Imidazoline Derivative

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Pierre Renard - One of the best experts on this subject based on the ideXlab platform.

  • effect of the new Imidazoline Derivative s 22068 pms 847 on insulin secretion in vitro and glucose turnover in vivo in rats
    European Journal of Pharmacology, 1999
    Co-Authors: Agnes Peletounian, Susan L F Chan, F Rondu, Gaelle Le Bihan, Mariehelene Giroix, A Lamouri, Estera Touboul, Bruno Pfeiffer, Dominique Manechez, Pierre Renard
    Abstract:

    We have investigated the possible mechanisms underlying the antihyperglycaemic effect of the Imidazoline Derivative S-22068. In vitro, in the presence of 5 mmol/l glucose, S-22068 (100 micromol/l) induced a significant and sustained increase in insulin secretion from isolated, perifused, rat islets and a marked sensitization to a subsequent glucose challenge (10 mmol/l). S-22068 (100 micromol/l was able to antagonize the stimulatory effect of diazoxide on 86Rb efflux from preloaded islets incubated in the presence of 20 mmol/l glucose. Experiments were also performed to investigate whether S-22068 can alter glucose turnover and peripheral insulin sensitivity in vivo in mildly diabetic rats and obese, insulin resistant, Zucker rats. Neither glucose production nor individual tissue glucose utilization was modified by S-22068 in either group of rats. Similar results were obtained whether the studies were performed under basal conditions or during euglycaemic/hyperinsulinemic clamps. The results suggest that S-22068 exerts part of its antihyperglycaemic effect by promoting insulin secretion without alteration of peripheral insulin sensitivity.

  • potent antihyperglycaemic property of a new Imidazoline Derivative s 22068 pms 847 in a rat model of niddm
    British Journal of Pharmacology, 1998
    Co-Authors: Agnes Peletounian, F Rondu, A Lamouri, Estera Touboul, Bruno Pfeiffer, Dominique Manechez, Xuan Wang, R Dokhan, S Marc, Pierre Renard
    Abstract:

    Recent data suggest that some Imidazoline Derivatives can lower plasma glucose in experimental animal models of diabetes. We studied the activity of an Imidazoline S-22068, in rat model of non-insulin-dependent diabetes mellitus (NIDDM) produced with a low dose of streptozotocin (35 mg kg(-1), i.v.) in the adult. The respective increase over basal value in glucose (deltaG) and insulin (deltaI), and the rate of glucose disappearance (K), were measured during a 30 min intravenous glucose tolerance test. After an intraperitoneal injection of S-22068 (24 mg kg(-1)), deltaG (mM min(-1)) was decreased (91.67+/-5.83 vs 120.5+/-3.65; P<0.001), whereas K was increased (1.74+/-0.09 vs 1.18+/-0.05; P<0.001). Although insulinaemia was increased at time-point 0 of the test, deltaI was unchanged. During oral glucose tolerance tests (OGTT), S-22068 (24 mg kg(-1), p.o.) improved glucose tolerance, and its efficiency was potentiated after chronic treatment (15 days). Basal glycaemia was unaffected by the treatment. Under the same conditions, a higher dose of S-22068 (40 mg kg(-1)) further improved glucose tolerance without causing hypoglycaemia. Binding experiments revealed that S-22068 displays no affinity for either adrenoceptors or the two Imidazoline receptors I1 or I2. These results demonstrate that S-22068 improves glucose tolerance without causing hypoglycaemia. Thus S-22068 represents a new potential option in the treatment of NIDDM.

