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Paul C. Dolber - One of the best experts on this subject based on the ideXlab platform.
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effect of 5 hydroxytryptamine1 Serotonin Receptor Agonists on noxiously stimulated micturition in cats with chronic spinal cord injury
The Journal of Urology, 2007Co-Authors: Karl B. Thor, Jerome P. Reiter, Paul C. DolberAbstract:Purpose: The Serotonin 5-hydroxytryptamine1A/7 Receptor agonist (R)-8-OH-DPAT (8-hydroxy-2-(di-n-propylamino)tetralin) (Sigma®) and the 5-hydroxytryptamine1A/1B/1D agonist GR-46611 (3-[3-(2-dimethylaminoethyl)-1H-indol-5-yl]-N-(4-methoxybenzyl)acrylamide) (Tocris Cookson, Ellisville, Missouri) inhibit bladder activity during saline infusion into the bladder of cats with chronic spinal cord injury (saline infused, spinal cord injured cats), suggesting an effect on mechanosensitive bladder afferent C fibers or their targets. We investigated the effects of (R)-8-OH-DPAT and GR-46611 on bladder activity in chronic spinal cord injured cats during infusion of dilute acetic acid into the bladder to stimulate chemosensitive bladder afferent C fibers (acid infused, spinal cord injured cats).Materials and Methods: Chloralose anesthetized, spinal cord injured cats were catheterized through the bladder dome for filling cystometry during 0.5% acetic acid infusion. Dose-response curves for (R)-8-OH-DPAT (0.3 to 30 μg/k...
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Inhibition of bladder activity by 5-hydroxytryptamine1 Serotonin Receptor Agonists in cats with chronic spinal cord injury.
Journal of Pharmacology and Experimental Therapeutics, 2004Co-Authors: Kenneth J. Olejar, Jerome P. Reiter, Karl B. Thor, Paul C. DolberAbstract:The Serotonin (5-hydroxytryptamine 1A ) 5-HT 1A Receptor agonist 8-OH-DPAT [( R )- (+)-8-hydroxy-2-(di- n -propylamino)tetralin] inhibits bladder activity under nociceptive but not innocuous conditions in cats with an intact spinal cord, suggestive of an effect on primary afferent C fibers or their targets. Because C fibers play a key role in reflex micturition in chronic spinal cord injury (SCI), we investigated the effect of 8-OH-DPAT on micturition in SCI cats. We also investigated GR-46611 (3-[3-(2-dimethylaminoethyl)-1 H -indol-5-yl]- N -(4-methoxybenzyl)acrylamide), which has agonist activity predominantly at 5-HT 1B and 5-HT 1D Receptors but also at the 5-HT 1A Receptor. Chloralose-anesthetized cats were catheterized through the bladder dome for saline-filling cystometry. Dose-response curves for i.v. 8-OH-DPAT (0.3-30 μg/kg) and GR-46611 (0.03-300 μg/kg) were followed in three cases each by 5-HT 1A antagonist WAY-100635 [ N -tert-butyl-3-(4-(2-methoxyphenyl)-piperazin-1-yl)-2-phenylpropanamide] at 300 μg/kg. Threshold volume, capacity, residual volume, micturition volume, and arterial pressure were measured. Intact cats showed few significant changes in cystometric variables. SCI cats responded to both 8-OH-DPAT and GR-46611 with dose-dependent increases in threshold volume, capacity, and residual volume, significant at ≥10 μg/kg for 8-OH-DPAT and at ≥3 μg/kg for GR-46611. Effects of 8-OH-DPAT but not GR-46611 were largely reversed by WAY-100635. Both 5-HT 1A and 5-HT 1B/1D Agonists may offer a promising means of reducing bladder hyperactivity and increasing bladder capacity in patients with chronic SCI.
Karl B. Thor - One of the best experts on this subject based on the ideXlab platform.
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effect of 5 hydroxytryptamine1 Serotonin Receptor Agonists on noxiously stimulated micturition in cats with chronic spinal cord injury
The Journal of Urology, 2007Co-Authors: Karl B. Thor, Jerome P. Reiter, Paul C. DolberAbstract:Purpose: The Serotonin 5-hydroxytryptamine1A/7 Receptor agonist (R)-8-OH-DPAT (8-hydroxy-2-(di-n-propylamino)tetralin) (Sigma®) and the 5-hydroxytryptamine1A/1B/1D agonist GR-46611 (3-[3-(2-dimethylaminoethyl)-1H-indol-5-yl]-N-(4-methoxybenzyl)acrylamide) (Tocris Cookson, Ellisville, Missouri) inhibit bladder activity during saline infusion into the bladder of cats with chronic spinal cord injury (saline infused, spinal cord injured cats), suggesting an effect on mechanosensitive bladder afferent C fibers or their targets. We investigated the effects of (R)-8-OH-DPAT and GR-46611 on bladder activity in chronic spinal cord injured cats during infusion of dilute acetic acid into the bladder to stimulate chemosensitive bladder afferent C fibers (acid infused, spinal cord injured cats).Materials and Methods: Chloralose anesthetized, spinal cord injured cats were catheterized through the bladder dome for filling cystometry during 0.5% acetic acid infusion. Dose-response curves for (R)-8-OH-DPAT (0.3 to 30 μg/k...
