[HTML][HTML] Morphine-like opiates selectively antagonize receptor-arrestin interactions

P Molinari, V Vezzi, M Sbraccia, C Grò, D Riitano… - Journal of biological …, 2010 - ASBMB
The addictive potential of opioids may be related to their differential ability to induce G protein
signaling and endocytosis. We compared the ability of 20 ligands (sampled from the main …

Synthesis and evaluation as NOP ligands of some spiro [piperidine-4, 2′(1′ H)-quinazolin]-4′(3′ H)-ones and spiro [piperidine-4, 5′(6′ H)-[1, 2, 4] triazolo [1, 5 …

C Mustazza, A Borioni, I Sestili, M Sbraccia… - Chemical and …, 2006 - jstage.jst.go.jp
Some spiro [piperidine-4, 2 (1 H)-quinazolin]-4 (3 H)-ones 3 and spiro [piperidine-4, 5 (6 H)-[1,
2, 4] triazolo-[1, 5-c] quinazolines] 4 were synthesized and evaluated as ligands of the …

A new synthetic approach of N-(4-amino-2-methylquinolin-6-yl)-2-(4-ethylphenoxymethyl) benzamide (JTC-801) and its analogues and their pharmacological …

…, A Rodomonte, L Turchetto, M Sbraccia… - European journal of …, 2004 - Elsevier
A series of 4-amino-2-methylquinoline and 4-aminoquinazoline derivatives, including the
reference NOP antagonist JTC-801, were synthesized by an alternative pathway and their in …

[HTML][HTML] Promiscuous coupling at receptor-Gα fusion proteins: the receptor of one covalent complex interacts with the α-subunit of another

P Molinari, C Ambrosio, D Riitano, M Sbraccia… - Journal of Biological …, 2003 - ASBMB
Fusion proteins between heptahelical receptors (GPCR) and G protein α-subunits show
enhanced signaling efficiency in transfected cells. This is believed to be the result of molecular …

“Induced-fit” mechanism for catecholamine binding to the β2-adrenergic receptor

R Del Carmine, P Molinari, M Sbraccia… - Molecular …, 2004 - ASPET
We engineered single and multiple mutations of serines 203, 204, and 207 in the fifth
transmembrane domain of the β 2 -adrenergic receptor, a region known to interact with hydroxyl …

Mutations inducing divergent shifts of constitutive activity reveal different modes of binding among catecholamine analogues to the β2‐adrenergic receptor

RD Carmine, C Ambrosio, M Sbraccia… - British journal of …, 2002 - Wiley Online Library
We compared the changes in binding energy generated by two mutations that shift in
divergent directions the constitutive activity of the human β 2 adrenergic receptor (β 2 AR). A …

Synthesis and structure–activity relationship studies in serotonin 5-HT4 receptor ligands based on a benzo [de][2, 6] naphthridine scaffold

…, F De Rienzo, MC Menziani, M Sbraccia… - European Journal of …, 2014 - Elsevier
A small series of serotonin 5-HT 4 receptor ligands has been designed from flexible 2-methoxyquinoline
compounds 7a,b by applying the conformational constraint approach. Ligands …

Synthesis and Pharmacological Evaluation of 1,2-Dihydrospiro[isoquinoline-4(3H),4′-piperidin]-3-ones as Nociceptin Receptor Agonists

…, A Borioni, I Sestili, M Sbraccia… - Journal of medicinal …, 2008 - ACS Publications
Some synthesized 1,2-dihydrospiro[isoquinoline-4(3H),4′-piperidin]-3-ones were evaluated
as ligands for nociceptin receptor (NOP receptor). Their affinity was established by binding …

Synthesis of New 4‐Heteroaryl‐2‐Phenylquinolines and Their Pharmacological Activity as NK‐2/NK‐3 Receptor Ligands

…, C Mustazza, I Sestili, M Sbraccia… - … der Pharmazie: An …, 2007 - Wiley Online Library
Substituted 4‐heteroaryl‐2‐phenylquinolines were synthesized and tested on NK‐2 and NK‐3
receptors in order to get a better insight in the structure‐activity relationship. On the whole…

In VivoCHCl3Bioactivation, Toxicokinetics, Toxicity, and Induced Compensatory Cell Proliferation in B6C3F1 Male Mice

S Gemma, S Faccioli, P Chieco, M Sbraccia… - Toxicology and applied …, 1996 - Elsevier
Chloroform carcinogenicity has often been associated with acute tissue damage and
consequent compensatory cell proliferation. However, available data do not fully support this …