| Name | 5 HT7 |
|---|---|
| Synonyms | 5 HT 7; 5 HT X; 5 HT X serotonin receptor; 5 HT7; 5 hydroxytryptamine (serotonin) receptor 7 (adenylate cyclase coupled); 5 hydroxytryptamine 7 receptor; 5 hydroxytryptamine receptor 7; 5 hydroxytryptamine receptor 7 isoform d… |
| Name | piperazine |
|---|---|
| CAS | piperazine |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 19560916 | Zajdel P, Subra G, Verdie P, Gabzdyl E, Bojarski AJ, Duszynska B, Martinez J, Pawlowski M: Sulfonamides with the N-alkyl-N'-dialkylguanidine moiety as 5-HT7 receptor ligands. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4827-31. Epub 2009 Jun 13. A series of arylsulfonamides containing incorporated in the structure of secondary amines (piperidine, piperazine) was synthesized on SynPhase Lanterns and evaluated for 5-HT (1A), 5-HT (2A), and 5-HT (7) receptors. |
83(1,1,1,3) | Details |
| 18456500 | Yoon J, Yoo EA, Kim JY, Pae AN, Rhim H, Park WK, Kong JY, Park Choo HY: Preparation of piperazine derivatives as 5-HT7 receptor antagonists. . Bioorg Med Chem. 2008 May 15;16(10):5405-12. Epub 2008 Apr 15. |
63(0,2,2,3) | Details |
| 17649988 | Leopoldo M, Lacivita E, Contino M, Colabufo NA, Berardi F, Perrone R: Structure-activity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides, a class of 5-HT7 receptor agents. 2. J Med Chem. 2007 Aug 23;50(17):4214-21. Epub 2007 Jul 25. Here we report the synthesis of N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinealkylamides 16-29 that were designed to elucidate both structure-affinity and -activity relationships for the 5-HT7 receptor, by targeting the substituent in 2-position of the aryl linked to the piperazine ring. |
36(0,1,1,6) | Details |
| 18800769 | Leopoldo M, Lacivita E, De Giorgio P, Fracasso C, Guzzetti S, Caccia S, Contino M, Colabufo NA, Berardi F, Perrone R: Structural modifications of N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides: influence on lipophilicity and 5-HT7 receptor activity. J Med Chem. 2008 Sep 25;51(18):5813-22. Starting from the previously reported 5-HT 7 receptor agents 4-7 with N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamide structure, the 1-(2-methylthiophenyl)-, 1-(2-diphenyl)-, 1-(2-isopropylphenyl)-, and 1-(2-methoxyphenyl) piperazine derivatives 8-31 were designed with the primary aim to obtain new compounds endowed with suitable physicochemical properties for rapid and extensive penetration into the brain. |
34(0,1,1,4) | Details |
| 15588097 | Leopoldo M, Berardi F, Colabufo NA, Contino M, Lacivita E, Niso M, Perrone R, Tortorella V: Structure-affinity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinealkylamides, a new class of 5-hydroxytryptamine7 receptor agents. J Med Chem. 2004 Dec 16;47(26):6616-24. In relation to 5-HT7 receptor affinity, receptor binding studies indicated that (i) the optimal alkyl chain length was five methylenes, (ii) an unsubstituted 1,2,3,4-tetrahydronaphthalenyl nucleus was preferred, and (iii) the substitution pattern of the aryl ring linked to the piperazine ring played a crucial role. |
34(0,1,1,4) | Details |
| 12570387 | Perrone R, Berardi F, Colabufo NA, Lacivita E, Leopoldo M, Tortorella V: Synthesis and structure-affinity relationships of 1-[omega-(4-aryl-1-piperazinyl) alkyl]-1-aryl ketones as 5-HT (7) receptor ligands. J Med Chem. 2003 Feb 13;46(4):646-9. The presence of a or methoxy substituent on aryl ketone moiety, alkyl chain length, and the nature of N-1-piperazine substituent were explored. 6-[4-(3-Benzisoxazolyl)-1-piperazinyl]-1-(2-hydroxyphenyl)-1- (40) and its methoxy analogue 43 exhibited high 5-HT (7) receptor affinities (Ki = 2.93 nM and 0.90 nM, respectively) and agonist properties when tested for 5-HT (7) receptor-mediated relaxation of substance P-induced guinea-pig ileum contraction. |