  • effect of s 21663 pms 812 an Imidazoline Derivative on glucose tolerance and insulin secretion in a rat model of type ii diabetes
    Journal of Pharmacology and Experimental Therapeutics, 1996
    Co-Authors: Xuan Wang, F Rondu, A Lamouri, Estera Touboul, Bruno Pfeiffer, Dominique Manechez, Pierre Renard, R Dokhan, S Marc, Beatrice Guardiolalemaitre
    Abstract:

    We have studied the activity of S-21663 (PMS 812), a new Imidazoline Derivative, in a rat model of Type II diabetes obtained by i.v. injection of a low dose (35 mg/kg) of streptozotocin, using glucose tolerance tests. Glucose tolerance and insulin secretion were measured as the delta G and the delta l, i.e., the respective increase in glycemia and insulinemia over 30 min after the glucose load. The rate of glucose disappearance was calculated as the K coefficient and the insulin response to glucose as the delta l/delta G. After i.p. injection of S-21663, delta G (millimoles per liter per minute) was decreased (71.7 +/- 10.1 vs. 112.6 +/- 15.1; P < .05), whereas K was increased (3.3 +/- 0.3 vs. 1.5 +/- 0.1; P < .05). Insulin secretion was also largely improved (delta l/delta G: 90.9 +/- 22.2 vs. 18.3 +/- 2.6; P < .05). Oral administration of the product was almost as efficient as i.p. injection. Chronic treatment (15 days) increased the efficiency. Insulin secretion measured in vitro at both 2.8 and 16.6 mM glucose was quadrupled by S-21663 (100 microM). S-21663 binds neither to alpha-2 adrenoceptors nor to known Imidazoline binding sites. S-21663 can be considered as a potential hypoglycemic agent in Type II diabetes.

Estera Touboul - One of the best experts on this subject based on the ideXlab platform.

  • effect of the new Imidazoline Derivative s 22068 pms 847 on insulin secretion in vitro and glucose turnover in vivo in rats
    European Journal of Pharmacology, 1999
    Co-Authors: Agnes Peletounian, Susan L F Chan, F Rondu, Gaelle Le Bihan, Mariehelene Giroix, A Lamouri, Estera Touboul, Bruno Pfeiffer, Dominique Manechez, Pierre Renard
    Abstract:

    We have investigated the possible mechanisms underlying the antihyperglycaemic effect of the Imidazoline Derivative S-22068. In vitro, in the presence of 5 mmol/l glucose, S-22068 (100 micromol/l) induced a significant and sustained increase in insulin secretion from isolated, perifused, rat islets and a marked sensitization to a subsequent glucose challenge (10 mmol/l). S-22068 (100 micromol/l was able to antagonize the stimulatory effect of diazoxide on 86Rb efflux from preloaded islets incubated in the presence of 20 mmol/l glucose. Experiments were also performed to investigate whether S-22068 can alter glucose turnover and peripheral insulin sensitivity in vivo in mildly diabetic rats and obese, insulin resistant, Zucker rats. Neither glucose production nor individual tissue glucose utilization was modified by S-22068 in either group of rats. Similar results were obtained whether the studies were performed under basal conditions or during euglycaemic/hyperinsulinemic clamps. The results suggest that S-22068 exerts part of its antihyperglycaemic effect by promoting insulin secretion without alteration of peripheral insulin sensitivity.

  • potent antihyperglycaemic property of a new Imidazoline Derivative s 22068 pms 847 in a rat model of niddm
    British Journal of Pharmacology, 1998
    Co-Authors: Agnes Peletounian, F Rondu, A Lamouri, Estera Touboul, Bruno Pfeiffer, Dominique Manechez, Xuan Wang, R Dokhan, S Marc, Pierre Renard
    Abstract:

    Recent data suggest that some Imidazoline Derivatives can lower plasma glucose in experimental animal models of diabetes. We studied the activity of an Imidazoline S-22068, in rat model of non-insulin-dependent diabetes mellitus (NIDDM) produced with a low dose of streptozotocin (35 mg kg(-1), i.v.) in the adult. The respective increase over basal value in glucose (deltaG) and insulin (deltaI), and the rate of glucose disappearance (K), were measured during a 30 min intravenous glucose tolerance test. After an intraperitoneal injection of S-22068 (24 mg kg(-1)), deltaG (mM min(-1)) was decreased (91.67+/-5.83 vs 120.5+/-3.65; P<0.001), whereas K was increased (1.74+/-0.09 vs 1.18+/-0.05; P<0.001). Although insulinaemia was increased at time-point 0 of the test, deltaI was unchanged. During oral glucose tolerance tests (OGTT), S-22068 (24 mg kg(-1), p.o.) improved glucose tolerance, and its efficiency was potentiated after chronic treatment (15 days). Basal glycaemia was unaffected by the treatment. Under the same conditions, a higher dose of S-22068 (40 mg kg(-1)) further improved glucose tolerance without causing hypoglycaemia. Binding experiments revealed that S-22068 displays no affinity for either adrenoceptors or the two Imidazoline receptors I1 or I2. These results demonstrate that S-22068 improves glucose tolerance without causing hypoglycaemia. Thus S-22068 represents a new potential option in the treatment of NIDDM.

