109960-06-7Relevant academic research and scientific papers
1-(Phenyl)isoquinoline carboxamides: A novel class of subtype selective inhibitors of thyrotropin-releasing hormone (TRH) receptors
Jiang, Jian-Kang,Thomas, Craig J.,Neumann, Susanne,Lu, Xinping,Rice, Kenner C.,Gershengorn, Marvin C.
, p. 733 - 736 (2007/10/03)
We report the synthesis of and binding to the two subtypes of mouse thyrotropin-releasing hormone (TRH) receptors, TRH-R1 and TRH-R2, of several 1-(phenyl)isoquinoline carboxamide analogues. These analogues showed a degree of selectivity for binding at TR
Synthesis of N-methyl-N-(1-methylpropyl)-1-(2-chlorophenyl)-isoquinoline-3-[11C]ca rboxamide ([11C-carbonyl]PK11195) and some analogues using [11C]carbon monoxide and 1-(2-chlorophenyl)isoquinolin-3-yl triflate
Rahman, Obaidur,Kihlberg, Tor,Langstroem, Bengt
, p. 2699 - 2703 (2007/10/03)
The benzodiazepine receptor ligand, N-methyl-N-(1-methylpropyl)-1-(2-chlorophenyl)isoquinoline-3-carboxamide (PK11195), and five structurally related analogues were 11C-labelled via a palladium-mediated carbonylation using [11C]carbon monoxide, 1-(2-chlorophenyl)isoquinolin-3-yl trifluoromethanesulfonate and various amines. The 11C-labelled products were obtained with decay-corrected radiochemical yields in the range of 10-55% and with high specific radioactivity (e.g. 200-900 GBq μmol-1). The radiochemical purity of the final products exceeded 98%. In a typical experiment starting with 3.75 GBq [11C]carbon monoxide, 0.57 GBq of LC-purified products were obtained within 35 min of the start of the carbonylation reaction. For confirmation of the labelling position, N-(1-methylethyl)-1-(2-chlorophenyl)-isoquinoline-3-(13C)carboxamide was prepared and analysed by NMR. The precursor 1-(2-chlorophenyl)isoquinolin-3-yl trifluoromethanesulfonate was synthesised in five steps starting from 2-chlorobenzophenone. The precursor N-methyl-sec-butylamine was prepared from sec-butylamine by the reaction with ethyl chloroformate followed by reduction with LiAlH4. The non-radioactive reference compounds for the analogues were synthesised from 1-(2-chlorophenyl)isoquinoline-3-carboxylic acid and the appropriate amines.
Novel irreversible ligands specific for 'peripheral' type benzodiazepine receptors: (±)-, (+)-, and (-)-1-(2-chlorophenyl)-N-(1 methylpropyl)-N-(2-isothiocyanatoethyl)-3-isoquinolinecarboxamide and 1-(2-isothiocyanatoethyl)-7-chloro-1,3-dihydro-5-(4-chlor
Newman,Lueddens,Skolnick,Rice
, p. 1901 - 1905 (2007/10/02)
Novel ligands that bind irreversibly and selectively to 'peripheral' type benzodiazepine receptors (PBR) have been prepared. These compounds inhibits radiolabeled binding to PBR in the nanomolar range. The 2-isothiocyanatoethyl analogue of Ro 5-4864 (1-me
