Research Publications - College of Medicine and Health Science

Department of Pharmacology
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Disorders
The development of selective antagonists
targeting central histamine H 3 receptors enables
the explanation of their physiological and
pathophysiological functions, as the difficulty
for developing satisfactory therapy of Alzheimer’s
disease (AD), Attention-Deficit-Hyperactivity-Disorder
(ADHAD), or drugs abuse (DA) lies
in the complex pathophysiology of the disease,
which involves numerous pathways that include
deficiency in cholinergic neurotransmission, abnormalities
of adrenergic, serotonergic and dopaminergic
neurotransmission. Thus, the development
of H 3 receptor antagonists belonging to
different chemical classes capable of penetrating
into the CNS and modulating histaminergic
neurotransmission in the central nervous system
can positively affect the multi-neurotransmitter
disorders, e.g. AD, ADHAD, or DA.
Research interest of Dr Bassem Shaban Sadek
focuses on the structural development of those
histamine H 3 receptor antagonists targeting
cognitive disorders. To this end, different chemical
classes of antagonists, e.g. piperidine- and
pyrrolidine-based antagonists will be synthesized
and investigated for their in-vitro antagonistic
effect at human histamine H 3 receptors.
Selected compounds with high in-vitro antagonist
activity will be further studied on their
in-vivo modulating effects on spatial memory
impairment and drug addiction using Radial
Maze, and Conditioned-Place Preference (CPP),
respectively, as such pharmacologic evaluation
is a key stone in the development of future
drugs of significant role in therapeutic management
of cognitive disorders, e.g. AD, ADHAD,
and DA.