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替洛利生, 组胺 H3 受体反向激动剂

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P126755-10mg
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P126755-25mg
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P126755-50mg
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P126755-100mg
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GPCR/G Protein (3176) H1 receptor Antagonist (64) H2 receptor Antagonist (15) H3 receptor Antagonist (29) H4 receptor Antagonist (16) Histamine Receptor (191) Immunology/Inflammation (1943) 神经元信号传导 (3333)
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基本描述

英文别名 1-[3-[3-(4-chlorophenyl)propoxy]propyl]piperidine | NNACHAUCXXVJSP-UHFFFAOYSA-N | Pitolisant | DB11642 | NSC-523123 | BDBM50247053 | N07XX11 | Piperidine, 1-[3-[3-(4-chlorophenyl)propoxy]propyl]- | Q426044 | Wakix (TN) | BCP13114 | SCHEMBL117648 | DTXSID3
规格或纯度 Moligand™, ≥98%
英文名称 Pitolisant
生化机理 说明：IC50 值：0.16 nM（Ki 值）；1.5 nM（EC50）[1]Pitolisant（BF2.649）是重组人 H3 受体的一种新型、强效、选择性非咪唑类反向激动剂。BF2.649 是一种竞争性拮抗剂，Ki 值为 0.16 nM，同时也是一种反向激动剂，EC50 值为 1.5 nM，其内在活性比环丙沙星高出约 50%。体外：BF2.649 是一种竞争性拮抗剂，Ki 值为 0.16 nM，是一种反向激动剂，EC50 值为 1.5 nM，内在活性比环丙西凡高出约 50%。Pitolisant 在啮齿动物受体上的体外效力约低 6 倍[1]。体内：在小鼠体内，口服生物利用系数（即口服和静注后曲线下血浆面积之比）为 84%。BF2.649 剂量依赖性地提高了小鼠大脑中的远甲基组胺水平，远甲基组胺是组胺能神经元的一个指标。
运输条件 常规运输
作用类型 拮抗剂
作用机制 组胺 H3 受体反向激动剂
产品介绍

Pitolisant(BF2.649;Ciproxidine)是新型的人重组H3受体选择性反向激动剂，Ki为0.16 nM。

Pitolisant (BF2.649) is a novel, potent, and selective nonimidazole inverse agonist at the recombinant human H3 receptor (Ki=0.16 nM).

AI解读

产品属性

ALogP 4.3

关联靶点（人）

HRH4 Tchem 组胺 H4 受体(Histamine H4 receptor) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
HRH3 Tclin 组胺 H3 受体(Histamine H3 receptor) (22 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
HRH2 Tclin 组胺 H2 受体(Histamine H2 receptor) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
HRH1 Tclin 组胺 H1 受体(Histamine H1 receptor) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
KCNH2 Tclin 钾电压门控通道亚家族 H 成员 2(Potassium voltage-gated channel subfamily H member 2) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
ESR1 Tclin Estrogen receptor alpha (17718 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
NR3C1 Tclin Glucocorticoid receptor (14987 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PGR Tclin Progesterone receptor (8562 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ADRB2 Tclin Beta-2 adrenergic receptor (11824 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CHRM2 Tclin Muscarinic acetylcholine receptor M2 (10671 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ADRB1 Tclin Beta-1 adrenergic receptor (6630 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HTR1A Tclin Serotonin 1a (5-HT1a) receptor (14969 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AR Tclin Androgen Receptor (11781 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CHRM1 Tclin Muscarinic acetylcholine receptor M1 (12690 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
DRD2 Tclin Dopamine D2 receptor (23596 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
GABRA1 Tclin GABA receptor alpha-1 subunit (399 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MAOA Tclin Monoamine oxidase A (11911 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CNR1 Tclin Cannabinoid CB1 receptor (20913 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
DRD1 Tclin Dopamine D1 receptor (9720 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ACHE Tclin Acetylcholinesterase (18204 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PTGS1 Tclin Cyclooxygenase-1 (9233 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SLC6A2 Tclin Norepinephrine transporter (10102 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HRH2 Tclin Histamine H2 receptor (5428 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MAOB Tclin Monoamine oxidase B (8835 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HTR2A Tclin Serotonin 2a (5-HT2a) receptor (14758 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HTR2C Tclin Serotonin 2c (5-HT2c) receptor (11471 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AVPR2 Tclin Vasopressin V2 receptor (2912 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ADORA1 Tclin Adenosine A1 receptor (17603 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AGTR1 Tclin Type-1 angiotensin II receptor (5176 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SLC6A4 Tclin Serotonin transporter (12625 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ADRA1A Tclin Alpha-1a adrenergic receptor (8359 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PTGS2 Tclin Cyclooxygenase-2 (13999 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HRH1 Tclin Histamine H1 receptor (7573 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
OPRM1 Tclin Mu opioid receptor (19785 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
DRD3 Tclin Dopamine D3 receptor (14368 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AVPR1A Tclin Vasopressin V1a receptor (5412 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
OPRD1 Tclin Delta opioid receptor (15096 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
OPRK1 Tclin Kappa opioid receptor (16155 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HTR3A Tclin Serotonin 3a (5-HT3a) receptor (3366 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SLC6A3 Tclin Dopamine transporter (10535 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
GRIN1 Tclin Glutamate (NMDA) receptor subunit zeta 1 (122 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
KCNH2 Tclin HERG (29587 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CACNA1C Tclin Voltage-gated L-type calcium channel alpha-1C subunit (766 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PDE3A Tclin Phosphodiesterase 3A (3309 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ADRA2B Tclin Alpha-2b adrenergic receptor (4412 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ADRA2C Tclin Alpha-2c adrenergic receptor (4876 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CHRM3 Tclin Muscarinic acetylcholine receptor M3 (7750 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HTR2B Tclin Serotonin 2b (5-HT2b) receptor (10323 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
TBXA2R Tclin Thromboxane A2 receptor (5717 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
EDNRA Tclin Endothelin receptor ET-A (5008 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ADORA2A Tclin Adenosine A2a receptor (16305 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ADORA3 Tchem Adenosine A3 receptor (15931 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BDKRB2 Tclin Bradykinin B2 receptor (3970 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HRH3 Tclin Histamine H3 receptor (10389 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CHRNA4 Tclin Neuronal acetylcholine receptor protein alpha-4 subunit (1265 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

