Published in Neuroscience research
The presence of substance P (SP) receptor (Neurokinin-1 receptor, NK1R) in the indusium griseum (IG) and anterior hippocampal continuation (AHC) during postnatal development was studied by immunocytochemistry (ICC). NK1R-immunopositive neurons (NK1RIP-n) first appeared in both areas on postnatal day (P) 5. From P5 onward, their distribution pattern...
Published in Cell biochemistry and biophysics
Copper is one of the most abundant biological metals, and its chemical properties mean that organisms need sophisticated and multilayer mechanisms in place to maintain homoeostasis and avoid deleterious effects. Studying copper proteins requires multiple techniques, but electron paramagnetic resonance (EPR) plays a key role in understanding Cu(II) ...
Published in International review of neurobiology
Substance P (SP) is an 11-amino acid neuropeptide of the tachykinin family that preferentially activates the neurokinin-1 receptor (NK1R). First isolated 85 years ago and sequenced 40 years later, SP has been extensively studied. Early studies identified a role for SP and the NK1R in contraction of intestinal smooth muscle, central pain processing,...
Published in World journal of gastroenterology
Immunohistochemical NK-1R and pEGFR positivity with VDR negativity can be used to identify areas of sporadic colorectal neoplasia. VDR immunoreactivity can distinguish CAC from sporadic cancer.
Anxiety disorders, including social anxiety disorder (SAD) and posttraumatic stress disorder (PTSD) are common and disabling conditions. Largely based on animal and pharmacological studies, both the serotonergic and substance P/neurokinin-1 (SP/NK1) systems have been implicated in their underlying pathology. However, only few neuroimaging studies h...
Published in Bioorganic & medicinal chemistry
The last two decades have provided a large weight of preclinical data implicating the neurokinin-1 receptor (NK1) and its cognate ligand substance P (SP) in a broad range of both central and peripheral disease conditions. However, to date, only the NK1 receptor antagonist aprepitant has been approved as a therapeutic and this is to prevent chemothe...
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...
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 ...
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 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...