  • effect of s 21663 pms 812 an Imidazoline Derivative on glucose tolerance and insulin secretion in a rat model of type ii diabetes
    Journal of Pharmacology and Experimental Therapeutics, 1996
    Co-Authors: Xuan Wang, F Rondu, A Lamouri, Estera Touboul, Bruno Pfeiffer, Dominique Manechez, Pierre Renard, R Dokhan, S Marc, Beatrice Guardiolalemaitre
    Abstract:

    We have studied the activity of S-21663 (PMS 812), a new Imidazoline Derivative, in a rat model of Type II diabetes obtained by i.v. injection of a low dose (35 mg/kg) of streptozotocin, using glucose tolerance tests. Glucose tolerance and insulin secretion were measured as the delta G and the delta l, i.e., the respective increase in glycemia and insulinemia over 30 min after the glucose load. The rate of glucose disappearance was calculated as the K coefficient and the insulin response to glucose as the delta l/delta G. After i.p. injection of S-21663, delta G (millimoles per liter per minute) was decreased (71.7 +/- 10.1 vs. 112.6 +/- 15.1; P < .05), whereas K was increased (3.3 +/- 0.3 vs. 1.5 +/- 0.1; P < .05). Insulin secretion was also largely improved (delta l/delta G: 90.9 +/- 22.2 vs. 18.3 +/- 2.6; P < .05). Oral administration of the product was almost as efficient as i.p. injection. Chronic treatment (15 days) increased the efficiency. Insulin secretion measured in vitro at both 2.8 and 16.6 mM glucose was quadrupled by S-21663 (100 microM). S-21663 binds neither to alpha-2 adrenoceptors nor to known Imidazoline binding sites. S-21663 can be considered as a potential hypoglycemic agent in Type II diabetes.

  • Glucose Tolerance and Insulin Secretion in a Rat Model of Type II Diabetes
    1996
    Co-Authors: Xuan Wang, Estera Touboul, R Dokhan, S Marc, Frederic Rondu, Azzdine Lamouri, Bruno Pfeiffer Dominique Manechez
    Abstract:

    We have studied the activity of S-21 663 (PMS 81 2), a new Imidazoline Derivative, in a rat model of Type II diabetes ob-tamed by i.v. injection of a low dose (35 mg/kg) of streptozo-tocin, using glucose tolerance tests. Glucose tolerance and insulin secretion were measured as the G and the iI, i.e., the respective increase in glycemia and insulinemia over 30 mm after the glucose load. The rate of glucose disappearance was calculated as the K coefficient and the insulin response to glucose as the il/iG. After i.p. injection of S-21663, zG (mil-limoles per liter per minute) was decreased (71.7 ± 1 0.1 vs. 1 1 2.6 ± 1 5.1; P <.05), whereas K was increased (3.3 ± 0.3 vs. 1.5 ± 0.1; P <.05). Insulin secretion was also largely improved (l/iG: 90.9 ± 22.2 vs. 18.3 ± 2.6; P <.05). Oral administration of the product was almost as efficient as i.p. injection. Chroni

P C Okafor - One of the best experts on this subject based on the ideXlab platform.