33(0,1,1,3) | Details |
| 15033384 | Hedlund PB, Kelly L, Mazur C, Lovenberg T, Sutcliffe JG, Bonaventure P: 8-OH-DPAT acts on both 5-HT1A and 5-HT7 receptors to induce hypothermia in rodents. Eur J Pharmacol. 2004 Mar 8;487(1-3):125-32. The 5-HT (1A) receptor antagonist (S)-N-tert-butyl-3-(4-(2-methoxyphenyl) piperazine-1-yl)-2-phenylpropanamid e (WAY-100135) (10 mg/kg, i.p.) inhibited the effect of 8-OH-DPAT at all doses in rats and mice. |
5(0,0,0,5) | Details |
| 15727878 | Bojarski AJ, Paluchowska MH, Duszynska B, Klodzinska A, Tatarczynska E, Chojnacka-Wojcik E: 1-Aryl-4-(4-succinimidobutyl) piperazines and their conformationally constrained analogues: synthesis, binding to (5-HT1A, 5-HT2A, 5-HT7), alpha1-adrenergic, and dopaminergic D2 receptors, and in vivo 5-HT1A functional characteristics. Bioorg Med Chem. 2005 Mar 15;13(6):2293-303. Starting with the structure of potent 5-HT (1A) ligands, that is, MM77 [1-(2-methoxyphenyl)-4-(4-succinimidobutyl) piperazine, 4] and its constrained version 5 (MP349), previously obtained in our laboratory, a series of their direct analogues with differently substituted aromatic ring (R=H, m-Cl, m-CF (3), m-OCH (3), p-OCH (3)) were synthesized. |
4(0,0,0,4) | Details |
| 17584957 | Papageorgiou A, Denef C: Stimulation of growth hormone release by in cultured rat anterior pituitary cell aggregates: evidence for mediation by 5-HT2B, 5-HT7, 5-HT1B, and ketanserin-sensitive receptors. Endocrinology. 2007 Sep;148(9):4509-22. Epub 2007 Jun 21. Basal GH release was stimulated by the 5-HTR2 agonists 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane, m-chlorophenyl piperazine, and alpha-methyl 5-carboxytryptamine (agonist at 5-HTR1, -5, and -7); (preferential 5-HTR7 agonist); and the selective 5-HTR1B agonist CP93129 but not the 5-HTR1A agonists 7-(dipropylamino) tetralin-1-ol-8--2-(di-n-propylamino) tetralin and the 5-HTR1B/D agonist |
4(0,0,0,4) | Details |
| 12692389 | Saifullah AS, Tomioka K: 5-HT (7)-like receptors mediate serotonergic modulation of photo-responsiveness of the medulla bilateral neurons in the cricket, Gryllus bimaculatus. Zoolog Sci. 2003 Mar;20(3):303-9. |
4(0,0,0,4) | Details |
| 16002064 | Takeda H, Tsuji M, Ikoshi H, Yamada T, Masuya J, Iimori M, Matsumiya T: Effects of a 5-HT7 receptor antagonist DR4004 on the exploratory behavior in a novel environment and on brain monoamine dynamics in mice. Eur J Pharmacol. 2005 Jul 25;518(1):30-9. Furthermore, co-injection of the selective reuptake inhibitor 1-(2-[bis (4-fluorophenyl) methoxy] ethyl)-4-(3-phenylpropyl) piperazine (GBR12909; 1.25-5 mg/kg, i.p.) or the selective reuptake inhibitor fluvoxamine (20 mg/kg, i.p.) significantly reversed the DR4004 (10 mg/kg, i.p.)-induced decrease in locomotor activity in the hole-board test. |
3(0,0,0,3) | Details |
| 11220775 | Smith BN, Sollars PJ, Dudek FE, Pickard GE: Serotonergic modulation of retinal input to the mouse suprachiasmatic nucleus mediated by 5-HT1B and 5-HT7 receptors. J Biol Rhythms. 2001 Feb;16(1):25-38. As previously described in the hamster, a mixed 5-HT (1A/1B) receptor agonist, 1-[3-(trifluoromethyl) phenyl]-piperazine hydrochloride (TFMPP), reduced the amplitude of glutamatergic excitatory postsynaptic currents (EPSCs) evoked by selectively stimulating the optic nerve of wild-type mice. |
2(0,0,0,2) | Details |
| 19190523 | Foong JP, Bornstein JC: antagonists NAN-190 and SB 269970 block alpha2-adrenoceptors in the guinea pig. Neuroreport. 2009 Feb 18;20(3):325-30. The initial aim of this study was to use intracellular recording and specific antagonists to identify roles of 5-HT1A and 5-HT7 receptors of submucosal noncholinergic secretomotor neurons of guinea pig ileum, in vitro. |
