1242443-29-3
1242443-29-3 structure
- Name: VU0364289
- Chemical Name: vu0364289
- CAS Number: 1242443-29-3
- Molecular Formula: C20H21N3O2
- Molecular Weight: 335.40000
- Catalog: Signaling Pathways GPCR/G Protein mGluR
- Create Date: 2018-06-03 08:48:00
- Modify Date: 2024-03-07 18:29:56
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VU0364289 is a highly selective mGlu5 positive allosteric modulator (PAM) (binds to the MPEP (HY-14609A) site), with an EC50 of 1.6 µM. VU0364289 can reverse amphetamine-induced hyperlocomotion in a dose-dependent manner, which can be used for schizophrenia and other psychiatric research[1][2][3].
| Name | vu0364289 |
|---|
| Description | VU0364289 is a highly selective mGlu5 positive allosteric modulator (PAM) (binds to the MPEP (HY-14609A) site), with an EC50 of 1.6 µM. VU0364289 can reverse amphetamine-induced hyperlocomotion in a dose-dependent manner, which can be used for schizophrenia and other psychiatric research[1][2][3]. |
|---|---|
| Related Catalog | |
| Target |
mGlu5:1.6 μM (EC50) |
| In Vivo | VU0364289 (10, 30, 56.6, 100 mg/kg ; i.p.; once) reverse amphetamine-induced hyperlocomotion in a dose-dependent manner, and (56.6, 100 mg/kg) shows significantly fewer ambulations[1]. VU0364289 (10 mg/kg; i.p.; once) is rapidly and significantly absorbed in rats, and shows excellent central nervous system penetration[1]. Animal Model: Adult male Sprague-Dawley rats (250-275 g)[1]. Dosage: 10, 30, 56.6, 100 mg/kg Administration: Intraperitoneal injection; once. Result: Showed activity of reversing the hyperlocomotion induced by amphetamine, and can also significantly fewer ambulations in rats when dose up to 56.6 mg/kg. Animal Model: Adult male Sprague-Dawley rats (250-275 g)[1]. Dosage: 10 mg/kg Administration: Intraperitoneal injection; once. Result: 1.19Pharmacokinetic Parameters of VU0364289 in male Sprague-Dawley rats[1]. Tmax (h) Cmax (ng/mL) Plasma protein binding Rat Fu (free fraction) IP (10 mg/kg) 0.25 1280 94% (h); 90% (r) 0.10 |
| References |
| Molecular Formula | C20H21N3O2 |
|---|---|
| Molecular Weight | 335.40000 |
| Exact Mass | 335.16300 |
| PSA | 56.57000 |
| LogP | 2.42658 |