Receptor ligands for

Tables. Selected non -peptide receptor ligands for diagnostic radiopharmaceuticals ...

F-18]fluorotropapride and 4-[F-18]fluorotropapride, 2 specific D2-receptor ligands for positron emission tomography—NCA syntheses and animal studies, Appl. Radiat. Isot. 43 (1992) 1265-1274. 

C.S. Dence, C.S. John, W.D. Bowen, M.J. Welch, Synthesis and evaluation of [F-18] labeled benzamides High affinity sigma receptor ligands for PET imaging, Nucl. Med. Biol. 24 (1997) 333-340. 

Notwithstanding the clinical use of many 5-HTj, receptor ligands for the treatment of anxiety, only one report was found that has investigated the potential to influence cognitive performance. In patients with a generalized anxiety disorder, Lucki et al. [1987] compared the effect of buspirone [at 5 and 10 mg] with that of diazepam [5 mg]. Diazepam impaired performance buspirone was without effect. 

Dichloropentane (1) and 1,6-dibromohexane (2) can be converted to the monofluoro derivatives 3 and 4 by heating with potassium fluoride in ethylene glycol at 125 C. The yields are low (< 20 %).74 These compounds are of interest because they can be converted to fluoroal-kylamines for use as synthetic intermediates in the preparation of histamine receptor ligands for use in positron emission tomography. 

Schieck C, Lee KS, Jones DW, et al. [123I]DOI a novel 5-HT2 serotonin receptor ligand for SPECT imaging 26th National Medicinal Chemistry Symposium, Richmond, VA, 1998. 

The 1,4-oxazepanes 133 were prepared by a ring closing reaction of epichlorohydrin with the appropriate A -benzyl ethanolamine derivative and subsequent introduction of the second aryl substituent group (A). These 1,4-oxazepanes were assessed as selective dopamine D4 receptor ligands. For example the compound 133 (R = OCH2CH3, R = H, R = Cl, R = R ... 

Very recently, Gmeiner and co-workers prepared metallocene-derived receptor ligands for G-protein-coupled receptors (GPGRs) such as dopamine and serotonin receptor subtypes. They used ruthenocene and ferrocene derivatives, in which the metallocenes replaced cyclophanes as so-called fancy bioisosters. In particular, compound 31 (Scheme 32) showed sub-nanomolar affinity and high specificity for the dopamine D4 and serotonin HTia receptor subtypes, and may thus be a suitable lead structure for the further development of selective organometallic GPCR ligands. 

The Bartoli indole synthesis has found utility in medicinal chemistry despite its infancy. For instance, the nitro-diarylether ketone was protected as a ketal and treated with vinylmagnesium bromide to afford the indole derivative. The resulting phenyl-indolyl ether is an intermediate for preparing serotonin (5HT) receptor ligands for treatment of nervous system disorders. Specifically, the diphenyl ether ligands exhibited activity as 5HT2 antagonists. 

Rowland DJ, Tu Z, Mach RH, Welch MJ. Investigation of a new sigma 2 receptor ligand for detection of breast cancer. Labelled Compd Radiopharm 2003 46 S6. 

Identification and usefulness of 5-HT6 receptor ligands for CNS disorders such as schizophrenia, depression and impairment of learning and memory has been the focus of several reports in the last decade. Earlier we have disclosed 3-aminoalkoxy-N-arylsulfonyl indoles (I) as highly potent and... 

Gewirtz GR, Gorman JM, Volavka J, Macaluso J (1994) BMY 14802, a sigma receptor ligand for the treatment of schizophrenia. Neuropsychopharmacology 10 37 0... 

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