  • corrosion inhibition of mild steel by ethylamino Imidazoline Derivative in co2 saturated solution
    Corrosion Science, 2009
    Co-Authors: P C Okafor, Yugui Zheng
    Abstract:

    The corrosion inhibition and adsorption behaviour of 2-undecyl-1-ethylamino Imidazoline (2UEI) on N80 mild steel in CO2-saturated 3% NaCl solutions was investigated using potentiodynamic polarization, electrochemical impedance spectroscopy techniques and SEM observation. Inhibitor efficiency increased with increase in 2UEI concentration. Temperature studies revealed an increase in inhibition efficiency with rise in temperature and corrosion activation energies decreased in the presence of 2UEI. A mechanism of chemical adsorption of 2UEI on the metal’s surface is proposed. The adsorption characteristics of the inhibitor were approximated by Temkin isotherm. The inhibition efficiency of 2UEI was enhanced in the presence of iodide ions.

  • synergistic inhibition behaviour of methylbenzyl quaternary Imidazoline Derivative and iodide ions on mild steel in h2so4 solutions
    Corrosion Science, 2009
    Co-Authors: P C Okafor, Yugui Zheng
    Abstract:

    The inhibition behaviour of 2-undecyl-1ethylamino-1methylbenzyl quaternary Imidazoline (2UMQI) and KI on mild steel in 1.0 M H(2)SO(4) solutions was investigated at 25 degrees C using electrochemical methods. The results indicated that 2UMQI inhibited the corrosion of mild steel and the extent of inhibition increased with 2UMQI concentrations. The inhibition action in the presence of 2UMQI is due to physical adsorption of 2UMQI. A mixed-inhibition mechanism is proposed for the inhibitive effects of 2UMQI. Inhibition efficiency of 2UMQI was enhanced by the addition of iodide ions. In the presence of KI, the potentials of unpolarization, E(u) was observed and increased with KI concentration. (C) 2009 Elsevier Ltd. All rights reserved.

Bruno Pfeiffer - One of the best experts on this subject based on the ideXlab platform.

  • effect of the new Imidazoline Derivative s 22068 pms 847 on insulin secretion in vitro and glucose turnover in vivo in rats
    European Journal of Pharmacology, 1999
    Co-Authors: Agnes Peletounian, Susan L F Chan, F Rondu, Gaelle Le Bihan, Mariehelene Giroix, A Lamouri, Estera Touboul, Bruno Pfeiffer, Dominique Manechez, Pierre Renard
    Abstract:

    We have investigated the possible mechanisms underlying the antihyperglycaemic effect of the Imidazoline Derivative S-22068. In vitro, in the presence of 5 mmol/l glucose, S-22068 (100 micromol/l) induced a significant and sustained increase in insulin secretion from isolated, perifused, rat islets and a marked sensitization to a subsequent glucose challenge (10 mmol/l). S-22068 (100 micromol/l was able to antagonize the stimulatory effect of diazoxide on 86Rb efflux from preloaded islets incubated in the presence of 20 mmol/l glucose. Experiments were also performed to investigate whether S-22068 can alter glucose turnover and peripheral insulin sensitivity in vivo in mildly diabetic rats and obese, insulin resistant, Zucker rats. Neither glucose production nor individual tissue glucose utilization was modified by S-22068 in either group of rats. Similar results were obtained whether the studies were performed under basal conditions or during euglycaemic/hyperinsulinemic clamps. The results suggest that S-22068 exerts part of its antihyperglycaemic effect by promoting insulin secretion without alteration of peripheral insulin sensitivity.

  • potent antihyperglycaemic property of a new Imidazoline Derivative s 22068 pms 847 in a rat model of niddm
    British Journal of Pharmacology, 1998
    Co-Authors: Agnes Peletounian, F Rondu, A Lamouri, Estera Touboul, Bruno Pfeiffer, Dominique Manechez, Xuan Wang, R Dokhan, S Marc, Pierre Renard
    Abstract:

