GALANIN, GALANTIDE AND GALANIN(1-14)-[α-AMINOBUTYRIC ACID8]-SCYLIORHININ-I: STRUCTURE DEPENDENT EFFECTS ON THE RAT ISOLATED GASTRIC FUNDUS

Korolkiewicz, Roman; Sliwiński, W; Rekowski, Piotr; Halama-Borowiec, A; Mucha, Piotr; Szczurowicz, A; Korolkiewicz, K.Z.

doi:10.1006/phrs.1996.0099

Cited by 14 publications

(7 citation statements)

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“…The experiments of isolated rat fundus stomach were performed according to the method described by Korolkiewicz et al 10 . Animals were killed by cervical dislocation.…”

Section: Methodsmentioning

confidence: 99%

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Mechanism of antiulcerogenic activity of semi-synthetic crotonin obtained from Croton cajucara Benth.

Almeida

Miotto

Nunes

et al. 2002

Rev. bras. farmacogn.

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2002Relegar a abordagem complexa em detrimento da abordagem reducionista prevalecente e tratar assimetricamente o conhecimento popular e científico envolve um grande risco. No que se refere ao conhecimento sobre o potencial terapêutico das plantas medicinais e de seus constituintes, isto poderia implicar na limitação da capacidade de compreensão da multidimensionalidade dos fenômenos e das estruturas biológicas, além de ocasionar a perda de uma grande quantidade de informações geradas a partir da relação ao longo dos tempos entre o homem e a natureza, podendo até mesmo contribuir para a extinção de culturas que não estão inseridas na sociedade industrial contemporânea. Referências

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“…The experiments of isolated rat fundus stomach were performed according to the method described by Korolkiewicz et al 10 . Animals were killed by cervical dislocation.…”

Section: Methodsmentioning

confidence: 99%

“…This plant is popularly is known as "chá da terra", "chá da américa", "chá das antilhas" and "chá da calçada" a plant used extensively in Northeast Brazil as antibiotic in the treatment of infections for fungi, dhermatofilus, yeasts and bacterias 6,10 .…”

Section: Introductionmentioning

confidence: 99%

Mechanism of antiulcerogenic activity of semi-synthetic crotonin obtained from Croton cajucara Benth.

Almeida

Miotto

Nunes

et al. 2002

Rev. bras. farmacogn.

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“…M15 blocks the neuronal action of galanin in the central nervous system [6]. In gastrointestinal smooth muscles galantide acts as a full agonist of galanin [7,8].…”

Section: Introductionmentioning

confidence: 99%

“…All the peptides were built up of the N-terminal galanin (GAL) fragment or its analogues, linked to the Cterminal portion of SP analogues or scyliorhinin I (SCY-I) analogues. M15 and all the six chimeric peptides were tested earlier as galanin agonists in contractile effect on rat isolated gastric fundus [8]. The chimeric peptides are bireceptor compounds, which can link to both galanin and tachykinin receptors.…”

Section: Introductionmentioning

confidence: 99%

New chimeric analogues of galanin: Synthesis and effects on the glucose-induced insulin secretion

et al. 1998

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SummaryThe solid-phase synthesis and in vitro assays on the glucose-induced insulin secretion from rat pancreatic islets of Langerhans with six new chimeric peptides were performed. All the peptides were built up of the N-terminal galanin (GAL) fragment or its analogues, linked to the C-terminal portion of substance P (SP) analogues or scyliorhinin I (SCY-I) analogues. Two strong antagonists of the inhibitory effect of galanin on the glucose-induced insulin release were found: [cycloleucine4]GAL(1-13)-SP(5-11)-amide and GAL(1-13)-[L-norleucinel~ 10)-amide.

