Endomorphin-1 and endomorphin-2: pharmacology of the selective endogenous μ-opioid receptor agonists

G Horvath - Pharmacology & therapeutics, 2000 - Elsevier
The recently discovered endogenous opioid peptides, endomorphins-1 and-2, appear to
have properties consistent with neurotransmitter/neuromodulator actions in mammals. This …

Cannabidiol Acts at 5-HT1A Receptors in the Human Brain: Relevance for Treating Temporal Lobe Epilepsy

C Martínez-Aguirre, F Carmona-Cruz… - Frontiers in behavioral …, 2020 - frontiersin.org
Experimental evidence indicates that cannabidiol (CBD) induces anxiolytic and antiepileptic
effects through the activation of 5-HT1A receptors. These receptors are coupled to Gi/o …

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 …

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 …

Enzymatic degradation studies of endomorphin-2 and its analogs containing N-methylated amino acids

A Janecka, R Kruszynski, J Fichna, P Kosson… - Peptides, 2006 - Elsevier
In this paper, we describe the synthesis of novel endomorphin-2 analogs, containing N-
methylated amino acids, consecutively in each position. The receptor-binding profile of the …

New endomorphin analogues containing alicyclic β-amino acids: Influence on bioactive conformation and pharmacological profile

A Keresztes, M Szucs, A Borics… - Journal of Medicinal …, 2008 - ACS Publications
Endomorphins were subjected to a number of structural modifications in a search for their
bioactive conformations. The alicyclic β-amino acids cis-(1 S, 2 R) ACPC/ACHC, cis-(1 R, 2 …

Recent advances in endomorphin engineering

A Keresztes, A Borics, G Tóth - ChemMedChem, 2010 - Wiley Online Library
Recent statistics from the World Health Organization indicate that a high percentage of
people worldwide suffer from a wide variety of acute or cancer‐associated chronic pain. At …

Liquid chromatographic study of the enzymatic degradation of endomorphins, with identification by electrospray ionization mass spectrometry

A Péter, G Tóth, C Tömböly, G Laus… - Journal of Chromatography …, 1999 - Elsevier
The recently discovered native endomorphins play an important role in opioid analgesia, but
their metabolic fate in the organism remains relatively little known. This paper describes the …

Structure− activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues

C Tömböly, KE Kövér, A Péter, D Tourwé… - Journal of medicinal …, 2004 - ACS Publications
Endomorphins-1 and-2 were substituted with all the β-MePhe stereoisomers in their Phe
residues to generate a conformationally constrained peptide set. This series of molecules …

Specific activation of the μ opioid receptor (MOR) by endomorphin 1 and endomorphin 2

K Monory, MC Bourin, M Spetea… - European Journal of …, 2000 - Wiley Online Library
The recently discovered endomorphin 1 (Tyr‐Pro‐Trp‐Phe‐NH2) and endomorphin 2 (Tyr‐
Pro‐Phe‐Phe‐NH2) were investigated with respect to their direct receptor‐binding …