Abstract:
:Compounds acting via the neurotensin receptor type 2 (NTS2) are known to be active in animal models of acute and chronic pain. To identify novel NTS2 selective analgesics, we searched for NTS2 selective nonpeptide compounds using a FLIPR assay and identified the title compound (NTRC-824, 5) that, to our knowledge, is the first nonpeptide that is selective for NTS2 versus NTS1 and behaves like the endogenous ligand neurotensin in the functional assay.
journal_name
J Med Chemjournal_title
Journal of medicinal chemistryauthors
Thomas JB,Giddings AM,Wiethe RW,Olepu S,Warner KR,Sarret P,Gendron L,Longpre JM,Zhang Y,Runyon SP,Gilmour BPdoi
10.1021/jm500857rsubject
Has Abstractpub_date
2014-09-11 00:00:00pages
7472-7issue
17eissn
0022-2623issn
1520-4804journal_volume
57pub_type
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abstract::A novel series of C-3 substituted 4,6-dichloroindole-2-carboxylic acids was synthesized to investigate the influence of different hydrogen-bond donor and acceptor groups at this specific position on the affinity to the glycine site of the NMDA receptor. These novel 3-indolylmethyl derivatives with ring-open (amines, s...
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journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
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abstract::Seven pyranoses and three furanoses with a nitrogen in the ring were prepared by chemical synthesis, microbial conversion, and isolation from plants to investigate the contribution of epimerization, deoxygenation, and conformation to the potency of inhibition and specificity of mammalian glycosidases. The seven pyrano...
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pub_type: 杂志文章
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journal_title:Journal of medicinal chemistry
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journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm00224a020
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abstract::Following the recent discoveries that some L-nucleosides are more or equal potent than their D-counterparts, we synthesized 2'-deoxy-2',2'-difluoro-L-erythro-pentofuranosyl nucleosides as potential antiviral agents. The target compounds were synthesized via the key intermediates 7a or 7b from L-gulono gamma-lactone. C...
journal_title:Journal of medicinal chemistry
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