LU AA33810Potent NPY Y5 receptor antagonist CAS# 304008-29-5 |
- HG-10-102-01
Catalog No.:BCC4271
CAS No.:1351758-81-0
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| Cas No. | 304008-29-5 | SDF | Download SDF |
| PubChem ID | 22254068 | Appearance | Powder |
| Formula | C19H25N3O2S3 | M.Wt | 423.62 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 100 mM in DMSO | ||
| Chemical Name | N-[[4-(4,5-dihydro-[1]benzothiepino[5,4-d][1,3]thiazol-2-ylamino)cyclohexyl]methyl]methanesulfonamide | ||
| SMILES | CS(=O)(=O)NCC1CCC(CC1)NC2=NC3=C(S2)CCSC4=CC=CC=C43 | ||
| Standard InChIKey | UWSBTSAJZMIHBL-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C19H25N3O2S3/c1-27(23,24)20-12-13-6-8-14(9-7-13)21-19-22-18-15-4-2-3-5-16(15)25-11-10-17(18)26-19/h2-5,13-14,20H,6-12H2,1H3,(H,21,22) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Potent neuropeptide Y (NPY) Y5 receptor antagonist (Ki = 1.5 nM in vitro). Displays ≥ 3300-fold affinity for Y5 over Y1, Y2 and Y4 receptors. Also binds human 5-HT2B and 5-HT1A receptors (Ki values are 247 and 478 nM respectively). Exerts anxiolytic- and antidepressant-like effects in rat models of stress sensitivity. |
LU AA33810 Dilution Calculator
LU AA33810 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.3606 mL | 11.803 mL | 23.6061 mL | 47.2121 mL | 59.0152 mL |
| 5 mM | 0.4721 mL | 2.3606 mL | 4.7212 mL | 9.4424 mL | 11.803 mL |
| 10 mM | 0.2361 mL | 1.1803 mL | 2.3606 mL | 4.7212 mL | 5.9015 mL |
| 50 mM | 0.0472 mL | 0.2361 mL | 0.4721 mL | 0.9442 mL | 1.1803 mL |
| 100 mM | 0.0236 mL | 0.118 mL | 0.2361 mL | 0.4721 mL | 0.5902 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Discovery of Lu AA33810: a highly selective and potent NPY5 antagonist with in vivo efficacy in a model of mood disorder.[Pubmed:21782428]
Bioorg Med Chem Lett. 2011 Sep 15;21(18):5436-41.
The structure-activity relationship of a series of tricyclic-sulfonamide compounds 11-32 culminating in the discovery of N-[trans-4-(4,5-dihydro-3,6-dithia-1-aza-benzo[e]azulen-2-ylamino)-cyclohexylmeth yl]-methanesulfonamide (15, LU AA33810) is reported. Compound 15 was identified as a selective and high affinity NPY5 antagonist with good oral bioavailability in mice (42%) and rats (92%). Dose dependent inhibition of feeding was observed after i.c.v. injection of the selective NPY5 agonist ([cPP(1-7),NPY(19-23),Ala(31),Aib(32),Gln(34)]-hPP). In addition, ip administration of LU AA33810 (10 mg/kg) produced antidepressant-like effects in a rat model of chronic mild stress.
Antidepressant-like activity of the neuropeptide Y Y5 receptor antagonist Lu AA33810: behavioral, molecular, and immunohistochemical evidence.[Pubmed:27975125]
Psychopharmacology (Berl). 2017 Feb;234(4):631-645.
