quetiapine in the treatment of anxiety disorders and substance use disorders. In the treatment of patients with psychotic or bipolar disorder with a comorbid substance abuse disorder even though quetiapine was prescribed primarily for the treatment of the underlying psychotic symptoms, patients taking this medication reported a significant reduction in substance use. Yet, there are also case reports of quetiapine abuse and dependence; in particular among prisoners and patients diagnosed with substance abuse. Though quetiapine should be used peroral, it is also used intranasally and intravenously in these patient groups. Moreover, in some cases quetiapine is combined with other substances, such as cocaine or marijuana, to increase sedation. This abuse of quetiapine is thought to occur due to the anxiolytic and sedative effects of the drug. There are no controlled studies on quetiapine dependence in the literature and it remains unknown whether or not quetiapine causes dependence. This review aimed to present all published case reports on quetiapine abuse and to discuss the possible mechanisms that underlie its abuse and dependence.
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PMID:[Quetiapine in substance use disorders, abuse and dependence possibility: a review]. 2051 67

Aripiprazole is an atypical antipsychotic used for schizophrenia, manic and mixed episodes associated with bipolar I disorder and as adjunctive therapy for major depressive disorder. It functions as a partial agonist at dopamine D2 and 5-HT1A receptors, and as an antagonist at the 5-HT2A receptor. The most recent results obtained from scientific research showed that dopaminergic mechanisms are involved in motivation, reward, and reinforcement of substance abuse. The use of aripiprazole and partial dopamine agonists could represent a novel strategy for normalizing dopamine neurotransmission. Many studies in the last few years have highlighted aripiprazole as a potential candidate for the treatment of different types of substance dependence. This review aims to describe recent scientific research using aripiprazole in different substance abuse disorders (i.e., alcoholism, cocaine, amphetamine and nicotine use). Furthermore, the efficacy of aripiprazole compared to other pharmacological therapies will be described. Given the low number of studies, the frequent absence of placebo or active comparators, and the low statistical power of the studies, a clear conclusion about the use of aripiprazole in alcohol/substance dependence cannot be drawn. Therefore, we suggest the need for further studies, preferably randomized and placebo-controlled.
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PMID:Aripiprazole, alcohol and substance abuse: a review. 2310 50

Bipolar disorder is a pernicious illness. Compared with the later-onset form, early onset bipolar disorder is associated with worse psychosocial outcomes, and is characterized by rapid cycling and increased risks of substance abuse and suicide attempts. Controlling mood episodes and preventing relapse in this group of pediatric patients requires careful treatment. Here, we review the effectiveness of aripiprazole for bipolar disorder in children and adolescents, with discussion of this drug's unique pharmacological profile and various clinical study outcomes. Aripiprazole acts as a serotonin 5-HT2A receptor antagonist, as well as a partial agonist of the serotonin 5-HT1A and dopamine D2 receptors. It can be safely used in children and adolescents, as it is highly tolerated and shows lower rates of the side effects typically observed with other antipsychotic drugs, including sedation, weight gain, hyperprolactinemia, and extrapyramidal syndrome. The presently reviewed randomized controlled trials (RCTs) and non-RCTs generally reported aripiprazole to be effective and well-tolerated in children and adolescents with bipolar disorder. However, due to the limited number of RCTs, the present conclusions must be evaluated cautiously. Furthermore, aripiprazole cannot yet be considered a preferred treatment for children and adolescents with bipolar disorder, as there is not yet evidence that aripiprazole shows greater efficacy compared to other second-generation antipsychotics. Additional data are needed from future head-to-head comparison studies.
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PMID:Profile of aripiprazole in the treatment of bipolar disorder in children and adolescents. 2547 24

We here describe a multimodality neuroimaging containing data from healthy volunteers and patients, acquired within the Lundbeck Foundation Center for Integrated Molecular Brain Imaging (Cimbi) in Copenhagen, Denmark. The data is of particular relevance for neurobiological research questions related to the serotonergic transmitter system with its normative data on the serotonergic subtype receptors 5-HT1A, 5-HT1B, 5-HT2A, and 5-HT4 and the 5-HT transporter (5-HTT), but can easily serve other purposes. The Cimbi database and Cimbi biobank were formally established in 2008 with the purpose to store the wealth of Cimbi-acquired data in a highly structured and standardized manner in accordance with the regulations issued by the Danish Data Protection Agency as well as to provide a quality-controlled resource for future hypothesis-generating and hypothesis-driven studies. The Cimbi database currently comprises a total of 1100 PET and 1000 structural and functional MRI scans and it holds a multitude of additional data, such as genetic and biochemical data, and scores from 17 self-reported questionnaires and from 11 neuropsychological paper/computer tests. The database associated Cimbi biobank currently contains blood and in some instances saliva samples from about 500 healthy volunteers and 300 patients with e.g., major depression, dementia, substance abuse, obesity, and impulsive aggression. Data continue to be added to the Cimbi database and biobank.
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PMID:The Center for Integrated Molecular Brain Imaging (Cimbi) database. 2589 75