Rees, H. Sluka, Kathleen A. Urban, Laszlo Walpole, Chris J. Willis, W. D.
Published in
Experimental Brain Research
Substance P, acting through neurokinin I receptors, is involved in the processing of nociceptive information in the spinal cord. Sensitization of spinothalamic tract neurons occurs to low-intensity stimuli following capsaicin injection. The current study tested the effects of the novel neurokinin 1 receptor antagonist, SDZ NKT 343, on the sensitiza...
Ladabaum, Uri Hasler, William L.
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...
Niess, Jan H. Mönnikes, Hubert Dignass, Axel U. Klapp, Burghard F. Arck, Petra C.
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...
Lieb, Klaus Treffurth, Yvonne Berger, Mathias Fiebich, Bernd L.
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 ...
Siuciak, Judith A. McCarthy, Sheryl A. Martin, A. N. Chapin, D. S. Stock, J. Nadeau, D. M. Kantesaria, S. Bryce-Pritt, D. McLean, S.
Published in
Psychopharmacology
RationaleThe structurally related neuropeptides, substance P, neurokinin A, and neurokinin B, belong to a family of molecules termed tachykinins and are widely distributed in the central and peripheral nervous systems. These peptides mediate their effects through three G protein coupled receptor subtypes, the neurokinin-1, neurokinin-2 and neurokin...
Mukai, Hidehito Kikuchi, Miharu Fukuhara, Shigetomo Kiso, Yoshiaki Munekata, Eisuke
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...
Nordquist, R. E. Delenclos, M. Ballard, T. M. Savignac, H. Pauly-Evers, M. Ozmen, L. Spooren, W.
Published in
Psychopharmacology
RationaleThe neurokinin 3 (NK3) receptor is a novel target under investigation for improvement of the symptoms of schizophrenia due to its ability to modulate dopaminergic signaling. However, research on effects of NK3 antagonism with animal models has been hindered because of species differences in the receptor between humans, rats, and mice.Objec...
Skinner, Donal C. Lang, A. Lee Pahl, Lindsay Wang, Qi
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...
Wasterlain, C.G. Tekchandani, L. Liu, H. Mazarati, A.M. Thompson, K.W. Suchomelova, L. Chen, J.W.Y. Niquet, J.
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 ...
Smith, Paul W Wyman, Paul A Lovell, Peter Goodacre, Caroline Serafinowska, Halina T Vong, Antonio Harrington, Frank Flynn, Sean Bradley, Daniel M Porter, Rod
...
Published in
Bioorganic & medicinal chemistry letters
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 lipophilicity led t...
