Protein Information

Name indol 1
Synonyms INDOL 1; INDOL1

Compound Information

Name piperazine
CAS piperazine

Reference List

PubMed Abstract RScore(About this table)
12734389 Hajos M, Hoffmann WE, Weaver RJ: Regulation of septo-hippocampal activity by 5-hydroxytryptamine (2C) receptors. J Pharmacol Exp Ther. 2003 Aug;306(2):605-15. Epub 2003 May 6.

Intravenous administration of 5-HT2C receptor agonists 1-(3-chlorophenyl) piperazine dihydrochloride (m-CPP) and [S]-2-(chloro-5-fluoro-indol-1-yl)-1-methyl-ethylamine fumarate (Ro 60-0175) dose dependently inhibited firing activity most of the recorded MS/DBv neurons and abolished theta oscillation in all tested MS/DBv and hippocampal neurons.
31(0,1,1,1) Details
12166933 Betti L, Botta M, Corelli F, Floridi M, Giannaccini G, Maccari L, Manetti F, Strappaghetti G, Tafi A, Corsano S: Alpha (1)-adrenoceptor antagonists. 4. J Med Chem. 2002 Aug 15;45(17):3603-11.

Our aim was also to study the influence of the position of both the chloro and the methoxy groups on the piperazine phenyl ring, as well as the effect of the lengthening or shortening of the polymethylene spacer linking the phenylpiperazine moiety to the terminal heterocyclic portion.
Compounds obtained by such structural optimization share a 6-(imidazol-1-yl)-, 6-(benzimidazol-1-yl)-, or 6-(indol-1-yl) pyridazin-3 (2H)-one as a common structural feature that represents an element of novelty in the SAR of arylpiperazine compounds acting toward alpha (1)-AR.
1(0,0,0,1) Details
12372512 Zhao H, Thurkauf A, He X, Hodgetts K, Zhang X, Rachwal S, Kover RX, Hutchison A, Peterson J, Kieltyka A, Brodbeck R, Primus R, Wasley JW: Indoline and piperazine containing derivatives as a novel class of mixed D (2)/D (4) receptor antagonists. Bioorg Med Chem Lett. 2002 Nov 4;12(21):3105-9.

Optimization of the lead compound 2-[-4-(4-chloro-benzyl)-piperazin-1-yl]-1-(2,3-dihydro-indol-1-yl)-ethanon e 1 by systematic structure-activity relation (SAR) studies lead to two potent compounds 2-[-4-(4-chloro-benzyl)-piperazin-1-yl]-1-(2-methy-2,3-dihydro-indol-1-yl) -ethanone 2n and 2-[-4-(4-chloro-benzyl)-piperazin-1-yl]-1-(2-methy-2,3-dihydro-indol-1-yl) -ethanone 7b.
1(0,0,0,1) Details
12372513 Zhao H, He X, Thurkauf A, Hoffman D, Kieltyka A, Brodbeck R, Primus R, Wasley JW: Indoline and piperazine containing derivatives as a novel class of mixed D (2)/D (4) receptor antagonists. Bioorg Med Chem Lett. 2002 Nov 4;12(21):3111-5.

A series of chiral benzylpiperazinyl-1-(2,3-dihydro-indol-1-yl) ethanone derivatives were prepared and examined for their affinity at dopamine D (2) and D (4) receptors.
1(0,0,0,1) Details