720691-69-0
Chemical Structure
GSK239512
- CAS No.: 720691-69-0
- Formula:C23H27N3O2
- Molecular Weight:377.48
IUPAC Name: 1-(6-((3-cyclobutyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-yl)oxy)pyridin-3-yl)pyrrolidin-2-one
InChIKey: YFRBKEVUUCQYOW-UHFFFAOYSA-N
SMILES: O=C1N(C2=CC=C(OC3=CC=C4CCN(C5CCC5)CCC4=C3)N=C2)CCC1
Biological Activity: GSK239512 is a blood-brain barrier-permeable, orally active H3 receptor antagonist, with a human pKi ranging from <5.5 to 9.92 and a murine pKi ranging from 9.44 to 9.83. GSK239512 modulates cholinergic and monoaminergic neurotransmission, blocks the inhibitory feedback of H3 receptors, and increases the release of pro-cognitive neurotransmitters. GSK239512 induces oligodendrocyte precursor cell differentiation and restores myelin gene expression at the cellular level. GSK239512 reverses Scopolamine (HY-N0296)-induced memory deficits and improves recognition memory in animal models. GSK239512 can be used in research related to Alzheimer's disease, chronic traumatic encephalopathy, relapsing-remitting multiple sclerosis, and schizophrenia[1][2][3][4][5][6].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
GSK239512 | 99.09% | GSK239512 is a blood-brain barrier-permeable, orally active H3 receptor antagonist, with a human pKi ranging from <5.5 to 9.92 and a murine pKi ranging from 9.44 to 9.83. GSK239512 modulates cholinergic and monoaminergic neurotransmission, blocks the inhibitory feedback of H3 receptors, and increases the release of pro-cognitive neurotransmitters. GSK239512 induces oligodendrocyte precursor cell differentiation and restores myelin gene expression at the cellular level. GSK239512 reverses Scopolamine (HY-N0296)-induced memory deficits and improves recognition memory in animal models. GSK239512 can be used in research related to Alzheimer's disease, chronic traumatic encephalopathy, relapsing-remitting multiple sclerosis, and schizophrenia. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
References
- [1]. Grove RA, et al. A randomized, double-blind, placebo-controlled, 16-week study of the H3 receptor antagonist, GSK239512 as a monotherapy in subjects with mild-to-moderate Alzheimer's disease. Current Alzheimer research. 2014 Jan;11(1):47-58. [Content Brief]
- [2]. Cheng H, et al. Tau overexpression exacerbates neuropathology after repeated mild head impacts in male mice. Neurobiol Dis. 2020 Feb;134:104683. [Content Brief]
- [3]. Schwartzbach CJ, et al. Lesion remyelinating activity of GSK239512 versus placebo in patients with relapsing-remitting multiple sclerosis: a randomised, single-blind, phase II study. Journal of neurology. 2017 Feb;264(2):304-315. [Content Brief]
- [4]. Jarskog LF, et al. A Phase II study of a histamine H₃ receptor antagonist GSK239512 for cognitive impairment in stable schizophrenia subjects on antipsychotic therapy. Schizophrenia research. 2015 May;164(1-3):136-42. [Content Brief]
- [5]. Ashworth S, et al. Unexpectedly high affinity of a novel histamine H(3) receptor antagonist, GSK239512, in vivo in human brain, determined using PET. British journal of pharmacology. 2014 Mar;171(5):1241-9. [Content Brief]
- [6]. Wilson DM, et al. Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists. Bioorganic & medicinal chemistry letters. 2013 Dec 15;23(24):6890-6. [Content Brief]