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Inhibition of bladder activity by 5-hydroxytryptamine1 Serotonin Receptor Agonists in cats with chronic spinal cord injury.
Journal of Pharmacology and Experimental Therapeutics, 2004Co-Authors: Kenneth J. Olejar, Jerome P. Reiter, Karl B. Thor, Paul C. DolberAbstract:The Serotonin (5-hydroxytryptamine 1A ) 5-HT 1A Receptor agonist 8-OH-DPAT [( R )- (+)-8-hydroxy-2-(di- n -propylamino)tetralin] inhibits bladder activity under nociceptive but not innocuous conditions in cats with an intact spinal cord, suggestive of an effect on primary afferent C fibers or their targets. Because C fibers play a key role in reflex micturition in chronic spinal cord injury (SCI), we investigated the effect of 8-OH-DPAT on micturition in SCI cats. We also investigated GR-46611 (3-[3-(2-dimethylaminoethyl)-1 H -indol-5-yl]- N -(4-methoxybenzyl)acrylamide), which has agonist activity predominantly at 5-HT 1B and 5-HT 1D Receptors but also at the 5-HT 1A Receptor. Chloralose-anesthetized cats were catheterized through the bladder dome for saline-filling cystometry. Dose-response curves for i.v. 8-OH-DPAT (0.3-30 μg/kg) and GR-46611 (0.03-300 μg/kg) were followed in three cases each by 5-HT 1A antagonist WAY-100635 [ N -tert-butyl-3-(4-(2-methoxyphenyl)-piperazin-1-yl)-2-phenylpropanamide] at 300 μg/kg. Threshold volume, capacity, residual volume, micturition volume, and arterial pressure were measured. Intact cats showed few significant changes in cystometric variables. SCI cats responded to both 8-OH-DPAT and GR-46611 with dose-dependent increases in threshold volume, capacity, and residual volume, significant at ≥10 μg/kg for 8-OH-DPAT and at ≥3 μg/kg for GR-46611. Effects of 8-OH-DPAT but not GR-46611 were largely reversed by WAY-100635. Both 5-HT 1A and 5-HT 1B/1D Agonists may offer a promising means of reducing bladder hyperactivity and increasing bladder capacity in patients with chronic SCI.
Jerome P. Reiter - One of the best experts on this subject based on the ideXlab platform.
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effect of 5 hydroxytryptamine1 Serotonin Receptor Agonists on noxiously stimulated micturition in cats with chronic spinal cord injury
The Journal of Urology, 2007Co-Authors: Karl B. Thor, Jerome P. Reiter, Paul C. DolberAbstract:Purpose: The Serotonin 5-hydroxytryptamine1A/7 Receptor agonist (R)-8-OH-DPAT (8-hydroxy-2-(di-n-propylamino)tetralin) (Sigma®) and the 5-hydroxytryptamine1A/1B/1D agonist GR-46611 (3-[3-(2-dimethylaminoethyl)-1H-indol-5-yl]-N-(4-methoxybenzyl)acrylamide) (Tocris Cookson, Ellisville, Missouri) inhibit bladder activity during saline infusion into the bladder of cats with chronic spinal cord injury (saline infused, spinal cord injured cats), suggesting an effect on mechanosensitive bladder afferent C fibers or their targets. We investigated the effects of (R)-8-OH-DPAT and GR-46611 on bladder activity in chronic spinal cord injured cats during infusion of dilute acetic acid into the bladder to stimulate chemosensitive bladder afferent C fibers (acid infused, spinal cord injured cats).Materials and Methods: Chloralose anesthetized, spinal cord injured cats were catheterized through the bladder dome for filling cystometry during 0.5% acetic acid infusion. Dose-response curves for (R)-8-OH-DPAT (0.3 to 30 μg/k...
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Inhibition of bladder activity by 5-hydroxytryptamine1 Serotonin Receptor Agonists in cats with chronic spinal cord injury.
