VU0453595
- Product Name
- VU0453595
- CAS No.
- 1432436-13-9
- Chemical Name
- VU0453595
- Synonyms
- VU453595;VU0453595;VU0453595, 10 mM in DMSO;6-(2-Fluoro-4-(1-methyl-1H-pyrazol-4-yl)benzyl)-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-5-one;6-[[2-Fluoro-4-(1-methyl-1H-pyrazol-4-yl)phenyl]methyl]-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-5-one;5H-Pyrrolo[3,4-b]pyridin-5-one, 6-[[2-fluoro-4-(1-methyl-1H-pyrazol-4-yl)phenyl]methyl]-6,7-dihydro-;Muscarinic acetylcholine receptor,modulator,systemically,allosteric,mAChR,PAM,positive,VU0453595,inhibit,schizophrenia,Inhibitor
- CBNumber
- CB04668659
- Molecular Formula
- C18H15FN4O
- Formula Weight
- 322.34
- MOL File
- 1432436-13-9.mol
VU0453595 Property
- Boiling point:
- 552.8±50.0 °C(Predicted)
- Density
- 1.35±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : 100 mg/mL (310.23 mM; Need ultrasonic)
- form
- Solid
- pka
- 2.98±0.20(Predicted)
- color
- Off-white to light yellow
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
- Precautionary statements
-
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P501Dispose of contents/container to..…
VU0453595 Chemical Properties,Usage,Production
Uses
VU0453595 is a highly selective, systemically active M1 positive allosteric modulator (PAM, EC50=2140nM) for the research of schizophrenia[1][2].
Biological Activity
VU0453595 is a highly selective, systemically active M1 positive allosteric modulator (PAM, EC50=2140 nM) for the research of schizophrenia[1][2]. Application of M1 PAM VU0453595 (3 μM) induces a transient increase in excitability of medium spiny neurons (MSNs)[3]. VU0453595 potentiates M1-mediated muscarinic long-term depression (mLTD)[1].VU0453595 (1-10 mg/kg; i.p.) reverses behavioral deficits induced by repeated phencyclidine (PCP) administration[1].
in vivo
VU0453595 potentiates M1-mediated muscarinic long-term depression (mLTD)[1].
VU0453595 (1-10mg/kg; i.p.) reverses behavioral deficits induced by repeated phencyclidine (PCP) administration[1].
| Animal Model: | Male C57BL6/J mice (8-9 weeks old)[1] |
| Dosage: | 1, 3, or 10mg/kg |
| Administration: | Intraperitoneal (i.p.); 10mL/kg; administered 30min before the social interaction test |
| Result: | Rescued deficits in social interaction observed in PCP-treated mice. |
References
[1]. A Ghoshal, et al. Potentiation of M1 Muscarinic Receptor Reverses Plasticity Deficits and Negative and Cognitive Symptoms in a Schizophrenia Mouse Model. Neuropsychopharmacology. 2016 Jan;41(2):598-610. [2]. Sean P Moran, et al. M1-positive allosteric modulators lacking agonist activity provide the optimal profile for enhancing cognition. Neuropsychopharmacology. 2018 Jul;43(8):1763-1771. [3]. Xiaohui Lv, et al. M1 muscarinic activation induces long-lasting increase in intrinsic excitability of striatal projection neurons. Neuropharmacology. 2017 May 15;118:209-222.
VU0453595 Preparation Products And Raw materials
Raw materials
Preparation Products
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