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“…However, due to the lack of specific antagonists, it is not clear which ef fects of Gal on gastrointestinal motility are physiological and which are pharmacological. In search of a specific inhibitor, we studied the activity of several pGal(l-29)-NH2 short analogues and hybridic peptides on rat iso lated gastric fundus [7], One of these peptides, [Lys14]pGal(I-15)-NH;>, has attracted our at tention, as it seems to possess the features of a partial agonist at Gal receptors.…”

Section: Introductionmentioning

confidence: 99%

Lysine <sup>14</sup>Galanin(1–15)-IMH<sub>2</sub>: A Partial Agonist at Galanin Receptors in Rat Isolated Gastric Fundus

Korolkiewicz

Sliwiński²,

Rekowski³

et al. 1997

Pharmacology

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The study was undertaken to characterize the effects of the porcine galanin [pGal(1–29)-NH2] analogue [Lys¹⁴]pGal(1–15)-NH₂ on rat gastric fundus. [Lys¹⁴]pGal(1–15)-NH₂ is a less potent contractile agent than pGal(1–29)-NH₂ (EC₅₀ 74.1 vs. 43.7 nmol/l, respectively) and shows a significantly lower maximal response than pGal(1–29)-NH2. Concentration-contraction curves were constructed for pGal(1–29)-NH₂ alone (control) and pGal(1–29)-NH₂ in the presence of 10, 100, and 1,000 nmol/l of [Lys¹⁴]pGal(1–15)-NH₂. [Lys¹⁴]pGal(1–15)-NH₂ shifted the concentration-contraction curves of pGal(1–29)-NH₂ significantly to the right, whereas their linear portions remained parallel to that for the pGal(1–29)-NH₂ control. [Lys¹⁴]pGal(1–15)-NH₂ markedly increased the EC₅₀ of the respective pGal(1–29)-NH₂ concentration-contraction curves. It did not substantially change the maximal response of the muscles to pGal(1–29)-NH₂ and the form of the respective concentration-contraction curves. Schild’s plot gave a straight line with a slope of 0.84. The pA₂ value for [Lys¹⁴]pGal(1–15)-NH₂ was 8.23. [Lys¹⁴]pGal(1–15)-NH₂seems to be a partial Gal receptor agonist. Since the lack of specific Gal receptor antagonists in the gastrointestinal tract makes a precise characterization of its role as a motility modulator difficult, the position 14 in the pGal(1–29)-NH₂ molecule looks as an attractive target in the search of a pure Gal receptor antagonist in the smooth muscles of the gut.

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GALANIN, GALANTIDE AND GALANIN(1-14)-[α-AMINOBUTYRIC ACID8]-SCYLIORHININ-I: STRUCTURE DEPENDENT EFFECTS ON THE RAT ISOLATED GASTRIC FUNDUS

Cited by 14 publications

References 0 publications

Mechanism of antiulcerogenic activity of semi-synthetic crotonin obtained from Croton cajucara Benth.

Mechanism of antiulcerogenic activity of semi-synthetic crotonin obtained from Croton cajucara Benth.

New chimeric analogues of galanin: Synthesis and effects on the glucose-induced insulin secretion

Lysine <sup>14</sup>Galanin(1–15)-IMH<sub>2</sub>: A Partial Agonist at Galanin Receptors in Rat Isolated Gastric Fundus

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GALANIN, GALANTIDE AND GALANIN(1-14)-[α-AMINOBUTYRIC ACID8]-SCYLIORHININ-I: STRUCTURE DEPENDENT EFFECTS ON THE RAT ISOLATED GASTRIC FUNDUS

Cited by 14 publications

References 0 publications

Mechanism of antiulcerogenic activity of semi-synthetic crotonin obtained from Croton cajucara Benth.

Mechanism of antiulcerogenic activity of semi-synthetic crotonin obtained from Croton cajucara Benth.

New chimeric analogues of galanin: Synthesis and effects on the glucose-induced insulin secretion

Lysine <sup>14</sup>Galanin(1&ndash;15)-IMH<sub>2</sub>: A Partial Agonist at Galanin Receptors in Rat Isolated Gastric Fundus

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About

Lysine <sup>14</sup>Galanin(1–15)-IMH<sub>2</sub>: A Partial Agonist at Galanin Receptors in Rat Isolated Gastric Fundus