2(0,0,0,2) | Details |
| 15582454 | Chu W, Tu Z, McElveen E, Xu J, Taylor M, Luedtke RR, Mach RH: Synthesis and in vitro binding of N-phenyl piperazine analogs as potential D3 receptor ligands. Bioorg Med Chem. 2005 Jan 3;13(1):77-87. Binding studies were also conducted to determine if the compounds bound to sigma (sigma (1) and sigma (2)) and (5-HT (1A), 5-HT (2A), 5-HT (2B), 5-HT (2C), 5-HT (3), 5-HT (4), 5-HT (5), 5-HT (6), and 5-HT (7)) receptors. |
1(0,0,0,1) | Details |
| 17825569 | Paluchowska MH, Bugno R, Duszynska B, Tatarczynska E, Nikiforuk A, Lenda T, Chojnacka-Wojcik E: The influence of modifications in imide fragment structure on 5-HT (1A) and 5-HT (7) receptor affinity and in vivo pharmacological properties of some new 1-(m-trifluoromethylphenyl) piperazines. Bioorg Med Chem. 2007 Nov 15;15(22):7116-25. Epub 2007 Aug 22. New, flexible (7, 9, 11 and 13) and rigid (8, 10, 12 and 14) imides with a 1-(m-trifluorophenyl) piperazine fragment and a tetramethylene or a 1e,4e-cyclohexylene spacer, respectively, showed very high affinity (K (i)=0.3-34 nM) and agonistic in vivo activity for 5-HT (1A) receptors. |
2(0,0,0,2) | Details |
| 16386718 | Egashira N, Yano A, Ishigami N, Mishima K, Iwasaki K, Fujioka M, Matsushita M, Nishimura R, Fujiwara M: Investigation of mechanisms mediating 8-OH-DPAT-induced impairment of spatial memory: involvement of 5-HT1A receptors in the dorsal hippocampus in rats. Brain Res. 2006 Jan 19;1069(1):54-62. Epub 2006 Jan 4. The purpose of this study was to identify mechanisms that mediate the impairment of spatial memory induced by 8--2-(di-n-propylamino) tetralin (8-OH-DPAT), a 5-HT1A/5-HT7 receptor agonist, in the eight-arm radial maze in rats. |
1(0,0,0,1) | Details |
| 12177685 | Hoerr R, Noeldner M: Ensaculin (KA-672 HCl): a multitransmitter approach to dementia treatment. CNS Drug Rev. 2002 Summer;8(2):143-58. Ensaculin, a novel benzopyranone substituted with a piperazine moiety, showed memory-enhancing effects in paradigms of passive and conditioned avoidance in both normal and artificially amnesic rodents. In receptor-binding studies, ensaculin was found to have high affinities to serotonergic 5-HT (1A) and 5-HT (7) receptors, adrenergic alpha (1), and dopaminergic D (2) and D (3) receptors. |
1(0,0,0,1) | Details |
| 16710314 | McCreary AC, Glennon JC, Ashby CR Jr, Meltzer HY, Li Z, Reinders JH, Hesselink MB, Long SK, Herremans AH, van Stuivenberg H, Feenstra RW, Kruse CG: SLV313 (1-(2,3-dihydro-benzo [1,4] dioxin-5-yl)-4- [5-(4--phenyl)-pyridin-3-ylmethyl]-piperazine monohydrochloride): a novel dopamine D2 receptor antagonist and 5-HT1A receptor agonist potential antipsychotic drug. Neuropsychopharmacology. 2007 Jan;32(1):78-94. Epub 2006 May 17. |
0(0,0,0,0) | Details |
| 15005884 | Leopoldo M, Berardi F, Colabufo NA, Contino M, Lacivita E, Perrone R, Tortorella V: Studies on 1-arylpiperazine derivatives with affinity for rat 5-HT7 and 5-HT1A receptors. J Pharm Pharmacol. 2004 Feb;56(2):247-55. Several 1-aryl-4-(2-arylethyl) piperazine derivatives were synthesized and tested in-vitro for their binding affinity for 5-HT (7) and 5-HT (1A) receptors. |
164(2,2,2,4) | Details |
| 17517509 | Leopoldo M, Lacivita E, Colabufo NA, Niso M, Berardi F, Perrone R: Bivalent ligand approach on 4-[2-(3-methoxyphenyl) ethyl]-1-(2-methoxyphenyl) piperazine: synthesis and binding affinities for 5-HT (7) and 5-HT (1A) receptors. Bioorg Med Chem. 2007 Aug 1;15(15):5316-21. Epub 2007 May 6. |
113(1,2,2,3) | Details |