Neuropeptide substance

Aguiar MS, Brandao ML (1996) Effects of microinjections of the neuropeptide substance P in the dorsal periaqueductal gray on the behaviour of rats in the plus-maze test. Physiol Behav 60 1183-1186... 

Mitsuhashi, M., Ohashi, Y., Shichijo, S., Christian, C., Sudduth, K. J., Harrowe, G., Payan, D. G. Multiple intracellular signaling pathways of the neuropeptide substance P receptor, J. Neurosci. Res. 

Utilizing the Grubbs alkene metathesis reaction, Katzenellenbogen et al. 164 described the synthesis of the ten-membered-ring lactam p-turn mimetic 129 (Scheme 47, some experimental details given below) and prepared a mimetic 130 of the neuropeptide substance P, and in particular of the four C-terminal amino acid sequence -Phe8-Gly-Leu-Metn-. Compound 130 was unable to inhibit the binding of radiolabeled substance P. 

These neuropeptides are coexpressed with GABA in subpopulations of striatal medium-sized spiny neurons, and therefore in subsets of the fibers which target the SN. As will be mentioned further (see Section 4.3), the striatal output reaches the SN through two main circuits distinct from the anatomical and functional points of view, defined as direct and indirect pathways. Direct pathway striatal neurons express the neuropeptide substance P and dynorphin, whereas indirect pathway striatal neurons express enkephalin (see Section 6.1). 

Krause, J.E., Chirgwin, J.M., Carter, M.S. etal. (1987). Three rat preprotachykinin mRNAs encode the neuropeptides substance P and neurokinin A. Proc. Natl. Acad. Sci. USA 84, 881-885. 

DA modulates the activity of local and efferent inhibitory GABAergic neurons as well as acetylcholinergic interneurons of caudate-putamen (12, 15, 17). Excitatory DA D -type receptors, together with the neuropeptides substance P and dynorphin, are mainly expressed by the striatonigral GABAergic neurons in the... 

TNFa is released in response to bacteria (endotoxins and LPS), viruses, protozoa, cytokines (GM-CSF, IL-1, IL-2, IFNy, and TNFa itself), immune complexes, complement component C5a, neuropeptide substance P, and reactive oxygen intermediates. Unhlce TNFa, sources of preformed TNFp have not been identified. ... 

Spiny projection neurons all contain glutamic acid decarboxylase (GAD) the synthetic enzyme for the neurotransmitter GABA (Kita and Kitai 1988). In addition, most of those neurons projecting to the globus pallidus alone contain the neuropeptide enkephalin, whereas most of those which project to the substantia nigra contain the neuropeptides substance P and dynorphin (Beckstead and Kersey 1985 Gerfen and Young 1988 Haber and Watson 1983). Spiny projection neurons contain different complements of neurotransmitter receptors, and other proteins that serve to characterize particular subpopulations of striatal output neurons. These will be discussed in further detail below. 

Fluoroalkenes have been recognized as one of the possible nonhydrolyzable mimetics of amides on the basis of the similarity of charge distribution of the amide bond with the fluoroalkene moiety (Figure 6.2) [31] and their dipole moments (3.7 and 0.97 D for N-methylacetamide and ( )-2-fluoro-2-butene, respectively) [32]. A comparison of the receptor-binding ability of neuropeptide substance P (SP) with some related isosteres with fluoroalkenyl moiety is shown in Table 6.5, which demonstrates the effectiveness of replacement of the amide bond with fluoroalkenyl moiety [33]. 

Regulations at the level of the central nervous systems are ensured by neurotransmitters. Such substances can be simple molecules (acetylcholine, y-aminobutyric acid, norepinephrine, etc.) or neuropeptides (substance P, vasopressin, corticotrophin releasing factor, neurotensin, etc.). Pharmacological interventions aim then to correct dysregu-lations, either in reducing an excessive neuronal activity or in stimulating a weak working system. The easiest ways for... 

Pean et a/. reported that (3- and y-CyD derivatives coupled with the neuropeptide substance P bind to the neurokinin receptor of rat brain and cultured Chinese hamster ovary (CHO) cells transfected with the human neurokinin receptor gene, in vitro. The in vivo intracerebral injection of substance P/y-CyD conjugate in the rat striatum induced a massive internalization of the receptor, and the conjugate recognized the neurokinin receptor-bearing neurons. Schaschke et al. prepared the (3-CyD conjugates linked covalently to tetra- and hepta-peptide analogues of... 

Finally, much neurogenic inflammation within the airways is a consequence of release of the neuropeptides substance P and other neurokinins. Antagonists of these agents have proven to be particularly poor in the heatment of asthma but have been developed in therapy of chemotherapy-induced nausea and vomiting. Their efficacy in chronic cough remains to be determined. 

Kim, J.H., Jung, Y., Kim, B.-S., Kim, S.H. Stem cell recruitment and angiogenesis of neuropeptide substance p coupled with self-assembling peptide nanofiber in a mouse hind limb ischemia model. Biomaterials 34, 1657-1668 (2013)... 

The temperature dependence of the partition of a neuropeptide, substance P (SP), in isotropic (q = 0.5) bicelles was investigated by using PFG NMR diffusion technique. The partition coefficient decreases as the temperature is increased from 295 to 325 K, indicating a favorable (neg.) enthalpy change upon partitioning of the peptide. Thermodynamic analysis of the data shows that the partitioning of SP at 300 K is driven by the enthalpic term (AH) with the value of — 4.03 kcal mol , while it is opposed by the entropic term ( — TAS) by approx. 1.28 k cal mol with a small neg. change in heat capacity (ACp). ... 

Desiderio, D. M., and I. Katakuse Fast Atom Bombardment-Collision Activated Dissociation-Linked Field Scanning Mass Spectrometry of the Neuropeptide Substance P. Analyt. Biochem. 129, 425 (1983). 

The biological actions of capsaicin are primarily attributable to release of the neuropeptide substance P, calcitonin gene-related peptide (CGRP), and neurokinin A from sensory neurons. These transmitters from primary sensory neurons communicate witir other cell types. They produce alterations in the airway mucosa and neurogenic inflammation of the respiratory epithelium, airway blood vessels, glands, and smooth muscle. Alterations in multiple effector organs lead to bronchoconstriction, increased vascular permeability, edema of the tracheobronchial mucosa, elevated mucosal secretion, and neutrophil chemotaxis (Tominack and Spyker, 1987). Capsaicin-induced effects of bronchoconstriction, vasodilation, and plasma protein extravasation are mediated by substance P. In addition, substance P can cause bronchoconstriction through stimulation of c-fibers in pulmonary and bronchial circulation. 

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