A synthetic enkephalin analogue with prolonged parenteral and oral analgesic activity

Roemer, D.; Buescher, H.-H.; Hill, Ronald C.; Pless, J.; Bauer, W.; Cardinaux, F.; Closse, Annemarie; Hauser, Daniel; Huguenin, R

doi:10.1038/268547a0

Cited by 411 publications

(101 citation statements)

References 21 publications

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“…FK 33-824 interacting with µ and, to a lesser degree, δ receptors [43,53] mimics the action of β-endorphin in this way. The effect of the opioid agonist and naloxone was observed both when they were added alone to the cultures and in combination with FSH or PRL.…”

Section: Discussionmentioning

confidence: 99%

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The physiological role of ?-endorphin in porcine ovarian follicles

et al. 2000

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-β-Endorphin-like immunoreactivity (β-END-LI) was measured by radioimmunoassay in porcine ovarian follicular fluid (FF) from small, medium and large follicles throughout the oestrous cycle. The concentration of β-END-LI in FF from small follicles collected on days 1-5 of the cycle was at least tenfold higher than in the fluid from any other follicles independently from their size and the period of the cycle. The level of β-END-LI in small follicles on days 6-10 was drastically decreased. Subsequently, on days 11-16 its concentration was enhanced and reduced again in preovulatory period of the cycle. Concentrations of β-END-LI in FF from medium follicles were relatively equal throughout the cycle (days 6-21). No significant differences in β-END-LI levels were found between small, medium and large follicles from days 17-21. However, β-END-LI concentrations in medium follicles on days 11-13 and 14-16 were statistically lower than those in small follicles. Moreover, the effects of FSH, prolactin (PRL), progesterone (P 4 ), testosterone (T) and 17 β-oestradiol (E 2 ) on β-END-LI release by granulosa cells (GCs) from large follicles and, on the other hand, the effects of the opioid agonist FK 33-824 alone or in combination with FSH, PRL or naloxone (NAL) on follicular steroidogenesis were studied. FSH drastically increased β-END-LI output in a dose-dependent fashion. This stimulatory effect of the gonadotrophin was inhibited by the highest dose of P 4 (10 -5 M). The effect of PRL and the steroids added to the cultures on β-END-LI release was negligible. FSH-or PRL-induced P 4 secretion by GCs was essentially abolished by both FK 33-824 and NAL. However, androstenedione (A 4 ) and testosterone output by the cells was greatly potentiated by FK 33-824. In the presence of NAL, FSH or PRL, A 4 release stimulated by FK 33-824 was suppressed to the basal level. Secretion of E 2 was completely free from the influence of FK 33-824 or NAL; only oestrone (E 1 ) output was modulated by them in cultures where FSH or PRL was present. In conclusion, FSH appears to be the key regulator of β-END-LI secretion by porcine granulosa cells. Moreover, steroidogenesis in pig granulosa cells is modulated by opioid peptides acting both alone and by way of interaction with FSH or PRL.opioid peptides / β-endorphin / porcine granulosa cells / steroid secretion Reprod. Nutr. Dev. 40 (2000) 63-75 63

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Section: Discussionmentioning

confidence: 99%

“…The effects of the opioid agonist FK 33-824, which interacts with µ and δ opioid receptors [43,53], and naloxone (blocker of opioid receptors) on secretion of progesterone, androstenedione, testosterone, oestradiol-17β, and oestrone by granulosa cells from large follicles.…”

Section: Isolation and Incubation Of Granulosa Cellsmentioning

confidence: 99%

The physiological role of ?-endorphin in porcine ovarian follicles

et al. 2000

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“…The ineffectiveness of morphine on rat vas deferens reflects its relatively low effectiveness at the receptors on which FK 33-824 acts, e.g. 103 times less potent (Roemer et al, 1977). Part of the depressant effect of FK 33-824 is likely to be non-specific due to the high concentration necessary for its effect compared with that in other tissues (Roemer et al, 1977;Kosterlitz, Lord, Paterson & Waterfield, 1980).…”

Section: Discussionmentioning

confidence: 99%

The Distribution of Adrenoceptors and Other Drug Receptors Between the Two Ends of the Rat Vas Deferens as Revealed by Selective Agonists and Antagonists

Macdonald

McGrath

1980

British J Pharmacology

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1 The effects of adrenoceptor agonists and other agonists on the contractile responses of the prostatic and epididymal portions of the rat isolated vas deferens to single pulse field stimulation were investigated. 2 a-Adrenoceptor agonists produced prejunctional c2-mediated inhibition and post-junctional cxl-mediated potentiation of the nerve-induced responses. Guanabenz and xylazine produced mainly inhibitory effects, xylazine being 10 times less potent. Clonidine and oxymetazoline produced inhibition with similar potency to guanabenz but at higher concentrations excitatory effects were present, particularly in the epididymal portion. Phenylephrine produced only potentiation of the nerveinduced response in both portions. Potentiation of nerve-induced responses was a more sensitive and quantitative index of excitation than was direct contraction of the tissue. 3 Isoprenaline and salbutamol both gave fl2-mediated inhibition of the nerve-induced responses in both portions of tissue. At least part of the effect was post-junctional since phenylephrine contractions were inhibited. Isoprenaline also produced a post-junctional ocx-mediated excitation. 4 Noradrenaline produced effects qualitatively similar to those of the other ax-adrenoceptor agonists, inhibition and excitation predominating in the prostatic and epididymal ends respectively. 5 Morphine produced inhibition in the mouse but not in the rat vas deferens. In rat vas, however, enkephalin analogues produced pre-junctional inhibition of responses in both portions which could be partly reversed by naloxone; restoration of the adrenergic component was more complete. Rat anococcygeus showed no equivalent effect. 6 Adenosine 5'-triphosphate (ATP) inhibited nerve-induced responses in each portion with a greater effect on the prostatic portion.

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“…Such patterns or structures are typically formed and maintained by non-covalent bonds [64]. Although non-covalent bonds such as hydrogen bonds, ionic bonds, and hydrophobic interactions are rather weak in isolation, when in concert they govern the self-assembly of biological macromolecules.…”

Section: Self-assemblymentioning

confidence: 99%

Biomimetic materials for tissue engineering

Peter

2008

Advanced Drug Delivery Reviews

1,213

819

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Tissue engineering and regenerative medicine is an exciting research area that aims at regenerative alternatives to harvested tissues for transplantation. Biomaterials play a pivotal role as scaffolds to provide three-dimensional templates and synthetic extracellular-matrix environments for tissue regeneration. It is often beneficial for the scaffolds to mimic certain advantageous characteristics of the natural extracellular matrix, or developmental or would healing programs. This article reviews current biomimetic materials approaches in tissue engineering. These include synthesis to achieve certain compositions or properties similar to those of the extracellular matrix, novel processing technologies to achieve structural features mimicking the extracellular matrix on various levels, approaches to emulate cell-extracellular matrix interactions, and biologic delivery strategies to recapitulate a signaling cascade or developmental/would-healing program. The article also provides examples of enhanced cellular/tissue functions and regenerative outcomes, demonstrating the excitement and significance of the biomimetic materials for tissue engineering and regeneration.

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A synthetic enkephalin analogue with prolonged parenteral and oral analgesic activity

Cited by 411 publications

References 21 publications

The physiological role of ?-endorphin in porcine ovarian follicles

The physiological role of ?-endorphin in porcine ovarian follicles

The Distribution of Adrenoceptors and Other Drug Receptors Between the Two Ends of the Rat Vas Deferens as Revealed by Selective Agonists and Antagonists

Biomimetic materials for tissue engineering

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