Published in Digestive Diseases
Nausea and vomiting are debilitating symptoms complicating many clinical conditions. Conventional antiemetic agents act as muscarinic, histamine, and dopamine receptor antagonists in the central nervous system. In a retrospective analysis, tricyclic antidepressant drugs demonstrated efficacy in long-term treatment of functional nausea. Some cases o...
Published in Digestion
Stress has long been postulated to influence the progression of inflammatory bowel disease (IBD). Our current understanding of the relationship between stress and IBD is still limited, and hence explanation for the occurrence of relapses has remained largely speculative. Stress affects the immune system, the neuroendocrine system and the intestinal...
Published in Neuropsychobiology
Substance P (SP) is a neuropeptide which is abundant in the periphery and the central nervous system, where it is colocalized with other neurotransmitters such as serotonin or dopamine. SP has been proposed to play a role in the regulation of pain including migraine and fibromyalgia, asthma, inflammatory bowel disease, emesis, psoriasis as well as ...
Published in Biochemical and Biophysical Research Communications
Amphiphilic peptides with positive charges such as substance P (SP) and mastoparan (MP) are known to induce exocytosis in rat peritoneal mast cells. To elucidate whether and how intracellular Ca 2+ signaling is involved in the peptide-induced exocytosis, here we investigated the relationships between an increase in intracellular free Ca 2+ concentr...
Published in Neuroendocrinology
The pars tuberalis (PT) is a distinct subdivision of the anterior pituitary gland that plays a central role in regulating seasonal prolactin release. In sheep, there is compelling evidence that seasonal changes in light, transformed into a melatonin signal, are interpreted by the PT to modulate the release of a factor which affects prolactin releas...
Published in Encyclopedia of Basic Epilepsy Research
There are at least seven tachykinins in the human body, and their actions are diverse. Tachykinins are predominantly excitatory, in the brain (presynaptic enhancement of glutamate release), and enhance motility in the gut and inflammation in many tissues. Substance P and neurokinin B are involved in status epilepticus, and are overexpressed in the ...
Published in Bioorganic & Medicinal Chemistry Letters
Abstract Lead optimisation starting from the previously reported selective quinoline NK 3 receptor antagonists talnetant 2 (SB-223412) and 3 (SB-222200) led to the identification of 3-aminoquinoline NK 3 antagonist 10 (GSK172981) with excellent CNS penetration. Investigation of a structurally related series of sulfonamides with reduced lipophilicit...
Published in Peptides
Abstract Neuropeptides related to vertebrate tachykinins have been identified in Drosophila and are referred to as drosotachykinins, or DTKs. Two Drosophila G protein-coupled receptors, designated NKD (neurokinin receptor from Drosophila; CG6515) and DTKR ( Drosophila tachykinin receptor; CG7887), display sequence similarities to mammalian tachykin...
Published in Neuropharmacology
Abstract The tachykinin NK 3 receptor shows promise as a novel target for antipsychotics, but knowledge of downstream activity following tachykinin NK 3 receptor activation is lacking. To determine the practical utility of senktide-induced tail whips in mice as a tool for determining and characterizing downstream activity following tachykinin NK 3 ...
Alcohol accounts for major disability worldwide and available treatments are insufficient. A massive growth in the area of addiction neuroscience over the last several decades has not resulted in a corresponding expansion of treatment options available to patients. In this chapter, we describe our experience with building translational research pro...
