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Neurochemical characterization of 5-HTR partial agonists with simultaneous PET-MRI.

J Cereb Blood Flow Metab

November 2024

Athinoula A. Martinos Center for Biomedical Imaging, Department of Radiology, Massachusetts General Hospital, Harvard Medical School, Charlestown, USA.

Article Synopsis
  • This study investigates the effects of different serotonin 2A receptor (5-HTR) agonists, such as psilocybin, lisuride, and 25CN-NBOH, to understand their potential in psychedelic drug applications.
  • Using advanced imaging techniques like PET and phMRI on nonhuman primates, the researchers evaluated how these agonists affect brain blood flow and receptor occupancy.
  • Findings suggest that mixed agonists like psilocybin and lisuride create complex blood volume responses while 25CN-NBOH leads to simpler responses, shedding light on how these drugs could be used to treat psychiatric disorders.
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The past three decades have witnessed a welcome expansion of the therapeutic armamentarium for the management of pulmonary arterial hypertension (PAH). However, against this backdrop, there have been some notable disappointments in drug development. Here we use these as case studies to emphasize the importance of informed drug target selection, the early evaluation of dose-response relationships in human studies, and the value of the deep phenotyping of patients in clinical studies to better understand inter-individual variation in patient response.

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Use of apomorphine in Parkinson's disease.

Neurol Sci

December 2008

Department of Neurology, IRCCS San Raffaele Pisana, Rome, Italy.

In the parkinsonian patient, the striatal levels of dopamine strictly depend on peripheral levodopa levels; short half-life of levodopa is responsible for plasmatic level fluctuations, which are consistent with a pulsatile receptor stimulation of the striatal system. This sort of non-physiologic stimulation induces a change of the condition of post-synaptic neurons, which is considered responsible for the fluctuations of clinical response. In this respect, apomorphine administration, via infusion pump, may be a good therapeutic option, aimed at obtaining continuous receptor stimulation, assisting in the management of motor fluctuations in the advanced phase of the disease.

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Transdermal treatment options for neurological disorders: impact on the elderly.

Drugs Aging

December 2006

Department of Neurology and Neurorehabilitation, IRCCS Istituto Auxologico Italiano, Piancavallo, Italy.

As people grow old, their need for medications increases dramatically because of the higher incidence of chronic pain, diabetes mellitus, cardiovascular and neurological diseases in the elderly population. Furthermore, the elderly require special consideration with respect to drug delivery, drug interactions and adherence. In particular, patients with chronic neurological diseases often require multiple administration of drugs during the day to maintain constant plasma medication levels, which in turn increases the likelihood of poor adherence.

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Pharmacokinetic optimisation in the treatment of Parkinson's disease : an update.

Clin Pharmacokinet

June 2006

Department of Neuroscience, Neurology, Uppsala University Hospital, Uppsala, Sweden.

Pharmacotherapy for Parkinson's disease is focused on dopaminergic drugs, mainly the dopamine precursor levodopa and dopamine receptor agonists. The elimination half-life (t(1/2)) of levodopa from plasma (in combination with a decarboxylase inhibitor) of about 1.5 hours becomes more influential as the disease progresses.

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