GR 46611 - CAS 185259-85-2
Category: Inhibitor
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Molecular Formula:
C23H27N3O2
Molecular Weight:
377.49
COA:
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Targets:
5-HT Receptor
Description:
GR 46611 is a 5-HT1D receptor agonist that may be beneficial for the treatment of migraine. 5-HT1D acts on the central nervous system.
Brife Description:
5-HT1D receptor agonist
Synonyms:
GR 46611; GR46611; GR-46611; 3-[3-(2-Dimethylaminoethyl)-1H-indol-5-yl]-N-(4-methoxybenzyl)acrylamide
MSDS:
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InChIKey:
LBVZWEWTNUDWNS-YRNVUSSQSA-N
InChI:
InChI=1S/C23H27N3O2/c1-26(2)13-12-19-16-24-22-10-6-17(14-21(19)22)7-11-23(27)25-15-18-4-8-20(28-3)9-5-18/h4-11,14,16,24H,12-13,15H2,1-3H3,(H,25,27)/b11-7+
Canonical SMILES:
CN(C)CCC1=CNC2=C1C=C(C=C2)C=CC(=O)NCC3=CC=C(C=C3)OC
1.Inhibition of bladder activity by 5-hydroxytryptamine1 serotonin receptor agonists in cats with chronic spinal cord injury.
Gu B1, Olejar KJ, Reiter JP, Thor KB, Dolber PC. J Pharmacol Exp Ther. 2004 Sep;310(3):1266-72. Epub 2004 May 19.
The serotonin (5-hydroxytryptamine1A) 5-HT1A 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)-1H-indol-5-yl]-N-(4-methoxybenzyl)acrylamide), which has agonist activity predominantly at 5-HT1B and 5-HT1D receptors but also at the 5-HT1A 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 microg/kg) and GR-46611 (0.03-300 microg/kg) were followed in three cases each by 5-HT1A antagonist WAY-100635 [N-tert-butyl-3-(4-(2-methoxyphenyl)-piperazin-1-yl)-2-phenylpropanamide] at 300 microg/kg.
2.Effect of 5-hydroxytryptamine1 serotonin receptor agonists on noxiously stimulated micturition in cats with chronic spinal cord injury.
Gu B1, Thor KB, Reiter JP, Dolber PC. J Urol. 2007 Jun;177(6):2381-5.
PURPOSE: The serotonin 5-hydroxytryptamine(1A/7) receptor agonist (R)-8-OH-DPAT (8-hydroxy-2-(di-n-propylamino)tetralin) (Sigma) and the 5-hydroxytryptamine(1A/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).
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CAS 185259-85-2 GR 46611

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