Neuropharmacology and analgesiaCentral benzodiazepine receptor occupancy by zolpidem in the human brain as assessed by positron emission tomography
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2010, Pharmacology and TherapeuticsTarget site occupancy: Emerging generalizations from clinical and preclinical studies
2009, Pharmacology and TherapeuticsCitation Excerpt :11C]Flumazenil PET studies with GABAA BZD site ligands demonstrate that ion channel positive allosteric modulators (PAMs, which serve to increase responses to agonists) can require very little target occupancy to elicit a therapeutic effect. Human volunteer studies with clinically-relevant doses of the GABAA PAMs alprazolam, zolpidem and lorazepam, which all demonstrate high levels of intrinsic activity, showed 16%, 26–29% and 5.6% receptor occupancies, respectively (Abadie et al., 1996; Fujita et al., 1999; Lingford-Hughes et al., 2005 and Fig. 6). Therapeutically relevant doses of lorazepam have also been shown to produce negligible occupancy in non-human primate studies using [123I]iomazenil SPECT (Sybirska et al., 1993) and [11C]flumazenil micro-PET (Atack et al., 2007).
In Vivo Characterization and Dynamic Receptor Occupancy Imaging of TPA023B, an α2/α3/α5 Subtype Selective γ-Aminobutyric Acid-A Partial Agonist
2008, Biological PsychiatryCitation Excerpt :Moreover, up to 20% differences in plasma concentration for this drug are present with comparable receptor occupancy, showing that direct determination of VT on the basis of receptor imaging data might be a more suitable outcome parameter with less intersubject variability. The fact that TPA023B was well-tolerated even at relatively high (50%) levels of occupancy contrasts with classical BZP-site agonists in which therapeutic benefits are observed at low levels of occupancy of, for example, lorazepam (<10%) (34) and sedation is seen in the region of 35% or less for midazolam (30), 24% for diazepam (35), 15%–24% for clonazepam (36), or 21% for zolpidem (37). These data clearly, therefore, highlight the novel pharmacological profile of TPA023B and might be attributed to the partial agonism at the α2, α3, and α5 subtypes and/or the lack of efficacy at the α1 subtype.
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