    Recent data suggest that some Imidazoline Derivatives can lower plasma glucose in experimental animal models of diabetes. We studied the activity of an Imidazoline S-22068, in rat model of non-insulin-dependent diabetes mellitus (NIDDM) produced with a low dose of streptozotocin (35 mg kg(-1), i.v.) in the adult. The respective increase over basal value in glucose (deltaG) and insulin (deltaI), and the rate of glucose disappearance (K), were measured during a 30 min intravenous glucose tolerance test. After an intraperitoneal injection of S-22068 (24 mg kg(-1)), deltaG (mM min(-1)) was decreased (91.67+/-5.83 vs 120.5+/-3.65; P<0.001), whereas K was increased (1.74+/-0.09 vs 1.18+/-0.05; P<0.001). Although insulinaemia was increased at time-point 0 of the test, deltaI was unchanged. During oral glucose tolerance tests (OGTT), S-22068 (24 mg kg(-1), p.o.) improved glucose tolerance, and its efficiency was potentiated after chronic treatment (15 days). Basal glycaemia was unaffected by the treatment. Under the same conditions, a higher dose of S-22068 (40 mg kg(-1)) further improved glucose tolerance without causing hypoglycaemia. Binding experiments revealed that S-22068 displays no affinity for either adrenoceptors or the two Imidazoline receptors I1 or I2. These results demonstrate that S-22068 improves glucose tolerance without causing hypoglycaemia. Thus S-22068 represents a new potential option in the treatment of NIDDM.

  • effect of s 21663 pms 812 an Imidazoline Derivative on glucose tolerance and insulin secretion in a rat model of type ii diabetes
    Journal of Pharmacology and Experimental Therapeutics, 1996
    Co-Authors: Xuan Wang, F Rondu, A Lamouri, Estera Touboul, Bruno Pfeiffer, Dominique Manechez, Pierre Renard, R Dokhan, S Marc, Beatrice Guardiolalemaitre
    Abstract:

    We have studied the activity of S-21663 (PMS 812), a new Imidazoline Derivative, in a rat model of Type II diabetes obtained by i.v. injection of a low dose (35 mg/kg) of streptozotocin, using glucose tolerance tests. Glucose tolerance and insulin secretion were measured as the delta G and the delta l, i.e., the respective increase in glycemia and insulinemia over 30 min after the glucose load. The rate of glucose disappearance was calculated as the K coefficient and the insulin response to glucose as the delta l/delta G. After i.p. injection of S-21663, delta G (millimoles per liter per minute) was decreased (71.7 +/- 10.1 vs. 112.6 +/- 15.1; P < .05), whereas K was increased (3.3 +/- 0.3 vs. 1.5 +/- 0.1; P < .05). Insulin secretion was also largely improved (delta l/delta G: 90.9 +/- 22.2 vs. 18.3 +/- 2.6; P < .05). Oral administration of the product was almost as efficient as i.p. injection. Chronic treatment (15 days) increased the efficiency. Insulin secretion measured in vitro at both 2.8 and 16.6 mM glucose was quadrupled by S-21663 (100 microM). S-21663 binds neither to alpha-2 adrenoceptors nor to known Imidazoline binding sites. S-21663 can be considered as a potential hypoglycemic agent in Type II diabetes.

F Rondu - One of the best experts on this subject based on the ideXlab platform.

  • effect of the new Imidazoline Derivative s 22068 pms 847 on insulin secretion in vitro and glucose turnover in vivo in rats
    European Journal of Pharmacology, 1999
    Co-Authors: Agnes Peletounian, Susan L F Chan, F Rondu, Gaelle Le Bihan, Mariehelene Giroix, A Lamouri, Estera Touboul, Bruno Pfeiffer, Dominique Manechez, Pierre Renard
    Abstract:

    We have investigated the possible mechanisms underlying the antihyperglycaemic effect of the Imidazoline Derivative S-22068. In vitro, in the presence of 5 mmol/l glucose, S-22068 (100 micromol/l) induced a significant and sustained increase in insulin secretion from isolated, perifused, rat islets and a marked sensitization to a subsequent glucose challenge (10 mmol/l). S-22068 (100 micromol/l was able to antagonize the stimulatory effect of diazoxide on 86Rb efflux from preloaded islets incubated in the presence of 20 mmol/l glucose. Experiments were also performed to investigate whether S-22068 can alter glucose turnover and peripheral insulin sensitivity in vivo in mildly diabetic rats and obese, insulin resistant, Zucker rats. Neither glucose production nor individual tissue glucose utilization was modified by S-22068 in either group of rats. Similar results were obtained whether the studies were performed under basal conditions or during euglycaemic/hyperinsulinemic clamps. The results suggest that S-22068 exerts part of its antihyperglycaemic effect by promoting insulin secretion without alteration of peripheral insulin sensitivity.

