Related Products of 124172-53-8, Catalysts allow a reaction to proceed via a pathway that has a lower activation energy than the uncatalyzed reaction. 124172-53-8, Name is N,N’-(Hexane-1,6-diyl)bis(N-(2,2,6,6-tetramethylpiperidin-4-yl)formamide), SMILES is O=CN(CCCCCCN(C1CC(C)(C)NC(C)(C)C1)C=O)C2CC(C)(C)NC(C)(C)C2, belongs to piperidines compound. In a article, author is Popiolek-Barczyk, Katarzyna, introduce new discover of the category.
Antinociceptive effects of novel histamine H-3 and H-4 receptor antagonists and their influence on morphine analgesia of neuropathic pain in the mouse
Background and Purpose The histaminergic system is a promising target for the development of new analgesics, as histamine H-3 and H-4 receptors are expressed in regions concerned with nociceptive transmission. Here we have determined the analgesic effects of new H-3 and H-4 receptor antagonists in naive and neuropathic mice. Experimental Approach We used chronic constriction injury (CCI) to the sciatic nerve in mice to model neuropathy. Effects of a new H-3 receptor antagonist, E-162(1-(5-(naphthalen-1-yloxy)pentyl)piperidine) and H-4 receptor antagonist, TR-7(4-(4-chlorophenyl)-6-(4-methylpiperazin-1-yl)-1,3,5-triazin-2-amine) were assessed on mechanical (von Frey) and thermal (cold plate, tail flick) stimuli in mice with and without CCI (7days after injury). Effects of these antagonists on morphine analgesia were also evaluated, along with the possible participation of H-1 receptors in their effects. We analysed the compounds in binding and functional cAMP assays at the H-3 and H-4 receptors and determined metabolic stability. Key Results E-162 and TR-7 attenuated nociceptive responses and profound morphine analgesia in males with CCI. These antagonists showed analgesia in naive mice (tail flick test) and produced prolonged analgesia in neuropathic females. E-162-induced analgesia was reversed by pyrilamine, an H-1 receptor antagonist. E-162 bound potently to H-3 receptors (K-i=55nM) and inhibited cAMP accumulation (IC50=165nM). TR-7 showed lower affinity for H-4 receptors (K-i=203nM) and IC(50)of 512nM. Conclusions and Implications We describe a therapeutic use for new H-3 (E-162) and H-4 receptor (TR-7) antagonists in neuropathy. Targeting H-3 and H-4 receptors enhanced morphine analgesia, consistent with multimodal pain therapy.
Related Products of 124172-53-8, Because enzymes can increase reaction rates by enormous factors and tend to be very specific, typically producing only a single product in quantitative yield, they are the focus of active research.you can also check out more blogs about 124172-53-8.
Reference:
Piperidine – Wikipedia,
,Piperidine | C5H11N – PubChem