- Radiosynthesis and Biological Evaluation of [18F]R91150, a Selective 5-HT2AReceptor Antagonist for PET-Imaging
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Serotonergic 5-HT2A receptors in cortical and forebrain regions are an important substrate for the neuromodulatory actions of serotonin in the brain. They have been implicated in the etiology of many neuropsychiatric disorders and serve as a target for an
- Willmann, Michael,Hegger, Julian,Neumaier, Bernd,Ermert, Johannes
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p. 738 - 744
(2021/05/04)
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- Synthesis, labelling and first evaluation of [18F]R91150 as a serotonin 5-HT2A receptor antagonist for PET
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In psychiatric disorders such as anxiety, depression and schizophrenia, 5-HT2A receptors play an important role. In order to investigate them in vivo there is an increasing interest in selective and high-affinity radioligands for receptor binding studies using positron emission tomography (PET). Since available radioligands have disadvantages, R91150, which is a selective and high-affinity ligand for 5-HT2A receptors, was labelled with fluorine-18. This was accomplished in six steps via 4-[ 18F]fluorophenol and 1-(3-bromopropoxy)-4-[18F] fluorobenzene within 190 min starting from no-carrier-added [ 18F]fluoride. The overall radiochemical yield was 3.8±2% and the specific activity was at least 335 GBq/μmol at the end of the synthesis. First ex vivo studies in mice proved the uptake of [18F]R91150 in the brain. Radiometabolite studies revealed no radiometabolites in the brain, whereas in the plasma at least two could be detected 30 min p.i. Further preclinical studies are encouraged to evaluate the potential of this new 5-HT2A ligand as a radiotracer for PET. Copyright
- Muehlhausen, Ute,Ermert, Johannes,Coenen, Heinz H.
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experimental part
p. 13 - 22
(2009/04/18)
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- COMPOUNDS WHICH HAVE ACTIVITY AT M1 RECEPTOR AND THEIR USES IN MEDICINE
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Compounds of formula (I) or a salt thereof are provided: (I) wherein R4, R5, R6, Q and R are as defined in the description. Uses of the compounds as medicaments and in the manufacture of medicaments for treating psychotic
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- (3R)-3-Amino-4-(2,4,5-trifluorophenyl)-N-{4-[6-(2-methoxyethoxy)benzothiazol-2-yl]tetrahydropyran-4-yl}butanamide as a potent dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes
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Novel series of 3-amino-N-(4-aryl-1,1-dioxothian-4-yl)butanamides and 3-amino-N-(4-aryltetrahydropyran-4-yl)butanamides were synthesized and evaluated as dipeptidyl peptidase IV (DPP-IV) inhibitors. Derivatives incorporating the 6-substituted benzothiazole group showed highly potent DPP-IV inhibitory activity. Oral administration of (3R)-3-amino-4-(2,4,5-trifluorophenyl)-N-{4-[6-(2-methoxyethoxy)benzothiazol-2-yl]tetrahydropyran-4-yl}butanamide (12u) reduced blood glucose excursion in an oral glucose tolerance test.
- Nitta, Aiko,Fujii, Hideaki,Sakami, Satoshi,Nishimura, Yutaka,Ohyama, Tomofumi,Satoh, Mikiya,Nakaki, Junko,Satoh, Shiho,Inada, Chifumi,Kozono, Hideki,Kumagai, Hiroki,Shimamura, Masahiro,Fukazawa, Tominaga,Kawai, Hideki
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scheme or table
p. 5435 - 5438
(2009/05/30)
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- CHEMICAL COMPOUNDS
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The present invention provides compounds of formula (I) wherein R1, R2, R3, R4, R5, m and n are as defined hereinabove. The compounds of the present invention are modulators, especially antagonists, of the activity of chemokine CCR5 receptors. Modulators of the CCR5 receptor may be useful in the treatment of various inflammatory diseases and conditions, and in the treatment of infection by HIV and genetically related retroviruses.
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Page/Page column 74-75
(2008/06/13)
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- 2-CYANOPYRROLIDINECARBOXAMIDE COMPOUND
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A compound of the formula (I) or a pharmaceutically acceptable salt thereof: [wherein X1 and X2 each is independently lower alkylene; X3 is =CH2, =CHF or =CF2; R1 is substituent, R2 and R3 each is independently H or lower alkyl; n is 0, 1, 2, 3 or 4.] having the activity inhibiting DPP-IV activity. They are therefore useful in the treatment of conditions mediated by DPP-IV, such as NIDDM.
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Page/Page column 64-65
(2008/06/13)
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- Pyrimido[5,4]-dipyrimidines, pharmaceuticals containing them, their use and processes for the preparation thereof
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Pyrimido[5,4-d]pyrimidines of the general formula [Figure] which have an inhibitory effect on signal transduction mediated by tyrosine kinases, their use for the treatment of disorders, in particular of oncoses, and their preparation. Exemplary compounds are: 4-[(3-Chloro-4-fluorophenyl)amino]-6-[1-methyl-4-piperidinylamino]pyrimido[5,4-d]pyrimidine, and 4-[(3-Chloro-4-fluorophenyl)amino]-6-[trans-4-dimethyl-aminocycohexylamino]pyrimido[5,4-d]pyrimidine.
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- 1-HALOPYRIDIN-4-AMINO-4-ALKYLPIPERIDINES
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The present invention relates to novel heteroarylpiperidines of formula (I): STR1 in which Hal is a halogen atom, Alk is a C 1-C. sub.4 alkyl group and X, Y and Z are each--CH= and their salts, to a process for their preparation and to their use as drugs active as 5-HT. sub.3 agonists.
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