Synthesis and evaluation of derivatives of leucine enkephalin as potential affinity labels for δ opioid receptors

A number of N-nitroso-2-chloroethyl-carbamoyl (Q(NO)) derivatives of α-melanotropin fragments have been synthesized and their effect on the frog skin melanocytes studied. Peptides substituted in this way possess the biological activity of the parent compounds, indicating that they preserved their receptor recognizing ability. These compounds can therefore serve as affinity labels. Some of these derivatives, related to the C-terminal sequence of α-melanotropin show prolonged darkening reaction, which does not influence the subsequent reaction of melanocytes with α-melanotropin. The Q(NO)-derivative of a fragment derived from the classical active site of the hormone shows, however, inhibition of the effect of α-melanotropin. It can be concluded that the latter peptide acts through the melanotropin receptor, while others, related to the C-terminal sequence of the hormone through another mechanism.

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Dermorphin-based potential affinity labels for µ-opioid receptors*

Journal of Peptide Research ◽

10.1034/j.1399-3011.2003.20030.x ◽

2002 ◽

Vol 61 (1) ◽

pp. 40-45 ◽

Cited By ~ 3

Author(s):

H. Choi ◽

T. F. Murray ◽

J. V. Aldrich

Keyword(s):

Opioid Receptors ◽

Affinity Labels

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Affinity Labels for Opioid Receptors

The Annual Review of Pharmacology and Toxicology ◽

10.1146/annurev.pa.25.040185.001205 ◽

1985 ◽

Vol 25 (1) ◽

pp. 193-223 ◽

Cited By ~ 78

Author(s):

A E Takemori ◽

P S Portoghese

Keyword(s):

Opioid Receptors ◽

Affinity Labels

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Potential Irreversible Ligands for Opioid Receptors. Cinnamoyl Derivatives of β-Naltrexamine

Journal of Pharmacy and Pharmacology ◽

10.1111/j.2042-7158.1996.tb07121.x ◽

1996 ◽

Vol 48 (2) ◽

pp. 192-196 ◽

Cited By ~ 6

Author(s):

IAN DERRICK ◽

JOHN W. LEWIS ◽

HUMPHREY A. MOYNIHAN ◽

JILLIAN BROADBEAR ◽

JAMES H. WOODS

Keyword(s):

Opioid Receptors ◽

Derivatives Of

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New psychoactive substances: psychiatrist's view

Interactive science ◽

10.21661/r-497066 ◽

2019 ◽

pp. 57-67

Author(s):

Andrey Viktorovich Antsyborov ◽

Irina Vladimirovna Dubatova

Keyword(s):

Opioid Receptors ◽

Psychotic Disorders ◽

Synthetic Cannabinoids ◽

Designer Drugs ◽

New Psychoactive Substances ◽

Psychoactive Substances ◽

Gaba A ◽

Psychoactive Effects ◽

Legal High ◽

Derivatives Of

Appearing not long ago, new psychoactive substances (designer drugs), including synthetic cannabinoids, derivatives of cathinone, phenethylamines, new stimulants, synthetic opioids, tryptamine derivatives, phencyclidine, piperazine, the GABA (A/B) receptors agonists, have become a serious problem for consumers and for physicians. Consumers of these substances are attracted primarily by the intensity of psychoactive effects, and the «legal high» declared by the black manufacturers, which indicates that significant difficulties in a laboratory identification of new surfactants. Designer drugs, when ingested, can be influenced on many neurotransmitter pathways/receptors: dopamine, cannabinoid (CB1), GABA (A/B), 5-HT2A, glutamate, and k-opioid receptors (KOR), the imbalance of which leads to the development of polymorphic psychotic disorders.

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