714978-26-4Relevant articles and documents
Discovery of N-(4-Aminobutyl)-N′-(2-methoxyethyl)guanidine as the First Selective, Nonamino Acid, Catalytic Site Inhibitor of Human Dimethylarginine Dimethylaminohydrolase-1 (hDDAH-1)
Lunk, Ina,Litty, Felix-Alexander,Hennig, Sven,Vetter, Ingrid R.,Kotthaus, Jürke,Altmann, Karin S.,Ott, Gudrun,Havemeyer, Antje,Garciá, Carmen Carrillo,Clement, Bernd,Schade, Dennis
supporting information, p. 425 - 432 (2020/02/04)
N-(4-Aminobutyl)-N′-(2-methoxyethyl)guanidine (8a) is a potent inhibitor targeting the hDDAH-1 active site (Ki = 18 μM) and derived from a series of guanidine- A nd amidine-based inhibitors. Its nonamino acid nature leads to high selectivities
A bivalent ligand (KDN-21) reveals spinal δ and κ opioid receptors are organized as heterodimers that give rise to δ1 and δ2 phenotypes. Selective targeting of δ-κ heterodimers
Bhushan, Rashmi G.,Sharma, Shiv K.,Xie, Zhihua,Daniels, David J.,Portoghese, Philip S.
, p. 2969 - 2972 (2007/10/03)
In view of recent pharmacological studies suggesting the existence of δ-κ opioid receptor heterodimers/oligomers in the spinal cord, we have synthesized and evaluated (intrathecally in mice) a series of bivalent ligands (KDN series) containing κ and δ antagonist pharmacophores. Pharmacological and binding data have provided evidence for the bridging of spinal δ-κ receptor heterodimers by KDN-21 and for their identification as δ1 and κ2. The selectivity profile of KDN-21 and the apparent absence of coupled δ 1-κ2 phenotypes in the brain suggest a new approach for targeting receptors.
