Tosh, Dilip K. published the artcileIn Vivo Phenotypic Screening for Treating Chronic Neuropathic Pain: Modification of C2-Arylethynyl Group of Conformationally Constrained A3 Adenosine Receptor Agonists, Product Details of C6H4N2, the publication is Journal of Medicinal Chemistry (2014), 57(23), 9901-9914, database is CAplus and MEDLINE.
(N)-Methanocarba adenosine 5′-methyluronamides containing 2-arylethynyl groups were synthesized as A3 adenosine receptor (AR) agonists and screened in vivo (po) for reduction of neuropathic pain. A small N6-Me group maintained binding affinity, with human > mouse A3AR and MW < 500 and other favorable physicochem. properties. Emax (maximal efficacy in a mouse chronic constriction injury pain model) of previously characterized A3AR agonist, 2-(3,4-difluorophenylethynyl)-N6-(3-chlorobenzyl) derivative 6a, MRS5698, was surpassed. More efficacious analogs (in vivo) contained the following C2-arylethynyl groups: pyrazin-2-yl 23 (binding Ki, hA3AR, nM 1.8), fur-2-yl 27 (0.6), thien-2-yl 32 (0.6) and its 5-chloro 33, MRS5980 (0.7) and 5-bromo 34 (0.4) equivalent, and physiol. unstable ferrocene 36, MRS5979 (2.7). 33 and 36 displayed particularly long in vivo duration (>3 h). Selected analogs were docked to an A3AR homol. model to explore the environment of receptor-bound C2 and N6 groups. Various analogs bound with μM affinity at off-target biogenic amine (M2, 5HT2A, β3, 5HT2B, 5HT2C, and α2C) or other receptors. Thus, we have expanded the structural range of orally active A3AR agonists for chronic pain treatment.
Journal of Medicinal Chemistry published new progress about 1017793-08-6. 1017793-08-6 belongs to pyridazine, auxiliary class Pyridazine,Alkynyl, name is 3-Ethynylpyridazine, and the molecular formula is C11H21BO2Si, Product Details of C6H4N2.
Referemce:
https://en.wikipedia.org/wiki/Pyridazine,
Pyridazine | C4H4N2 – PubChem