73367-80-3Relevant articles and documents
A Novel Agonist of the Type 1 Lysophosphatidic Acid Receptor (LPA1), UCM-05194, Shows Efficacy in Neuropathic Pain Amelioration
González-Gil, Inés,Zian, Debora,Vázquez-Villa, Henar,Hernández-Torres, Gloria,Martínez, R. Fernando,Khiar-Fernández, Nora,Rivera, Richard,Kihara, Yasuyuki,Devesa, Isabel,Mathivanan, Sakthikumar,Del Valle, Cristina Rosell,Zambrana-Infantes, Emma,Puigdomenech, María,Cincilla, Giovanni,Sanchez-Martinez, Melchor,Rodríguez De Fonseca, Fernando,Ferrer-Montiel, Antonio V.,Chun, Jerold,López-Vales, Rubén,López-Rodríguez, María L.,Ortega-Gutiérrez, Silvia
, p. 2372 - 2390 (2020/01/02)
Neuropathic pain (NP) is a complex chronic pain state with a prevalence of almost 10% in the general population. Pharmacological options for NP are limited and weakly effective, so there is a need to develop more efficacious NP attenuating drugs. Activation of the type 1 lysophosphatidic acid (LPA1) receptor is a crucial factor in the initiation of NP. Hence, it is conceivable that a functional antagonism strategy could lead to NP mitigation. Here we describe a new series of LPA1 agonists among which derivative (S)-17 (UCM-05194) stands out as the most potent and selective LPA1 receptor agonist described so far (Emax = 118%, EC50 = 0.24 μM, KD = 19.6 nM; inactive at autotaxin and LPA2-6 receptors). This compound induces characteristic LPA1-mediated cellular effects and prompts the internalization of the receptor leading to its functional inactivation in primary sensory neurons and to an efficacious attenuation of the pain perception in an in vivo model of NP.
Amantadine hapten and preparing method and application thereof
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Paragraph 0074; 0076; 0082, (2019/10/01)
The invention relates to the field of preparation of haptens, in particular to an amantadine hapten and a preparing method and application thereof. When the amantadine hapten is prepared, amantadine and bromine polyhydroxyalkanoate serve as raw materials, and through a nucleophilic substitution reaction, amidogen groups in amantadine molecules are connected with the bromine polyhydroxyalkanoate; then through a hydrolysis reaction, carboxyl groups are introduced to obtain a corresponding product. The amantadine hapten can be coupled with a carrier protein to prepare an artificial antigen, the artificial antigen is prepared into a monoclonal antibody or a polyclonal antibody through an immune animal, and then the monoclonal antibody or the polyclonal antibody can be used for quickly detecting residues of the amantadine in an animal product.
Synthesis of fluorescent C24-ceramide: Evidence for acyl chain length dependent differences in penetration of exogenous NBD-ceramides into human skin
Novotny, Jakub,Pospěchová, Kate?ina,Hrabálek, Alexandr,?áp, Robert,Vávrová, Kate?ina
supporting information; experimental part, p. 6975 - 6977 (2010/06/16)
Topical skin lipid supplementation may provide opportunities for controlling ceramide (Cer) deficiency in skin diseases such as atopic dermatitis or psoriasis. Here we describe the synthesis of a long-chain 7-nitrobenzo[c][1,2,5]oxadiazol-4-yl (NBD)-labeled Cer and its different penetration through human skin compared to widely used short-chain fluorescent Cer tools.
