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  • 1
    Electronic Resource
    Electronic Resource
    5-HT4 receptor mediated stimulation of gastric emptying in rats (1995)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 351 (1995), S. 589-595 
    Details
    ISSN: 1432-1912
    Keywords: 5-HT4 receptors ; Gastric emptying ; Benzamides ; SC 49518 ; SC 53116 ; RS 23597-190 ; SB 204070
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract It is well documented that certain substituted benzamides, such as cisapride, and benzimidazolones, such as BIMU 8, enhance gastric emptying in rats. As these compounds possess 5-HT3 antagonistic and 5-HT4 agonistic properties, the precise mechanisms (5-HT3 or 5-HT4) underlying their gastroprokinesic effects is still unclear. In the present study, we used SC 49518 (a benzamide and selective 5-HT4 receptor agonist) and two selective 5-HT4 receptor antagonists (RS 23597-190 and SB 204070) to elucidate the role of 5-HT4 receptors in gastroprokinesis. SC 49518 (1–316 μg/kg; ip) produced significant and dose-dependent stimulation of gastric emptying in rats (ED50 = 2.3 μg/kg; ip). SC 49518 also produced dose-dependent inhibition of bradycardia induced by 2-methyl 5-HT (von Bezold-Jarisch reflex) but with a 156 fold lower potency (ID50 = 0.36 mg/kg; ip). The gastroprokinetic effects of SC 49518 (3–316 μg/kg; ip) were significantly antagonized by the selective 5-HT4 receptor antagonist RS 23597-190 (0.1 mg/kg/min; iv). SB 204070 (0.003-1 mg/kg; ip), another selective 5-HT4 receptor antagonist, produced dose-dependent inhibition of the gastroprokinesic effects of SC 49518 (10 μg/kg; ip), the inhibition attaining statistical significance at the dose of 0.1 mg/kg; ip. RS 23597-190 had no effects on gastric emptying per se whereas SB 204070 significantly increased gastric emptying by itself at 1 mg/kg; ip but not at 0.1 mg/kg; ip. These findings show, for the first time, that SC 49518, a selective 5-HT4 receptor agonist, produces potent stimulation of gastric emptying in rats via a mechanism involving activation of 5-HT4 receptors. It is suggested that a similar mechanism may account for the gastroprokinetic effects of other non-selective benzamides and benzimidazolones.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00170157
    Library Location Call Number Volume/Issue/Year Availability
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    Paper (German National Licenses)
    Fulltext
  • 2
    Electronic Resource
    Electronic Resource
    5-HT4 receptor mediated stimulation of gastric emptying in rats (1995)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 351 (1995), S. 589-595 
    Details
    ISSN: 1432-1912
    Keywords: Key words 5-HT4 receptors ; Gastric emptying ; Benzamides ; SC 49518 ; SC 53116 ; RS 23597-190 ; SB 204070
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract  It is well documented that certain substituted benzamides, such as cisapride, and benzimidazolones, such as BIMU 8, enhance gastric emptying in rats. As these compounds possess 5-HT3 antagonistic and 5-HT4 agonistic properties, the precise mechanisms (5-HT3 or 5-HT4) underlying their gastroprokinetic effects is still unclear. In the present study, we used SC 49518 (a benzamide and selective 5-HT4 receptor agonist) and two selective 5-HT4 receptor antagonists (RS 23597-190 and SB 204070) to elucidate the role of 5-HT4 receptors in gastroprokinesis. SC 49518 (1–316 μg/kg; ip) produced significant and dose-dependent stimulation of gastric emptying in rats (ED50=2.3 μg/kg; ip). SC 49518 also produced dose-dependent inhibition of bradycardia induced by 2-methyl 5-HT (von Bezold-Jarisch reflex) but with a 156 fold lower potency (ID50=0.36 mg/kg; ip). The gastroprokinetic effects of SC 49518 (3–316 μg/kg; ip) were significantly antagonized by the selective 5-HT4 receptor antagonist RS 23597-190 (0.1 mg/kg/min; iv). SB 204070 (0.003–1 mg/kg; ip), another selective 5-HT4 receptor antagonist, produced dose-dependent inhibition of the gastroprokinetic effects of SC 49518 (10 μg/kg; ip), the inhibition attaining statistical significance at the dose of 0.1 mg/kg; ip. RS 23597-190 had no effects on gastric emptying per se whereas SB 204070 significantly increased gastric emptying by itself at 1 mg/kg; ip but not at 0.1 mg/kg; ip. These findings show, for the first time, that SC 49518, a selective 5-HT4 receptor agonist, produces potent stimulation of gastric emptying in rats via a mechanism involving activation of 5-HT4 receptors. It is suggested that a similar mechanism may account for the gastro-prokinetic effects of other non-selective benzamides and benzimidazolones.