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David C. Blakemore Justin S. Bryans Pauline Carnell Mark J. Field Natasha Kinsella Jack K. Kinsora Leonard T. Meltzer Simon A. Osborne Lisa R. Thompson Sophie C. Williams 《Bioorganic & medicinal chemistry letters》2010,20(1):248-251
A range of 3,4-alkylated five-membered ring derivatives of gabapentin were synthesised. One compound (21) had an excellent level of potency against α2δ and was profiled in in vivo models of pain and anxiety. 相似文献
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JJ. ALDASORO C. AEDO F. MUÑOZ GARMENDIA 《Botanical journal of the Linnean Society. Linnean Society of London》1996,121(2):143-158
A multivariate morphometric study of the genus Pyrus in south-west Europe and North Africa shows that five species may be recognized in the area: P. bourgaeana Decne., P. communis L., P. cordata Dew., P. spinosa Forssk, and P. nivalis Jacq. Some valuable characters for identification of these species are proposed. In particular the width of fruit peduncle, petal size, leaf width and petiole length served to discriminate the taxa. Several names such as P. gharbiona Trab., P. cossonii Rehder (|M= P. longipes Balansa ex Coss. & Durieu) and P. boisseriana Buhse, are regarded as synonyms of P. cordata , while P. marnormis Trab. of P. bourgaeana. Consequently a check-list and a key to these species are provided. 相似文献
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Milbank JB Knauer CS Augelli-Szafran CE Sakkab-Tan AT Lin KK Yamagata K Hoffman JK Zhuang N Thomas J Galatsis P Wendt JA Mickelson JW Schwarz RD Kinsora JJ Lotarski SM Stakich K Gillespie KK Lam WW Mutlib AE 《Bioorganic & medicinal chemistry letters》2007,17(16):4415-4418
Rational replacement of the alkyne linker of mGluR5 antagonist MPEP gave 7-arylquinolines. SAR optimization gave an orally active compound with high affinity for the MPEP binding site. 相似文献
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Wendt JA Deeter SD Bove SE Knauer CS Brooker RM Augelli-Szafran CE Schwarz RD Kinsora JJ Kilgore KS 《Bioorganic & medicinal chemistry letters》2007,17(19):5396-5399
A novel series of potent 2-aryl pyrido[2,3-d]pyrimidine mGlu5 receptor antagonists are described. The synthesis and pharmacological activities of these analogs are discussed. 相似文献
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Leo AB Joosten Erik Lubberts Monique MA Helsen Tore Saxne Christina JJ Coenen-de Roo Dick Heinegård Wim B van den Berg 《Arthritis research & therapy》1999,1(1):81-11
Destruction of cartilage and bone are hallmarks of human rheumatoid arthritis (RA), and controlling these erosive processes
is the most challenging objective in the treatment of RA. Systemic interleukin-4 treatment of established murine collagen-induced
arthritis suppressed disease activity and protected against cartilage and bone destruction. Reduced cartilage pathology was
confirmed by both decreased serum cartilage oligomeric matrix protein (COMP) and histological examination. In addition, radiological
analysis revealed that bone destruction was also partially prevented. Improved suppression of joint swelling was achieved
when interleukin-4 treatment was combined with low-dose prednisolone treatment. Interestingly, synergistic reduction of both
serum COMP and inflammatory parameters was noted when low-dose interleukin-4 was combined with prednisolone. Systemic treatment
with interleukin-4 appeared to be a protective therapy for cartilage and bone in arthritis, and in combination with prednisolone
at low dosages may offer an alternative therapy in RA. 相似文献