LY-293559 - CAS 150010-68-7
Catalog number: 150010-68-7
Category: Inhibitor
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LY 215490, a decahydroisoquinoline derivative, has been found to be an AMPA receptor antagonist that could be a neuroprotective agent in the study of focal ischaemia.
LY-293559; LY 215490; LY-215490; CHEMBL70937; SCHEMBL3678843; ZINC5760; (3R,4aS,6S,8aS)-6-[2-(2H-tetrazol-5-yl)ethyl]-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid
Store in a cool and dry place and at 0 - 4 °C for short term (days to weeks) or -20 °C for long term (months to years).
Quality Standard:
In-house standard
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1.Supraspinal and spinal alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid and N-methyl-D-aspartate glutamatergic control of the micturition reflex in the urethane-anesthetized rat.
Yoshiyama M;de Groat WC Neuroscience. 2005;132(4):1017-26.
Effects of i.c.v. and i.t. administration of (3SR,4aRS,6RS,8aRS)-6-[2-(1H-tetrazol-5-yl)ethyl]decahydroisoquinoline-3-carboxylic acid (LY215490), a competitive alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptor antagonist and MK-801, a non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist on the micturition reflex were evaluated in urethane-anesthetized rats, to determine if glutamatergic mechanisms in brain as well as spinal cord are important for the control of micturition. I.c.v. or i.t. injection of LY215490 in low doses (0.01-0.03 microg) did not change rhythmic bladder or external urethral sphincter (EUS) electromyogram (EMG) activity during continuous cystometrograms (CMGs; 0.21 ml/min), whereas higher doses (0.1-1 microg) markedly suppressed these responses. During single CMGs (0.04 ml/min), 0.1-1 microg i.c.v. or 0.1-10 microg i.t. doses increased volume threshold and pressure threshold for inducing micturition, and decreased bladder contraction amplitude and voiding efficiency. MK-801 in low doses (0.6 microg i.c.v. or 0.6-1.8 microg for i.t.) did not change bladder contraction amplitude or EUS EMG activity during continuous CMGs, whereas higher doses 6-60 microg markedly suppressed these responses.
2.Effects of N-methyl-D-aspartate (dizocilpine) and alpha-amino-3-hydroxy-4-isoxazolepropionate (LY215490) receptor antagonists on the voiding reflex induced by perineal stimulation in the neonatal rat.
Yoshiyama M;Erickson KA;Erdman SL;De Groat WC Neuroscience. 1999;90(4):1415-20.
The present study was undertaken to examine the role of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionate and N-methyl-D-aspartate glutamate receptors in the regulation of voiding reflexes induced by perineal stimulation in the neonatal rat. Four-, six- and 10-day-old awake rats were used in the experiments and perineal stimulation was applied using the tip of a 1-ml syringe to evoke voiding. Voided volume and residual volume were measured. In 10-day-old rats, LY215490 (3-10 mg/kg, i.p.), a competitive alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionate receptor antagonist, significantly inhibited reflex voiding, increasing the residual volume 34-53-fold. A 3 mg/kg dose decreased the urine release by 55%, whereas 10 mg/kg totally suppressed the voiding reflex induced by the perineal stimulation. LY215490 (10 mg/kg, i.p.) produced similar effects in four- and six-day-old rats. Dizocilpine (1-3 mg/kg, i.p.), a non-competitive N-methyl-D-aspartate receptor antagonist, also significantly decreased the urine release (62-82%) and increased residual volume (180-230-fold). Combined administration of LY215490 (1 mg/kg, i.p.) and dizocilpine (0.3 mg/kg, i.p.) to 10-day-old rats, in doses that individually had no effect on perineal stimulation-evoked voiding, depressed voided volume by 65%.
3.Effect of bilateral hypogastric nerve transection on voiding dysfunction in rats with spinal cord injury.
Yoshiyama M;de Groat WC Exp Neurol. 2002 May;175(1):191-7.
We determined if bilateral section of the hypogastric nerves (HGN), which provide the major sympathetic input to the urinary bladder neck/proximal urethra, could improve voiding by reducing urethral resistance in conscious, female spinal-cord-injured (SCI) rats 2-3 weeks after T(7-9) transection of the spinal cord. Cystometry was performed in animals with HGN intact and with HGN sectioned bilaterally 1-2 h before the experiment. Residual volume (RV), volume threshold for inducing micturition (VT), maximal voiding pressure, and bladder compliance were significantly lower (71, 35, 33, and 31%, respectively) in SCI rats with sectioned HGN than in rats with intact HGN, whereas voided volume (VV), pressure threshold for micturition, and bladder contraction duration (BCD) in the two groups were similar. Voiding efficiency (VE) in the HGN-sectioned group was 36% greater than that in the HGN-intact group. Antagonists for AMPA and NMDA glutamatergic receptors (LY215490 and MK-801, respectively) were administered to rats with sectioned HGN, to determine if activity in the HGN contributes to the previously reported inhibitory effects of these drugs, on voiding function after SCI. MK-801 (3 mg/kg iv) significantly reduced VV (75%) and VE (85%) and increased RV (8-fold), VT (87%), and bladder compliance (60%), whereas LY215490 (10 mg/kg iv) significantly increased VT and BCD by 15 and 19%, respectively.
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