Current Topics in Medicinal Chemistry - Volume 8, Issue 12, 2008

Decades ago, in the 1950s, dopamine (DA) and serotonin (5-hydroxytriptamine, 5-HT) were discovered in the mammalian central and peripheral nervous systems and successively their role as essential neurotransmitters was revealed. Advances in understanding the effect of DA and 5-HT have represented one of the success stories of neuropharmacology. In these years an enormous amount of experimental evidence has Read More

Since the initial observations linking 5-HT to psychiatric illness, evidence for a role of 5-HT and, in particular, a decreased brain serotonergic function in the pathology of a plethora of related disorders, has grown. However, it is the role of 5-HT in the pathogenesis of anxiety disorders and depression and the mechanism of action of antidepressants which has received the most attention. Thus enhanced serotonergic neurotr Read More

The serotonin receptor subtype 5-HT1A was one of the first serotonin receptor subtypes pharmacologically characterized. Over the last twenty years the 5-HT1A receptor has been the object of intense research efforts as witnessed by the 5-HT1A acting drugs marketed as anxiolytics. In recent years, several new chemical entities targeting the 5-HT1A receptor (alone or in combination with other molecular targets) have b Read More

Recently, the serotonin 5-HT6 receptor has been identified as a drug target for attenuating cognitive deficits associated with Alzheimer's disease (AD). Additionally, this receptor may also play a role in schizophrenia, anxiety and obesity. Reports in the literature suggest that the production of selective antagonists for the 5-HT6 receptor has increased during the last 10 years, with some compounds currently in clinical trials for t Read More

This review describes symptoms and pathophysiology of Parkinson's diseases (PD) and restless legs syndrome (RLS), and discusses the relationship between clinical outcome of DA agonists and their receptor-binding and pharmacokinetics. Oral DA agonists are divided into 2 classes; the ergots and the non-ergots. Both classes are in general equally effective against PD motor symptoms. Ergots (apart from bromocriptine) stimula Read More

A remarkable diversity of psychiatric and neurological disorders have been associated with dysfunction of dopamine (DA)-containing neurons, including schizophrenia, bipolar disorder (BD), Parkinson's disease (PD), and restless legs syndrome (RLS). In such disorders, transmission in discrete DA pathways may range from hypoactivation to hyperactivation of DA receptors, particularly those of the D2 subtype, providing Read More

Dopamine agonists have been usually used as adjunctive therapy for the cure of Parkinson's disease. It is generally believed that treatment with these drugs is symptomatic rather than curative and it does not stop or delay the progression of neuronal degeneration. However, several dopamine agonists of the D2-receptor family have recently been shown to possess neuroprotective properties in different in vitro and in Read More

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