Endomorphins: potential roles and therapeutic indications in the development of opioid peptide analgesic drugs

WX Liu, R Wang - Medicinal research reviews, 2012 - Wiley Online Library
The application of endomorphins as clinical available analgesic drugs has been impeded by
their relatively poor receptor selectivity compared with alkaloid analgesics, rapid …

Pain inhibition by endomorphins

R Przewłocki, D Łabuz, J Mika… - Annals of the new …, 1999 - Wiley Online Library
Spinal analgesic effects of endomorphin‐1 and endomorphin‐2 were studied during acute,
inflammatory, and neuropathic pain in rats chronically implanted with intrathecal cannulas …

In vitro quantitative study of the degradation of endomorphins

C Tömböly, A Péter, G Tóth - Peptides, 2002 - Elsevier
The catabolism of the endomorphins was investigated in detail. The endomorphins were
degraded relatively slowly in the rat brain homogenate (t1/2 (endomorphin-1)= 4.94 min; t1/2 …

Dissociation of analgesic and rewarding effects of endomorphin-1 in rats

AM Wilson, RD Soignier, JE Zadina, AJ Kastin… - Peptides, 2000 - Elsevier
The μ-receptor is the primary mediator of the effects of morphine and the endogenous
opiates, endomorphin-1 and endomorphin-2. Here we demonstrate a dissociation of the …

Enzymatic degradation of endomorphins

A Janecka, R Staniszewska, K Gach, J Fichna - Peptides, 2008 - Elsevier
Centrally acting plant opiates, such as morphine, are the most frequently used analgesics for
the relief of severe pain, even though their undesired side effects are serious limitation to …

Peripheral antinociceptive effects of exogenous and immune cell-derived endomorphins in prolonged inflammatory pain

D Labuz, S Berger, SA Mousa, C Zöllner… - Journal of …, 2006 - Soc Neuroscience
Endomorphins (EMs) are endogenous selective μ-opioid receptor agonists. Their role in
inflammatory pain has not been fully elucidated. Here we examine peripheral …

Synthesis and binding activity of endomorphin-1 analogues containing β-amino acids

G Cardillo, L Gentilucci, P Melchiorre… - Bioorganic & medicinal …, 2000 - Elsevier
Endomorphin-1 (Tyr-Pro-Trp-PheNH2) has been proposed as the most potent endogenous
ligand of the μ-opioid receptors. In this paper, we describe the synthesis of some …

From MIF-1 to endomorphin: the Tyr-MIF-1 family of peptides

W Pan, AJ Kastin - Peptides, 2007 - Elsevier
The Tyr-MIF-1 family of small peptides has served a prototypic role in the introduction of
several novel concepts into the peptide field of research. MIF-1 (Pro-Leu-Gly-NH2) was the …

Development of opioid peptide analogs for pain relief

A Janecka, R Perlikowska, K Gach… - Current …, 2010 - ingentaconnect.com
Opioid receptors and opioid peptides constitute the endogenous opioid system. The most
relevant function of the opioid system seems to be the inhibitory modulation of nociceptive …

μ‐opioid receptor modulation of calcium channel current in periaqueductal grey neurons from C57B16/J mice and mutant mice lacking MOR‐1

M Connor, A Schuller, JE Pintar… - British journal of …, 1999 - Wiley Online Library
The actions of opioid receptor agonists on the calcium channel currents (IBa) of acutely
dissociated periaqueductal grey (PAG) neurons from C57B16/J mice and mutant mice …