Structure-Activity Studies of Dermorphin. Synthesis and Some Pharmacological Data of Dermorphin and Its 1-Substituted Analogues

Krzysztof Darlak; Zbigniew Grzonka; Piotr Janicki; Andrzej Czlonkowski; S. Witold Gumulka

doi:10.1021/jm00364a016

Structure-Activity Studies of Dermorphin. Synthesis and Some Pharmacological Data of Dermorphin and Its 1-Substituted Analogues

Krzysztof Darlak, Zbigniew Grzonka, Piotr Janicki, Andrzej Czlonkowski, S. Witold Gumulka

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25 Scopus citations

Abstract

Dermorphin and its analogues substituted at position 1 by N-acetyltyrosine, O-methyltyrosine, phenylalanine, D-phenylalanine, or alanine were obtained by solid-phase peptide synthesis. Their pharmacological effects were studied in vitro by the guinea pig ileum method and in vivo by the hot plate method, and the results were compared with those of morphine. The most pronounced activity was shown for dermorphin. A radioreceptor study showed a moderate affinity of dermorphin and its Tyr(Me) analogue for the opiate receptor sites from striatal homogenates.

Original language	English (US)
Pages (from-to)	1445-1447
Number of pages	3
Journal	Journal of Medicinal Chemistry
Volume	26
Issue number	10
DOIs	https://doi.org/10.1021/jm00364a016
State	Published - Oct 1983

All Science Journal Classification (ASJC) codes

Molecular Medicine
Drug Discovery

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abstract = "Dermorphin and its analogues substituted at position 1 by N-acetyltyrosine, O-methyltyrosine, phenylalanine, D-phenylalanine, or alanine were obtained by solid-phase peptide synthesis. Their pharmacological effects were studied in vitro by the guinea pig ileum method and in vivo by the hot plate method, and the results were compared with those of morphine. The most pronounced activity was shown for dermorphin. A radioreceptor study showed a moderate affinity of dermorphin and its Tyr(Me) analogue for the opiate receptor sites from striatal homogenates.",

author = "Krzysztof Darlak and Zbigniew Grzonka and Piotr Janicki and Andrzej Czlonkowski and Gumulka, {S. Witold}",

year = "1983",

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AU - Darlak, Krzysztof

AU - Grzonka, Zbigniew

AU - Janicki, Piotr

AU - Czlonkowski, Andrzej

AU - Gumulka, S. Witold

PY - 1983/10

Y1 - 1983/10

N2 - Dermorphin and its analogues substituted at position 1 by N-acetyltyrosine, O-methyltyrosine, phenylalanine, D-phenylalanine, or alanine were obtained by solid-phase peptide synthesis. Their pharmacological effects were studied in vitro by the guinea pig ileum method and in vivo by the hot plate method, and the results were compared with those of morphine. The most pronounced activity was shown for dermorphin. A radioreceptor study showed a moderate affinity of dermorphin and its Tyr(Me) analogue for the opiate receptor sites from striatal homogenates.

AB - Dermorphin and its analogues substituted at position 1 by N-acetyltyrosine, O-methyltyrosine, phenylalanine, D-phenylalanine, or alanine were obtained by solid-phase peptide synthesis. Their pharmacological effects were studied in vitro by the guinea pig ileum method and in vivo by the hot plate method, and the results were compared with those of morphine. The most pronounced activity was shown for dermorphin. A radioreceptor study showed a moderate affinity of dermorphin and its Tyr(Me) analogue for the opiate receptor sites from striatal homogenates.

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Structure-Activity Studies of Dermorphin. Synthesis and Some Pharmacological Data of Dermorphin and Its 1-Substituted Analogues

Abstract

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