654663-32-8Relevant articles and documents
Design, synthesis, and biological evaluation of 17-cyclopropylmethyl-3, 14β-dihydroxy-4,5α-epoxy-6β-[(4′-pyridyl)carboxamido] morphinan derivatives as peripheral selective μ opioid receptor agents
Yuan, Yunyun,Elbegdorj, Orgil,Chen, Jianyang,Akubathini, Shashidhar K.,Zhang, Feng,Stevens, David L.,Beletskaya, Irina O.,Scoggins, Krista L.,Zhang, Zhenxian,Gerk, Phillip M.,Selley, Dana E.,Akbarali, Hamid I.,Dewey, William L.,Zhang, Yan
, p. 10118 - 10129 (2013/01/16)
Peripheral selective μ opioid receptor (MOR) antagonists could alleviate the symptoms of opioid-induced constipation (OIC) without compromising the analgesic effect of opioids. However, a variety of adverse effects were associated with them, partially due to their relatively low MOR selectivity. NAP, a 6β-N-4′-pyridyl substituted naltrexamine derivative, was identified previously as a potent and highly selective MOR antagonist mainly acting within the peripheral nervous system. The noticeable diarrhea associated with it prompted the design and synthesis of its analogues in order to study its structure-activity relationship. Among them, compound 8 showed improved pharmacological profiles compared to the original lead, acting mainly at peripheral while increasing the intestinal motility in morphine-pelleted mice (ED50 = 0.03 mg/kg). The slight decrease of the ED50 compared to the original lead was well compensated by the unobserved adverse effect. Hence, this compound seems to be a more promising lead to develop novel therapeutic agents toward OIC.
HARMFUL ARTHROPOD CONTROL COMPOSITION, AND FUSED HETEROCYCLIC COMPOUND
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Page/Page column 93-94, (2011/04/13)
Disclosed is a harmful arthropod control composition comprising, as an active ingredient, a fused heterocyclic compound represented by formula (1) [wherein A1 and A2 independently represent a nitrogen atom or the like; R1 and R4 independently represent a halogen atom or the like; R2 and R3 independently represent a halogen atom or the like; R5 and R6 independently represent a linear C1-C6 hydrocarbon group which may be substituted, or the like (provided that both R5 and R6 cannot represent a hydrogen atom simultaneously); and n represents 0 or 1]. The harmful arthropod control composition has an excellent efficacy to control harmful arthropods.
COMPOSITION AND METHOD FOR CONTROLLING ARTHROPOD PESTS
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Page/Page column 243, (2011/05/06)
The present invention provides: an arthropod pests control composition comprising, as active ingredients, a condensed heterocyclic compound and a pyrethroid compound; a method for controlling arthropod pests which comprises applying effective amounts of a condensed heterocyclic compound and a pyrethroid compound to the arthropod pests or a locus where the arthropod pests inhabit; and so on.