RATIONALE: It has recently been found that chronic treatment with the highly selective, brain-penetrating Y5 receptor antagonist, LU AA33810 [N-[[trans-4-[(4,5-dihydro [1] benzothiepino[5,4-d] thiazol-2-yl) amino] cyclohexyl]methyl]-methanesulfonamide], produces antidepressant-like effects in the rat chronic mild stress model. OBJECTIVE: In the present study, we investigated the possible antidepressant-like activity of LU AA33810 in rats subjected to glial ablation in the prefrontal cortex (PFC) by the gliotoxin L-AAA, which is an astroglial degeneration model of depression. RESULTS: We observed that LU AA33810 administered intraperitoneally at a single dose of 10 mg/kg both reversed depressive-like behavioral changes in the forced swim test (FST) and prevented degeneration of astrocytes in the mPFC. The mechanism of antidepressant and glioprotective effects of LU AA33810 has not been studied, so far. We demonstrated the contribution of the noradrenergic rather than the serotonergic pathway to the antidepressant-like action of LU AA33810 in the FST. Moreover, we found that antidepressant-like effect of LU AA33810 was connected with the influence on brain-derived neurotrophic factor (BDNF) protein expression. We also demonstrated the antidepressant-like effect of LU AA33810 in the FST in rats which did not receive the gliotoxin. We found that intracerebroventricular injection of the selective MAPK/ERK inhibitor U0126 (5 mug/2 mul) and the selective PI3K inhibitor LY294002 (10 nmol/2 mul) significantly inhibited the anti-immobility effect of LU AA33810 in the FST in rats, suggesting that MAPK/ERK and PI3K signaling pathways could be involved in the antidepressant-like effect of LU AA33810. CONCLUSION: Our results indicate that LU AA33810 exerts an antidepressant-like effect and suggest the Y5 receptors as a promising target for antidepressant therapy.
The novel neuropeptide Y Y5 receptor antagonist Lu AA33810 [N-[[trans-4-[(4,5-dihydro[1]benzothiepino[5,4-d]thiazol-2-yl)amino]cyclohexyl]me thyl]-methanesulfonamide] exerts anxiolytic- and antidepressant-like effects in rat models of stress sensitivity.[Pubmed:19098165]
J Pharmacol Exp Ther. 2009 Mar;328(3):900-11.
Neuropeptide Y (NPY) regulates physiological processes via receptor subtypes (Y(1), Y(2), Y(4), Y(5), and y(6)). The Y(5) receptor is well known for its role in appetite. Based on expression in the limbic system, we hypothesized that the Y(5) receptor might also modulate stress sensitivity. We identified a novel Y(5) receptor-selective antagonist, LU AA33810 [N-[[trans-4-[(4,5-dihydro[1]-benzothiepino[5,4-d]thiazol-2-yl)amino]cyclohexyl]m ethyl]-methanesulfonamide], that bound to cloned rat Y(5) receptors (K(i) = 1.5 nM) and antagonized NPY-evoked cAMP and calcium mobilization in vitro. LU AA33810 (3-30 mg/kg p.o.) blocked feeding elicited by intracerebroventricular injection of the Y(5) receptor-selective agonist [cPP(1-7),NPY(19-23),Ala(31),Aib(32),Gln(34)]-hPancreatic Polypeptide in Sprague-Dawley rats. In vivo effects of LU AA33810 were correlated with brain exposure > or = 50 ng/g and ex vivo Y(5) receptor occupancy of 22 to 95%. LU AA33810 was subsequently evaluated in models of stress sensitivity. In Fischer 344 rats, LU AA33810 (30 mg/kg p.o.) attenuated increases in plasma ACTH and corticosterone elicited by intracerebroventricular injection of [cPP(1-7),NPY(19-23),Ala(31),Aib(32),Gln(34)]-hPancreatic Polypeptide. In Sprague-Dawley rats subjected to the social interaction test, LU AA33810 (3-30 mg/kg p.o.) produced anxiolytic-like effects after acute or chronic treatment. In Flinders sensitive line rats, chronic dosing of LU AA33810 (10 mg/kg/day i.p.) produced anxiolytic-like effects in the social interaction test, plus antidepressant-like effects in the forced swim test. In Wistar rats exposed to chronic mild stress, chronic dosing of LU AA33810 (3 and 10 mg/kg/day i.p.) produced antidepressant-like activity, i.e., normalization of stress-induced decrease in sucrose consumption. We propose that Y(5) receptors may function as part of an endogenous stress-sensing system to mediate social anxiety and reward or motivational deficits in selected rodent models.