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00170157
    Library Location Call Number Volume/Issue/Year Availability
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    Paper (German National Licenses)
    Fulltext
  • 3
    Electronic Resource
    Electronic Resource
    Synthesis of hydroxyl-containing polyimides derived from 4,6-diamino-resorcinol dihydrochloride and aromatic tetracarboxylic dianhydrides (1994)
    Bognor Regis [u.a.] : Wiley-Blackwell
    Journal of Polymer Science Part A: Polymer Chemistry 32 (1994), S. 1903-1908 
    Details
    ISSN: 0887-624X
    Keywords: polyimides ; pendant hydroxyl ; hydrophilic ; amine hydrochloride ; Chemistry ; Polymer and Materials Science
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: High Tg polyimides containing pendant phenolic hydroxyl groups were synthesized in high molecular weight via one-step solution polymerization of the dihydrochloride salt of 4,6-diaminoresorcinol with various commercially available dianhydrides. Polymerization proceeds via initial dissociation of diaminoresorcinol dihydrochloride to hydrogen chloride gas and diaminoresorcinol, followed by rapid dissolution of diaminoresorcinol and polymerization with the dianhydride monomer to afford soluble, fully-cyclized polyimide. The resulting poly(hydroxy-imide)s, which contain two phenolic hydroxyl groups per repeat unit, were soluble in amide solvents and dilute aqueous bases, displayed reasonably high glass transition temperatures and a high degree of water uptake. © 1994 John Wiley & Sons, Inc.
    Additional Material: 4 Ill.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/pola.1994.080321012
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    Paper (German National Licenses)
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  • 4
    Electronic Resource
    Electronic Resource
    Synthesis of soluble, thermosetting polymides derived from 1,4-phenylenebis(phenylmaleic anhydride) and aromatic diamines (1994)
    Bognor Regis [u.a.] : Wiley-Blackwell
    Journal of Polymer Science Part A: Polymer Chemistry 32 (1994), S. 2377-2385 
    Details
    ISSN: 0887-624X
    Keywords: thermosetting imides ; 1,4-phenylenebis(phenylmaleic anhydride) ; Chemistry ; Polymer and Materials Science
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: The dianhydride monomer 1,4-phenylenebis(phenylmaleic anhydride) was polymerized with various aromatic diamines in a one-step solution polymerization to afford high molecular weight, soluble polyimides containing backbone phenylmaleimide structures. The polymides were soluble in amide solvents, chlorinated hydrocarbons, and tetrahydrofuran at 25°C at a concentration of 15% (w/v), displayed molecular weight distributions (Mw/Mn) of 2.0-2.2 as determined by absolute GPC and showed Tg values of 240°C and above as measured by differential scanning calorimetry. In addition, polyimide thermosets were prepared from these materials by thermal cure at 350-360°C. The crosslinked polyimides displayed Tgs 20-25°C higher than their soluble precursors, and chloroform extraction indicated gel fractions ranging from 74-100% after cure. © 1994 John Wiley & Sons, Inc.
    Additional Material: 9 Ill.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/pola.1994.080321218
    Library Location Call Number Volume/Issue/Year Availability
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    Paper (German National Licenses)
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