- Methods for cancer imaging and therapy using benzamine compounds
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The present invention relates to a class of compounds having affinity for certain cancer cells, e.g. lung carcinomas, colon carcinomas, renal carcinomas, prostate carcinomas, breast carcinomas, malignant melanomas, gliomas, neuroblastomas and pheochromocy
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- Benzamide compounds for cancer imaging and therapy
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The present invention relates to a class of compounds having affinity for certain cancer cells, e.g. lung carcinomas, colon carcinomas, renal carcinomas, prostate carcinomas, breast carcinomas, malignant melanomas, gliomas, neuroblastomas and pheochromocy
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- Potential antipsychotic agents. 7. Synthesis and antidopaminergic properties of the atypical highly potent (S)-5-bromo-2,3-dimethoxy-N-[(1-ethyl-2-pyrrolidinyl)methyl]benzamide and related compounds. A comparative study
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(S)-5-Bromo-2,3-dimethoxy-N-[(1-ethyl-2-pyrrolidinyl)methyl]benzamide (6) and some related compounds, i.e. the R isomer 7, the 3-hydroxy analogue 8, the desbromo derivative 9, the monomethoxy compound 10, and the 2,4-dimethoxy analogue 11, have been synth
- Hogberg,De Paulis,Johansson,Kumar,Hall,Ogren
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p. 2305 - 2309
(2007/10/02)
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- Synthesis and characterization of iodobenzamide analogues: Potential D-2 dopamine receptor imaging agents
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(S)-N-[(1-Ethyl-2-pyrrolidinyl)methyl]-2-hydroxy-3-iodo-6-methoxybenza mide ([123I]IBZM) is a central nervous system (CNS) D-2 dopamine receptor imaging agent. In order to investigate the versatility of this parent structure in specific dopamine receptor localization and the potential for developing new dopamine receptor imaging agents, a series of new iodinated benzamides with fused ring systems, naphthalene (INAP) and benzofuran (IBF), was synthesized and radiolabeled, and the in vivo and in vitro biological properties were characterized. The best analogue of IBZM is IBF (21). The specific binding of [125I]IBF (21) with rat striatal tissue preparation was found to be saturable and displayed a K(d) of 0.106 ± 0.015 nM. Competition data of various receptor ligands (for [125I]IBF (21) binding show the following rank order of potency: spiperone > IBF (21) > IBZM > (+)-butaclamol > (±)-ADTN,6,7 > ketanserin > SCH-23390 >> propranolol. The in vivo biodistribution results confirm that [125I]IBF (21) concentrated in the striatal area after iv injection into rats. The study demonstrates that [123I]IBF (21) is a potential agent for imaging CNS D-2 dopamine receptors.
- Murphy,Kung,Kung,Billings
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p. 171 - 178
(2007/10/02)
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- CARBOXAMIDES USEFUL AS ANTIEMETIC OR ANTIPSYCHOTIC AGENTS
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Carboxamides represented by the formula (I): STR1 wherein Z represents the carbon atoms necessary to complete a 5-to 7-membered ring, R 1, R 2, and R 3 may be the same or different and are selected from the group consisting of a hydrogen atom, a lower alkyl group, a cycloalkyl group, a halogen atom, an amino group, a lower alkylamino group, an alkoxy group, an acylamido group, a sulfonamido group, and a nitro group; andA represents an aminoalkyl moiety and acid addition salts thereof.
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