125104-37-2Relevant academic research and scientific papers
New κ-Receptor Agonists Based upon a 2-piperidine Nucleus
Scopes, David I. C.,Hayes, Norman F.,Bays, David E.,Belton, David,Brain, John,et al.
, p. 490 - 501 (2007/10/02)
The syntheses of some 1--2-piperidines and their activities as κ-opioid receptor agonists are described.Selected structural modifications are made to the basic moiety and at the 2-, 3-, 4-, 5-, and 6-positions on the piperidine nucleus to enable structure-activity relationships to be delineated.As a result, some highly potent and selective κ-receptor agonists have been identified.In particular, this has been achieved by introduction of oxygen-containing functionality into the 4-position of the piperidine nucleus or the 3-position of the pyrrolidinylmethyl side chain.Thus, 1--2-piperidine (10) possesses high activity in the rabbit vas deferens (LVD, κ-specific tissue) (IC50 = 0.20 nM) and is a potent antinociceptive agent, as determined by the mouse acetylcholine-induced abdominal constriction test (MAC) (ED50 = 0.06 mg/kg, sc).The spirocyclic analogue 8--7-(1-pyrrolidinylmethyl)-1,4-dioxa-8-azaspirodecane (39) showed exceptionally potent activity: LVD, IC50 = 0.10 nM; MAC, ED50 = 0.001 mg/kg, sc.Both 10 and 39 displayed high selectivity for κ-opioid receptors over both μ- and δ-opioid receptor subtypes.
SPIROPIPERIDINE DERIVATIVES
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, (2008/06/13)
Compounds are disclosed of formula (I) STR1 wherein R 1 represents hydroxy, C 1-6 alkyl, C 1-6 hydroxyalkyl, C 1-6 carboxyalkyl, phenyl, oxo, amino, carboxy, amido,--NR 4 COR 5 (where R 4 and R 5 both represent C 1-6 alkyl), optionally substituted methyli
Piperidine derivatives
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, (2014/02/04)
Compounds are disclosed of formula (I) wherein, R1 represents hydroxy, C1 6 alkyl, C1 6 hydroxyalkyl, C1 6 carboxyalkyl, phenyl, oxo, amino, carboxy, amido, -NR4CORsu
