neuroleptic malignant syndrome (nms) is a rare fatal medical complication that occurs as a result of dopaminergic receptor blockage in the caudate at the termination of the nigrostriatal pathways (1), and may occur at any time following consumption of dopamine antagonists. this disorder also occurs in cases of sudden discontinuation of dopamine agonists and antagonists (2,3). some studies have ...

Diabetic neuropathic pain, an important micro vascular complication in diabetes mellitus, has been recognized as one of the most difficult types of pain to treat. Lack of understanding of etiology involved, inadequate relief, development of tolerance and potential toxicity of classical anti-nociceptive agents warrants the investigation of newer agents to relieve this pain. The aim of the presen...

Flibanserin is a novel antagonist small molecule to treat the hypoactive sexual desire disorder (HSDD) in the premenopausal women. The present article is related to the structural and electronic properties study and docking analysis of the title compound with 5-hydroxytryptamine 2A (5-HT2A) serotonin receptor. To access these aims, the molecular structure of the said compound was optimized usin...

First-generation serotonin receptor antagonists greatly improved the control of chemotherapy-induced nausea and vomiting (CINV) during the 1990s. A new class of agents, neurokinin-1 receptor antagonists, was introduced in March 2003 and produced even greater control of CINV when used in combination with a serotonin receptor antagonist and a corticosteroid. In July 2003, palonosetron, a new seco...

Serotonin receptors play central roles in neuromodulation and are critical drug targets for psychiatric disorders. Optical control of serotonin receptor subtypes has the potential to greatly enhance our understanding spatiotemporal dynamics function. While other neuromodulatory have been successfully rendered photoswitchable, reversible photocontrol not achieved, representing a major gap GPCR p...

A series of photolabile o-nitrobenzyl derivatives of serotonin (caged serotonin) were synthesized: the amine-linked serotonin derivatives N-(2-nitrobenzyl) serotonin (Bz-5HT) and N-(alpha-carboxy-2-nitrobenzyl) serotonin (N-CNB-5HT), and O-alpha-carboxy-2-nitrobenzyl) serotonin (O-CNB-5HT), which has the caging group attached to the phenolic OH group. All the derivatives released free serotonin...

CONTEXT MDMA (3,4-methylenedioxymethamphetamine, also popularly known as "ecstasy") is a popular recreational drug that produces loss of serotonin axons in animal models. Whether MDMA produces chronic reductions in serotonin signaling in humans remains controversial. OBJECTIVE To determine whether MDMA use is associated with chronic reductions in serotonin signaling in the cerebral cortex of ...

The pathogenesis of pulmonary arterial hypertension (PAH) remains uncertain. Both the serotonin and endothelin (ET) systems are believed to be involved. Recent studies pointed to the importance of the serotonin 2B receptor as a limiting step. The current authors investigated the lung tissue expression of serotonin receptors and of the serotonin transporter (5-HTT) by real-time-quantitative poly...

A full-length serotonin receptor mRNA from the 5Hthpr gene was sequenced from larvae of the sea urchin, Hemicentrotus pulcherrimus. The DNA sequence was most similar to 5HT-1A of the sea urchin Strongylocentrotus purpuratus found by The Sea Urchin Genome Project, and the protein sequence predicted the presence of seven transmembrane domains. Immunohistochemistry with anti-5HThpr antibodies indi...