“…Given that species-specific metabolic differences are well-described for prodrugs, ,, we developed an in vitro multispecies screening platform to identify prodrugs that were stable (and thus inert) in plasma and liver ( highly metabolic sites) and gastrointestinal tract (toxicity site) ,, yet readily taken up and cleaved to DON in tumor cells (efficacy target site). All compounds were tested for in vitro plasma stability in mouse, swine, and human plasma (Table ).…”
Exaggerated anticipatory anxiety is common in social anxiety disorder (SAD).
Neuroimaging studies have revealed altered neural activity in response to social stimuli in SAD, but fewer studies have examined neural activity during anticipation of feared social stimuli in SAD.
The current study examined the time course and magnitude of activity in threat processing brain regions during speech anticipation in socially anxious individuals and healthy controls (HC).
Method Participants (SAD n = 58; HC n = 16) underwent functional magnetic resonance imaging (fMRI) during which they completed a 90s control anticipation task and 90s speech anticipation task.
Exaggerated anticipatory anxiety is common in social anxiety disorder (SAD).
Neuroimaging studies have revealed altered neural activity in response to social stimuli in SAD, but fewer studies have examined neural activity during anticipation of feared social stimuli in SAD.
The current study examined the time course and magnitude of activity in threat processing brain regions during speech anticipation in socially anxious individuals and healthy controls (HC).
Method Participants (SAD n = 58; HC n = 16) underwent functional magnetic resonance imaging (fMRI) during which they completed a 90s control anticipation task and 90s speech anticipation task.
“…Given that species-specific metabolic differences are well-described for prodrugs, ,, we developed an in vitro multispecies screening platform to identify prodrugs that were stable (and thus inert) in plasma and liver ( highly metabolic sites) and gastrointestinal tract (toxicity site) ,, yet readily taken up and cleaved to DON in tumor cells (efficacy target site). All compounds were tested for in vitro plasma stability in mouse, swine, and human plasma (Table ).…”
Exaggerated anticipatory anxiety is common in social anxiety disorder (SAD).
Neuroimaging studies have revealed altered neural activity in response to social stimuli in SAD, but fewer studies have examined neural activity during anticipation of feared social stimuli in SAD.
The current study examined the time course and magnitude of activity in threat processing brain regions during speech anticipation in socially anxious individuals and healthy controls (HC).
Method Participants (SAD n = 58; HC n = 16) underwent functional magnetic resonance imaging (fMRI) during which they completed a 90s control anticipation task and 90s speech anticipation task.
Exaggerated anticipatory anxiety is common in social anxiety disorder (SAD).
Neuroimaging studies have revealed altered neural activity in response to social stimuli in SAD, but fewer studies have examined neural activity during anticipation of feared social stimuli in SAD.
The current study examined the time course and magnitude of activity in threat processing brain regions during speech anticipation in socially anxious individuals and healthy controls (HC).
Method Participants (SAD n = 58; HC n = 16) underwent functional magnetic resonance imaging (fMRI) during which they completed a 90s control anticipation task and 90s speech anticipation task.
“…Recently, we have been engaged in investigating the driving force(s) responsible for significant accelerations in rate of some intramolecular processes that have been used as enzyme models and pro-drug hosts (3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14)(15). Using different molecular orbital calculation methods, we have explored: (i) the acid-catalyzed lactonization of hydroxy acids as studied by Cohen (16-21) and Menger (22)(23)(24)(25)(26)(27); (ii) the intramolecular proton transfer in rigid systems as investigated by ; and (iii) the S N 2-based cyclization as researched by Brown, Bruice and Mandolini (28)(29)(30)(31) arriving at the following conclusions: the driving force for rate enhancements in intramolecular processes can be attributable to proximity and ⁄ or steric effects, depending on the nature of the system, and the accelerations in rate for intramolecular reactions are a result of both entropy and enthalpy effects.…”
Section: Cad Of Pro-drugs For Antimalarial Atovaquonementioning
Exaggerated anticipatory anxiety is common in social anxiety disorder (SAD).
Neuroimaging studies have revealed altered neural activity in response to social stimuli in SAD, but fewer studies have examined neural activity during anticipation of feared social stimuli in SAD.
The current study examined the time course and magnitude of activity in threat processing brain regions during speech anticipation in socially anxious individuals and healthy controls (HC).
Method Participants (SAD n = 58; HC n = 16) underwent functional magnetic resonance imaging (fMRI) during which they completed a 90s control anticipation task and 90s speech anticipation task.
Exaggerated anticipatory anxiety is common in social anxiety disorder (SAD).
Neuroimaging studies have revealed altered neural activity in response to social stimuli in SAD, but fewer studies have examined neural activity during anticipation of feared social stimuli in SAD.
The current study examined the time course and magnitude of activity in threat processing brain regions during speech anticipation in socially anxious individuals and healthy controls (HC).
Method Participants (SAD n = 58; HC n = 16) underwent functional magnetic resonance imaging (fMRI) during which they completed a 90s control anticipation task and 90s speech anticipation task.
“…As stated several times, the prodrug strategy is especially promising to achieve pharmaceutical and/or pharmacokinetic properties that would be incompatible with a given pharmacophore. A prodrug might be considered when the structure−activity relationship (SAR) of a compound class for the drug target and the pharmacokinetic properties appear chemically incompatible, as schematized in Figure , e.g., when pharmacokinetically problematic moieties are essential requisites for biological activity (e.g., amidines, guanidines, phenolic groups, phosphate groups). , Alternatively, a prodrug can be designed for tissue (e.g., tumor) targeting to reduce systemic toxicity. 19 Two schematic situations encountered in a research project.…”
Section: Strategic Considerationsmentioning
confidence: 99%
“…A prodrug might be considered when the structure-activity relationship (SAR) of a compound class for the drug target and the pharmacokinetic properties appear chemically incompatible, as schematized in Figure 19, e.g., when pharmacokinetically problematic moieties are essential requisites for biological activity (e.g., amidines, guanidines, phenolic groups, phosphate groups). 75,76 Alternatively, a prodrug can be designed for tissue (e.g., tumor) targeting to reduce systemic toxicity.…”
Exaggerated anticipatory anxiety is common in social anxiety disorder (SAD).
Neuroimaging studies have revealed altered neural activity in response to social stimuli in SAD, but fewer studies have examined neural activity during anticipation of feared social stimuli in SAD.
The current study examined the time course and magnitude of activity in threat processing brain regions during speech anticipation in socially anxious individuals and healthy controls (HC).
Method Participants (SAD n = 58; HC n = 16) underwent functional magnetic resonance imaging (fMRI) during which they completed a 90s control anticipation task and 90s speech anticipation task.
Exaggerated anticipatory anxiety is common in social anxiety disorder (SAD).
Neuroimaging studies have revealed altered neural activity in response to social stimuli in SAD, but fewer studies have examined neural activity during anticipation of feared social stimuli in SAD.
The current study examined the time course and magnitude of activity in threat processing brain regions during speech anticipation in socially anxious individuals and healthy controls (HC).
Method Participants (SAD n = 58; HC n = 16) underwent functional magnetic resonance imaging (fMRI) during which they completed a 90s control anticipation task and 90s speech anticipation task.
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