Unique high-affinity synthetic μ-opioid receptor agonists with central-and systemic-mediated analgesia

Y Okada, Y Tsuda, Y Fujita, T Yokoi… - Journal of medicinal …, 2003 - ACS Publications
Unique opioid mimetic substances containing identical N-terminal aromatic residues
separated by an unbranched alkyl chain containing two to eight methylene groups were …

Structure–Activity Relationships and Discovery of a G Protein Biased μ Opioid Receptor Ligand, [(3-Methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro …

XT Chen, P Pitis, G Liu, C Yuan… - Journal of medicinal …, 2013 - ACS Publications
The concept of “ligand bias” at G protein coupled receptors has been introduced to describe
ligands which preferentially stimulate one intracellular signaling pathway over another …

Bifunctional [2',6'-Dimethyl-l-tyrosine]endomorphin-2 Analogues Substituted at Position 3 with Alkylated Phenylalanine Derivatives Yield Potent Mixed μ-Agonist/δ …

T Li, K Shiotani, A Miyazaki, Y Tsuda… - Journal of medicinal …, 2007 - ACS Publications
Endomorphin-2 (H-Tyr-Pro-Phe-Phe-NH2) and [Dmt1] EM-2 (Dmt= 2 ', 6 '-dimethyl-l-
tyrosine) analogues, containing alkylated Phe3 derivatives, 2 '-monomethyl (2, 2 '), 3 ', 5 ' …

[HTML][HTML] Retention of supraspinal delta-like analgesia and loss of morphine tolerance in δ opioid receptor knockout mice

Y Zhu, MA King, AGP Schuller, JF Nitsche, M Reidl… - Neuron, 1999 - cell.com
Gene targeting was used to delete exon 2 of mouse DOR-1, which encodes the δ opioid
receptor. Essentially all 3H-[D-Pen 2, D-Pen 5] enkephalin (3 H-DPDPE) and 3H-[D-Ala 2, D …

Syntheses, opioid binding affinities, and potencies of dynorphin A analogues substituted in positions 1, 6, 7, 8 and 10

AM KAWASAKI, RJ KNAPP, A WALTON… - … journal of peptide …, 1993 - Wiley Online Library
Structural, stereochemical, stereoelectronic and conformational requirements for biological
activity of dynorphin A1–11‐NH2 analogues at opioid receptors were explored by …

Dopamine D3 Receptor Ligands with Antagonist Properties

AE Hackling, H Stark - ChemBioChem, 2002 - Wiley Online Library
The dopamine D3 receptor has been recognized to play an important role in the molecular
mechanisms of various neuropsychiatric disorders. The development of new dopamine D3 …

JNJ-20788560 [9-(8-azabicyclo [3.2. 1] oct-3-ylidene)-9H-xanthene-3-carboxylic acid diethylamide], a selective delta opioid receptor agonist, is a potent and …

EE Codd, JR Carson, RW Colburn, DJ Stone… - … of Pharmacology and …, 2009 - ASPET
μ-Opioid analgesics are a mainstay in the treatment of acute and chronic pain of multiple
origins, but their side effects, such as constipation, respiratory depression, and abuse …

Recent progress in development of dopamine receptor subtype-selective agents: potential therapeutics for neurological and psychiatric disorders

A Zhang, JL Neumeyer, RJ Baldessarini - Chemical reviews, 2007 - ACS Publications
Dopamine (DA) is a critical neurotransmitter in the mammalian central nervous system
(CNS). The cerebral dopaminergic system is implicated in the pathophysiology of several …

[PDF][PDF] A novel, potent and selective nonpeptidic delta opioid receptor agonist BW373U86

KJ Chang, GC Rigdon, JL Howard, RW McNUTT - J Pharmacol Exp Ther, 1993 - Citeseer
Four different oploid receptor binding assays and three different isolated tissue studies were
used to screen for delta receptor-selective nonpeptidic compounds.(ą-((a-R5)-a-((2S5, 5R5) …

Synthesis and structure-activity relationships of dynorphin A-(1-8) amide analogs

H Yoshino, T Nakazawa, Y Arakawa… - Journal of medicinal …, 1990 - ACS Publications
In order to study the structure-activity relationships of dynorphin A-(1-8) amide [Dyn (l-8)-
NH2], 20 analogues were synthesized by the solution method. Their biological activities …