145301-48-0
Chemical Structure
BIBN-99
- CAS No.: 145301-48-0
- Formula:C31H42ClN5O3
- Molecular Weight:568.15
IUPAC Name: N-(3-(1-(2-(8-chloro-6-oxo-5,6-dihydro-11H-benzo[e]pyrido[3,2-b][1,4]diazepin-11-yl)-2-oxoethyl)piperidin-4-yl)propyl)-N-ethyl-2,2-dimethylpentanamide
InChIKey: LUPAFPUKESJDMZ-UHFFFAOYSA-N
SMILES: CCCC(C)(C(N(CC)CCCC1CCN(CC1)CC(N2C3=NC=CC=C3NC(C4=CC(Cl)=CC=C42)=O)=O)=O)C
Biological Activity: BIBN-99 is a lipophilic M2 muscarinic receptor antagonist that crosses the blood-brain barrier (human pKi = 7.52; rat pKi = 7.57). BIBN-99 enhances acetylcholine release by blocking presynaptic M2 autoreceptors and heteroreceptors, and reverses impaired acetylcholine release. BIBN-99 can be used in research on dementia, age-related cognitive decline, Alzheimer's disease, and traumatic brain injury[1][2][3][4][5][6][7][8][9].
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BIBN-99 | 98.02% | BIBN-99 is a lipophilic M2 muscarinic receptor antagonist that crosses the blood-brain barrier (human pKi = 7.52; rat pKi = 7.57). BIBN-99 enhances acetylcholine release by blocking presynaptic M2 autoreceptors and heteroreceptors, and reverses impaired acetylcholine release. BIBN-99 can be used in research on dementia, age-related cognitive decline, Alzheimer's disease, and traumatic brain injury. | ||||||||||||||||||||
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References
- [1]. Doggrell SA, et al. Treatment of dementia with neurotransmission modulation. Expert opinion on investigational drugs. 2003 Oct 1;12(10):1633-54.
- [2]. Tombaugh GC, et al. Theta-frequency synaptic potentiation in CA1 in vitro distinguishes cognitively impaired from unimpaired aged Fischer 344 rats. The Journal of neuroscience : the official journal of the Society for Neuroscience. 2002 Nov 15;22(22):9932-40.
- [3]. Müller DM, et al. Muscarinic M1 receptor agonists increase the secretion of the amyloid precursor protein ectodomain. Life sciences. 1997 Feb 21;60(13-14):985-91.
- [4]. Doods H, et al. Characterization of BIBN 99: a lipophilic and selective muscarinic M2 receptor antagonist. European journal of pharmacology. 1993 Sep 21;242(1):23-30. [Content Brief]
- [5]. Doods HN, et al. Therapeutic potential of CNS-active M2 antagonists: novel structures and pharmacology. Life sciences. 1993;52(5-6):497-503.
- [6]. Boyle CD, et al. Orally active and selective benzylidene ketal M2 muscarinic receptor antagonists for the treatment of Alzheimer's disease. Drug development research. 2002 Jul;56(3):310-20.
- [7]. Nobuhara K, et al. Z-IQNP: a potential radioligand for SPECT imaging of muscarinic acetylcholine receptors in Alzheimer's disease. Psychopharmacology. 2000 Mar;149(1):45-55.
- [8]. Quirion R, et al. Facilitation of acetylcholine release and cognitive performance by an M(2)-muscarinic receptor antagonist in aged memory-impaired. The Journal of neuroscience : the official journal of the Society for Neuroscience. 1995 Feb;15(2):1455-62.
- [9]. Pearson D M. Effects of M2 autoreceptor blockade on the cognitive performance of aged impaired, aged unimpaired and young rats. 2000.
