Pirimidinilpiperazin

Pirimidinilpiperazin
Nazivi
	IUPAC naziv 2-(piperazin-1-il)pirimidin
Identifikacija
3D model (Jmol)	interaktivna slika;
ChemSpider	80080 ;
ECHA InfoCard	100.040.107
PubChem C ID	88747;
	SMILES n1cccnc1N2CCNCC2; ; ; ; ; ;
Svojstva
Hemijska formula	C8H12N4
Molarna masa	164,21 g/mol
	Ukoliko nije drugačije napomenuto, podaci se odnose na standardno stanje materijala (na 25 °C [77 °F], 100 kPa).
	verifikuj (šta je ?)
	Reference infokutije

1-(2-Pirimidinil)piperazin (1-PP, 1-PmP) je hemijsko jedinjenje koje je derivat piperazina. Poznato je da deluje kao antagonist α₂-adrenergičkog receptora,^[3] i u znatno manjoj meri kao parcijalni agonist 5-HT_1A receptora.^[4] 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.^[3]^[5] 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. PMID 20970519. doi:10.1016/j.drudis.2010.10.003. уреди
^ 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.
^ ^а ^б 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. PMID 1681447. doi:10.1016/0028-3908(91)90176-C.
^ 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. PMID 12438536. doi:10.1124/jpet.102.036798.
^ 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. PMID 12505530. doi:10.1016/S0014-2999(02)02814-5.

Spoljašnje veze

[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. PMID 20970519. doi:10.1016/j.drudis.2010.10.003. уреди

[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.

[pmid1681447-3] а ^б 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. PMID 1681447. doi:10.1016/0028-3908(91)90176-C.

[pmid12438536-4] 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. PMID 12438536. doi:10.1124/jpet.102.036798.

[pmid12505530-5] 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. PMID 12505530. doi:10.1016/S0014-2999(02)02814-5.

[1]

[2]

[3]

[4]

[5]