UFP-112 a Potent and Long-Lasting Agonist Selective for the Nociceptin/Orphanin FQ Receptor

被引：25

作者：

Calo', Girolamo ^{[1
,2
,3
]}

Rizzi, Anna ^{[1
,2
,3
]}

Cifani, Carlo ^{[4
]}

Di Bonaventura, Maria Vittoria Micioni ^{[4
]}

Regoli, Domenico ^{[1
,2
,3
]}

Massi, Maurizio ^{[4
]}

Salvadori, Severo ^{[5
,6
]}

Lambert, David G. ^{[7
]}

Guerrini, Remo ^{[5
,6
]}

机构：

[1] Univ Ferrara, Dept Expt & Clin Med, Pharmacol Sect, I-44100 Ferrara, Italy

[2] Univ Ferrara, Neurosci Ctr, I-44100 Ferrara, Italy

[3] Natl Inst Neurosci, Ferrara, Italy

[4] Univ Camerino, Dept Expt Med & Publ Hlth, I-62032 Camerino, MC, Italy

[5] Univ Ferrara, Dept Pharmaceut Sci, I-44100 Ferrara, Italy

[6] Univ Ferrara, Ctr Biotechnol, I-44100 Ferrara, Italy

[7] Univ Leicester, Dept Cardiovasc Sci, Div Anaesthesia Crit Care & Pain Management, Pharmacol & Therapeut Grp,Leicester Royal Infirma, Leicester, Leics, England

来源：

CNS NEUROSCIENCE & THERAPEUTICS | 2011年 / 17卷 / 03期

关键词：

In vitro and in vivo studies; Nociceptin; orphanin FQ; NOP receptor; NOP(-; -) mice; Pharmacological profile; UFP-112; NEUROPEPTIDE ORPHANIN FQ; VIVO PHARMACOLOGICAL CHARACTERIZATION; NEUROGENIC DETRUSOR OVERACTIVITY; CONDITIONED PLACE PREFERENCE; ALCOHOL-PREFERRING RATS; DELTA-OPIOID RECEPTOR; FORCED SWIMMING TEST; MOUSE VAS-DEFERENS; AC-RYYRIK-OL; IN-VITRO;

D O I：

10.1111/j.1755-5949.2009.00107.x

中图分类号：

Q189 [神经科学];

学科分类号：

071006 [神经生物学];

摘要：

Nociceptin/orphanin FQ (N/OFQ) controls several biological functions via selective activation of the N/OFQ peptide receptor (NOP). [(pF)Phe4Aib7Arg14Lys15]N/OFQ-NH2 (UFP-112) is an NOP receptor ligand designed using a combination of several chemical modifications in the same peptide sequence that increase NOP receptor affinity/potency and/or reduce susceptibility to enzymatic degradation. In the present review article, we summarize data from the literature and present original findings on the in vitro and in vivo pharmacological features of UFP-112. Moreover, important biological actions and possible therapeutic indications of NOP receptor agonists are discussed based on the results obtained with UFP-112 and compared with other peptide and nonpeptide NOP receptor ligands.

引用

页码：178 / 198

页数：21

共 157 条

[1]

Peripheral anti-nociceptive effect of nociceptin/orphanin FQ in inflammation and stress-induced colonic hyperalgesia in rats [J].