Introduction Cerebral glucose levels in humans can be measured non-invasively by C MRS to determine the kinetics of glucose transport into the brain. This transport can be described by a reversible Michaelis-Menten (MM) model [1], which is characterized by a half-maximal transport constant (Kt) and maximal transport rate (Tmax) or maximal transport rate relative to CMRglc (Tmax/CMRglc). Several...

Most reverse transcriptase and protease inhibitors used in highly active antiretroviral therapy for treating human immunodeficiency virus (HIV) infections exhibit poor penetration into the brain, raising the concern that the brain may be a sanctuary site for the development of resistant HIV variants. This study explores the relationship between the dose and plasma and brain concentrations of zo...

Supplementing brain cholesterol is emerging as a potential treatment for Huntington's disease (HD), genetic neurodegenerative disorder characterized, among other abnormalities, by inefficient biosynthesis. However, delivering to the challenging due blood-brain barrier (BBB), which prevents it from reaching striatum, especially, with therapeutically relevant doses. Here we describe distribution,...

Background Controversy exists with respect to the etiological role of cerebral small vessel disease (CSVD) in Alzheimer’s (AD). We thus evaluated association between white matter hyperintensity (WMH), an MRI marker CSVD, brain amyloid β (Aβ) and tau burden their plasma markers among subjects varying severity levels cognitive impairment. Methods recruited 84 from CU-SEEDS (The Chinese University...

Capillary endothelial cells isolated from rat brain exhibit Na+-dependent uptake of the neutral amino acid analog alpha-(methylamino)isobutyric acid. Since studies in vivo demonstrate that this transport system is not present on the blood side of brain capillaries we conclude that Na+-dependent neutral amino acid transport is located on the brain side. Therefore, the luminal plasma membrane and...

Most of the existing anti-human immunodeficiency virus agents enter the central nervous system (CNS) inefficiently and thus may allow slow viral replication in the brain. This may provide a sanctuary for the virus in the CNS and contribute to the development of acquired immunodeficiency syndrome dementia complex. This study evaluates a prodrug approach to improve the CNS delivery of the reverse...

The distribution, clearance, and bioavailability of (2S,6S)-hydroxynorketamine has been studied in the Wistar rat. The plasma and brain tissue concentrations over time of (2S,6S)-hydroxynorketamine were determined after intravenous (20 mg/kg) and oral (20 mg/kg) administration of (2S,6S)-hydroxynorketamine (n = 3). After intravenous administration, the pharmacokinetic parameters were estimated ...

The brain renin-angiotensin system (RAS) contributes to increased sympathetic drive in heart failure (HF). The factors upregulating the brain RAS in HF remain unknown. We hypothesized that aldosterone (ALDO), a downstream product of the systemic RAS that crosses the blood-brain barrier, signals the brain to increase RAS activity in HF. We examined the relationship between circulating and brain ...

Angelicae Pubescentis Radix (APR) is a widely-used traditional Chinese medicine. Pharmacological studies have begun to probe its biological activities on neurological disorders recently. To assess the brain penetration and distribution of APR, a validated ultra-performance liquid chromatography tandem mass spectrometry method was applied to the simultaneous determinations of the main coumarins ...