Pirimidinilpiperazin

Pirimidinilpiperazin
	2-(piperazin-1-il)pirimidin
Identifikacija
PubChem	88747
ChemSpider	80080
ChEMBL	CHEMBL724
Jmol-3D slike	Slika 1
SMILES
	n1cccnc1N2CCNCC2
InChI
	InChI=1S/C8H12N4/c1-2-10-8(11-3-1)12-6-4-9-5-7-12/h1-3,9H,4-7H2 ; Kod: MRBFGEHILMYPTF-UHFFFAOYSA-N InChI=1S/C8H12N4/c1-2-10-8(11-3-1)12-6-4-9-5-7-12/h1-3,9H,4-7H2 InChI=1S/C8H12N4/c1-2-10-8(11-3-1)12-6-4-9-5-7-12/h1-3,9H,4-7H2; Kod: MRBFGEHILMYPTF-UHFFFAOYSA-N
Svojstva
Molekulska formula	C8H12N4
Molarna masa	164,21 g/mol
	(šta je ovo?) (verifikuj) ; Ukoliko nije drugačije napomenuto, podaci se odnose na standardno stanje (25 °C, 100 kPa) materijala
	Infobox references

1-(2-Pirimidinil)piperazin (1-PP, 1-PmP) je hemijsko jedinjenje koje je derivat piperazina. Poznato je da deluje kao antagonist α₂-adrenergičkog receptora,^[5] i u znatno manjoj meri kao parcijalni agonist 5-HT_1A receptora.^[6] On nema primetni afinitet za D₂ ili α₁-adrenergički receptor.

Poznat je znata broj lekova koji su pirimidinilpiperazinski derivati, neki od njih su:

Buspiron - Anksiolitik
Dasatinib - Lek protiv kancera
Eptapiron - Anksiolitik
Gepiron - Anksiolitik
Ipsapiron - Anksiolitik
Piribedil - Antiparkinsonski agens
Revospiron - Anksiolitik
Tandospiron - Anksiolitik
Tirilazad - Alfa blokator
Umespiron - Anksiolitik
Zalospiron - Anksiolitik

Anksiolitici se još klasifikuju kao azapironi usled prisustva Azaspirodekandionskog motiva u njihovoj strukturi. 1-PP je zajednički metabolit većine ako ne i svih gore navedenih agenasa.^[5]^[7] Alnespiron, binospiron, i enilospiron su azapironi, ali nisu piperazini, te stoga njihov metabolizam ne proizvodi 1-PP.

Reference

↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit
↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.
↑ Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846. edit
↑ Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594. edit
↑ ^5,0 ^5,1 Blier; Curet, O.; Chaput, Y.; De Montigny, C. (1991). „Tandospirone and its metabolite, 1-(2-pyrimidinyl)-piperazine--II. Effects of acute administration of 1-PP and long-term administration of tandospirone on noradrenergic neurotransmission”. Neuropharmacology 30 (7): 691–701. DOI:10.1016/0028-3908(91)90176-C. PMID 1681447. Greška u referenci: Nevaljana oznaka <ref>; naziv "pmid1681447" je zadan više puta s različitim sadržajem
↑ Zuideveld, K. P.; Rusic-pavletic, J.; Maas, H. J.; Peletier, L. A.; Van Der Graaf, P. H.; Danhof, M. (2002). „Pharmacokinetic-pharmacodynamic modeling of buspirone and its metabolite 1-(2-pyrimidinyl)-piperazine in rats”. The Journal of Pharmacology and Experimental Therapeutics 303 (3): 1130–1137. DOI:10.1124/jpet.102.036798. PMID 12438536.
↑ Astier; Lambás Señas, L.; Soulière, F.; Schmitt, P.; Urbain, N.; Rentero, N.; Bert, L.; Denoroy, L. et al (2003). „In vivo comparison of two 5-HT1A receptors agonists alnespirone (S-20499) and buspirone on locus coeruleus neuronal activity”. European Journal of Pharmacology 459 (1): 17–26. DOI:10.1016/S0014-2999(02)02814-5. PMID 12505530.

Spoljašnje veze

Portal Hemija

[1] Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit

[2] Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.

[3] Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846. edit

[4] Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594. edit

[pmid1681447-5] 5,0 ^5,1 Blier; Curet, O.; Chaput, Y.; De Montigny, C. (1991). „Tandospirone and its metabolite, 1-(2-pyrimidinyl)-piperazine--II. Effects of acute administration of 1-PP and long-term administration of tandospirone on noradrenergic neurotransmission”. Neuropharmacology 30 (7): 691–701. DOI:10.1016/0028-3908(91)90176-C. PMID 1681447. Greška u referenci: Nevaljana oznaka <ref>; naziv "pmid1681447" je zadan više puta s različitim sadržajem

[pmid12438536-6] Zuideveld, K. P.; Rusic-pavletic, J.; Maas, H. J.; Peletier, L. A.; Van Der Graaf, P. H.; Danhof, M. (2002). „Pharmacokinetic-pharmacodynamic modeling of buspirone and its metabolite 1-(2-pyrimidinyl)-piperazine in rats”. The Journal of Pharmacology and Experimental Therapeutics 303 (3): 1130–1137. DOI:10.1124/jpet.102.036798. PMID 12438536.

[pmid12505530-7] Astier; Lambás Señas, L.; Soulière, F.; Schmitt, P.; Urbain, N.; Rentero, N.; Bert, L.; Denoroy, L. et al (2003). „In vivo comparison of two 5-HT1A receptors agonists alnespirone (S-20499) and buspirone on locus coeruleus neuronal activity”. European Journal of Pharmacology 459 (1): 17–26. DOI:10.1016/S0014-2999(02)02814-5. PMID 12505530.

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