Sökning: "receptor occupancy"

Visar resultat 1 - 5 av 34 avhandlingar innehållade orden receptor occupancy.

  1. 1. Nonlinear Mixed Effects Methods for Improved Estimation of Receptor Occupancy in PET Studies

    Författare :Matts Kågedal; Mats Karlsson; Andrew C Hooker; Gitte Knudsen; Uppsala universitet; []
    Nyckelord :NATURVETENSKAP; NATURAL SCIENCES; PET; positron emission tomography; receptor occupancy; nonlinear mixed effects; NONMEM; optimal design; dose finding; Pharmacokinetics and Drug Therapy; Farmakokinetik och läkemedelsterapi;

    Sammanfattning : Receptor occupancy assessed by Positron Emission Tomography (PET) can provide important translational information to help bridge information from one drug to another or from animal to man. The aim of this thesis was to develop nonlinear mixed effects methods for estimation of the relationship between drug exposure and receptor occupancy for the two mGluR5 antagonists AZD9272 and AZD2066 and for the 5HT1B receptor antagonist AZD3783. LÄS MER

  3. 2. Role of the Blood-Brain Barrier in Stereoselective Distribution and Delay in H1 Receptor Occupancy of Cetirizine in the Guinea Pig Brain

    Författare :Anubha Gupta; Margareta Hammarlund-Udenaes; Niclas E. Jonsson; Joseph W. Polli; Uppsala universitet; []
    Nyckelord :MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; Pharmacokinetics Pharmacotherapy; Cetirizine enantiomers; Brain distribution; Microdialysis; H1 receptor occupancy; Stereoselective-pharmacokinetics; Farmakokinetik Farmakoterapi; PHARMACY; FARMACI;

    Sammanfattning : Cetirizine, an H1-antihistamine, is prescribed for allergic disorders. It exists as a racemic mixture, with levocetirizine being the active enantiomer. The central nervous system side-effects of H1-antihistamines are caused by their penetration into the brain. LÄS MER

  4. 3. Depot neuroleptic maintenance treatment: clinical, pharmacological and neuropsychological aspects

    Författare :Eva Tuninger; Lund Psykiatri; []
    Nyckelord :MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; clinical psychology; Psychiatry; laterality.; chronic psychosis; schizophrenia; outcome; maintenance treatment; follow-up; longitudinal; neuropsychology; SPECT; auditory hallucinations; dopamine receptor occupancy; psychosomatics; Psykiatri; klinisk psykologi; psykosomatik;

    Sammanfattning : Neuroleptic maintenance treatment is effective to reduce the risk of further episodes of schizophrenia and other chronic psychoses, except affective. Lack of insight often lead to poor compliance to the prescripted medication. Then, neuroleptics might be given as depot injections. LÄS MER

  5. 4. Population Pharmacodynamic Modeling and Methods for D2-receptor Antagonists

    Författare :Klas Petersson; Lena Friberg; Mats Karlsson; An Vermeulen; Robert Bies; Uppsala universitet; []
    Nyckelord :MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; population modeling; schizophrenia; D2-antagonists; pharmacodynamics; drug development;

    Sammanfattning : Early predictions of a potential drug candidate’s time-course of effect and side-effects, based on models describing drug concentrations, drug effects and disease progression, would be valuable to make drug development more efficient. Pharmacodynamic modeling can incorporate and propagate prior knowledge and be used for simulations of different scenarios. LÄS MER

  7. 5. Modulation of nuclear receptor signaling by RBR ubiquitin ligases

    Författare :Nina Gustafsson Sheppard; Karolinska Institutet; Karolinska Institutet; []
    Nyckelord :;

    Sammanfattning : Nuclear receptors (NRs) constitute a superfamily of transcription factors and play important roles in physiology. Transcriptional regulation by NRs can be modulated through interactions with various coregulators that activate or repress transcription through mediating receptor and chromatin modifications as well as communicating with the general transcription factor machinery. LÄS MER