  • potent antihyperglycaemic property of a new Imidazoline Derivative s 22068 pms 847 in a rat model of niddm
    British Journal of Pharmacology, 1998
    Co-Authors: Agnes Peletounian, F Rondu, A Lamouri, Estera Touboul, Bruno Pfeiffer, Dominique Manechez, Xuan Wang, R Dokhan, S Marc, Pierre Renard
    Abstract:

    Recent data suggest that some Imidazoline Derivatives can lower plasma glucose in experimental animal models of diabetes. We studied the activity of an Imidazoline S-22068, in rat model of non-insulin-dependent diabetes mellitus (NIDDM) produced with a low dose of streptozotocin (35 mg kg(-1), i.v.) in the adult. The respective increase over basal value in glucose (deltaG) and insulin (deltaI), and the rate of glucose disappearance (K), were measured during a 30 min intravenous glucose tolerance test. After an intraperitoneal injection of S-22068 (24 mg kg(-1)), deltaG (mM min(-1)) was decreased (91.67+/-5.83 vs 120.5+/-3.65; P<0.001), whereas K was increased (1.74+/-0.09 vs 1.18+/-0.05; P<0.001). Although insulinaemia was increased at time-point 0 of the test, deltaI was unchanged. During oral glucose tolerance tests (OGTT), S-22068 (24 mg kg(-1), p.o.) improved glucose tolerance, and its efficiency was potentiated after chronic treatment (15 days). Basal glycaemia was unaffected by the treatment. Under the same conditions, a higher dose of S-22068 (40 mg kg(-1)) further improved glucose tolerance without causing hypoglycaemia. Binding experiments revealed that S-22068 displays no affinity for either adrenoceptors or the two Imidazoline receptors I1 or I2. These results demonstrate that S-22068 improves glucose tolerance without causing hypoglycaemia. Thus S-22068 represents a new potential option in the treatment of NIDDM.

  • effect of s 21663 pms 812 an Imidazoline Derivative on glucose tolerance and insulin secretion in a rat model of type ii diabetes
    Journal of Pharmacology and Experimental Therapeutics, 1996
    Co-Authors: Xuan Wang, F Rondu, A Lamouri, Estera Touboul, Bruno Pfeiffer, Dominique Manechez, Pierre Renard, R Dokhan, S Marc, Beatrice Guardiolalemaitre
    Abstract:

    We have studied the activity of S-21663 (PMS 812), a new Imidazoline Derivative, in a rat model of Type II diabetes obtained by i.v. injection of a low dose (35 mg/kg) of streptozotocin, using glucose tolerance tests. Glucose tolerance and insulin secretion were measured as the delta G and the delta l, i.e., the respective increase in glycemia and insulinemia over 30 min after the glucose load. The rate of glucose disappearance was calculated as the K coefficient and the insulin response to glucose as the delta l/delta G. After i.p. injection of S-21663, delta G (millimoles per liter per minute) was decreased (71.7 +/- 10.1 vs. 112.6 +/- 15.1; P < .05), whereas K was increased (3.3 +/- 0.3 vs. 1.5 +/- 0.1; P < .05). Insulin secretion was also largely improved (delta l/delta G: 90.9 +/- 22.2 vs. 18.3 +/- 2.6; P < .05). Oral administration of the product was almost as efficient as i.p. injection. Chronic treatment (15 days) increased the efficiency. Insulin secretion measured in vitro at both 2.8 and 16.6 mM glucose was quadrupled by S-21663 (100 microM). S-21663 binds neither to alpha-2 adrenoceptors nor to known Imidazoline binding sites. S-21663 can be considered as a potential hypoglycemic agent in Type II diabetes.