Journal of Pharmacology and Experimental Therapeutics, 2004Co-Authors: Kenneth J. Olejar, Jerome P. Reiter, Karl B. Thor, Paul C. DolberAbstract:The Serotonin (5-hydroxytryptamine 1A ) 5-HT 1A Receptor agonist 8-OH-DPAT [( R )- (+)-8-hydroxy-2-(di- n -propylamino)tetralin] inhibits bladder activity under nociceptive but not innocuous conditions in cats with an intact spinal cord, suggestive of an effect on primary afferent C fibers or their targets. Because C fibers play a key role in reflex micturition in chronic spinal cord injury (SCI), we investigated the effect of 8-OH-DPAT on micturition in SCI cats. We also investigated GR-46611 (3-[3-(2-dimethylaminoethyl)-1 H -indol-5-yl]- N -(4-methoxybenzyl)acrylamide), which has agonist activity predominantly at 5-HT 1B and 5-HT 1D Receptors but also at the 5-HT 1A Receptor. Chloralose-anesthetized cats were catheterized through the bladder dome for saline-filling cystometry. Dose-response curves for i.v. 8-OH-DPAT (0.3-30 μg/kg) and GR-46611 (0.03-300 μg/kg) were followed in three cases each by 5-HT 1A antagonist WAY-100635 [ N -tert-butyl-3-(4-(2-methoxyphenyl)-piperazin-1-yl)-2-phenylpropanamide] at 300 μg/kg. Threshold volume, capacity, residual volume, micturition volume, and arterial pressure were measured. Intact cats showed few significant changes in cystometric variables. SCI cats responded to both 8-OH-DPAT and GR-46611 with dose-dependent increases in threshold volume, capacity, and residual volume, significant at ≥10 μg/kg for 8-OH-DPAT and at ≥3 μg/kg for GR-46611. Effects of 8-OH-DPAT but not GR-46611 were largely reversed by WAY-100635. Both 5-HT 1A and 5-HT 1B/1D Agonists may offer a promising means of reducing bladder hyperactivity and increasing bladder capacity in patients with chronic SCI.
Najam A. Sharif - One of the best experts on this subject based on the ideXlab platform.
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β-Oxygenated Analogues of the 5-HT2A Serotonin Receptor Agonist 1-(4-Bromo-2,5-dimethoxyphenyl)-2-aminopropane
Journal of Medicinal Chemistry, 2004Co-Authors: Richard A. Glennon, Mikhail L. Bondarev, Nantaka Khorana, Richard Young, Jesse A. May, Mark R. Hellberg, Marsha A. Mclaughlin, Najam A. SharifAbstract:Activation of 5-HT2A Serotonin Receptors represents a novel approach to lowering intraocular pressure. Because 5-HT2A Serotonin Receptor Agonists might also produce undesirable central effects should sufficient quantities enter the brain, attempts were made to identify 5-HT2 Serotonin Receptor Agonists with reduced propensity to penetrate the blood−brain barrier. 1-(4-Bromo-2,5-dimethoxyphenyl)-2-aminopropan-1-ol (6), an analogue of the 5-HT2 Serotonin Receptor agonist 1-(4-bromo-2,5-dimethoxyphenyl)-2-aminopropane (DOB; 1a) bearing a benzylic hydroxyl group, was identified as a candidate structure. Of the four optical isomers of 6, the 1R,2R-isomer (6d; Ki = 0.5 nM) was found to bind at 5-HT2A Receptors with an affinity similar to that of R(−)DOB (Ki = 0.2 nM). Like R(−)DOB, 6d behaved as a partial agonist (efficacy ca. 50%) in a 5-HT2-mediated calcium mobilization assay. However, in an in vivo test of central action (i.e., stimulus generalization with rats as subjects), 6d was >15 times less potent than...
Kenneth J. Olejar - One of the best experts on this subject based on the ideXlab platform.
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Inhibition of bladder activity by 5-hydroxytryptamine1 Serotonin Receptor Agonists in cats with chronic spinal cord injury.
Journal of Pharmacology and Experimental Therapeutics, 2004Co-Authors: Kenneth J. Olejar, Jerome P. Reiter, Karl B. Thor, Paul C. DolberAbstract:The Serotonin (5-hydroxytryptamine 1A ) 5-HT 1A Receptor agonist 8-OH-DPAT [( R )- (+)-8-hydroxy-2-(di- n -propylamino)tetralin] inhibits bladder activity under nociceptive but not innocuous conditions in cats with an intact spinal cord, suggestive of an effect on primary afferent C fibers or their targets. Because C fibers play a key role in reflex micturition in chronic spinal cord injury (SCI), we investigated the effect of 8-OH-DPAT on micturition in SCI cats. We also investigated GR-46611 (3-[3-(2-dimethylaminoethyl)-1 H -indol-5-yl]- N -(4-methoxybenzyl)acrylamide), which has agonist activity predominantly at 5-HT 1B and 5-HT 1D Receptors but also at the 5-HT 1A Receptor. Chloralose-anesthetized cats were catheterized through the bladder dome for saline-filling cystometry. Dose-response curves for i.v. 8-OH-DPAT (0.3-30 μg/kg) and GR-46611 (0.03-300 μg/kg) were followed in three cases each by 5-HT 1A antagonist WAY-100635 [ N -tert-butyl-3-(4-(2-methoxyphenyl)-piperazin-1-yl)-2-phenylpropanamide] at 300 μg/kg. Threshold volume, capacity, residual volume, micturition volume, and arterial pressure were measured. Intact cats showed few significant changes in cystometric variables. SCI cats responded to both 8-OH-DPAT and GR-46611 with dose-dependent increases in threshold volume, capacity, and residual volume, significant at ≥10 μg/kg for 8-OH-DPAT and at ≥3 μg/kg for GR-46611. Effects of 8-OH-DPAT but not GR-46611 were largely reversed by WAY-100635. Both 5-HT 1A and 5-HT 1B/1D Agonists may offer a promising means of reducing bladder hyperactivity and increasing bladder capacity in patients with chronic SCI.