关联靶点（其它种属）

Npy1r Neuropeptide Y receptor type 1 (8 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Hrh4 Histamine H4 receptor (388 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Cckar Cholecystokinin A receptor (90 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Pde4d Phosphodiesterase 4D (4 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Hdac6 Histone deacetylase 6 (222 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Mus musculus (284745 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Rattus norvegicus (775804 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BCHE Cholinesterase (8742 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
8238086 Cytochrome P450 (0 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SARS-CoV-2 (38078 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

作用机制

作用机制 Action Type target ID Target Name Target Type Target Organism Binding Site Name 参考文献

名称和识别符

PubChem SID 504765139
分子类型 小分子
IUPAC Name 1-[3-[3-(4-chlorophenyl)propoxy]propyl]piperidine
INCHI InChI=1S/C17H26ClNO/c18-17-9-7-16(8-10-17)6-4-14-20-15-5-13-19-11-2-1-3-12-19/h7-10H,1-6,11-15H2
InChi Key NNACHAUCXXVJSP-UHFFFAOYSA-N
Canonical SMILES C1CCN(CC1)CCCOCCCC2=CC=C(C=C2)Cl
Isomeric SMILES C1CCN(CC1)CCCOCCCC2=CC=C(C=C2)Cl
PubChem CID 9948102
分子量 295.85

化学和物理性质

溶解性 DMSO
分子量 295.800 g/mol
XLogP3 4.300
氢键供体数Hydrogen Bond Donor Count 0
氢键受体数Hydrogen Bond Acceptor Count 2
可旋转键计数Rotatable Bond Count 8
精确质量Exact Mass 295.17 Da
单同位素质量Monoisotopic Mass 295.17 Da
拓扑极表面积Topological Polar Surface Area 12.500 Ų
重原子数Heavy Atom Count 20
形式电荷Formal Charge 0
复杂度Complexity 235.000
同位素原子数Isotope Atom Count 0
定义的原子立体中心计数Defined Atom Stereocenter Count 0
未定义的原子立体中心计数Undefined Atom Stereocenter Count 0
定义的键立体中心计数Defined Bond Stereocenter Count 0
未定义的键立体中心计数Undefined Bond Stereocenter Count 0
所有立体化学键的总数The total count of all stereochemical bonds 0
共价键合单元计数Covalently-Bonded Unit Count 1

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批号(Lot Number) 证书类型 日期 货号
G1520086 分析证书 23-02-03 P126755
A2213424 分析证书 22-02-12 P126755
A2214123 分析证书 22-02-12 P126755
A2214124 分析证书 22-02-12 P126755

参考文献

1. Ligneau X, Perrin D, Landais L, Camelin JC, Calmels TP, Berrebi-Bertrand I, Lecomte JM, Parmentier R, Anaclet C, Lin JS et al..  (2007)  BF2.649 [1-{3-[3-(4-Chlorophenyl)propoxy]propyl}piperidine, hydrochloride], a nonimidazole inverse agonist/antagonist at the human histamine H3 receptor: Preclinical pharmacology..  J Pharmacol Exp Ther,  320  (1): (365-75).  [PMID:17005916] [10.1021/op500134e]
2. Lin JS, Dauvilliers Y, Arnulf I, Bastuji H, Anaclet C, Parmentier R, Kocher L, Yanagisawa M, Lehert P, Ligneau X et al..  (2008)  An inverse agonist of the histamine H(3) receptor improves wakefulness in narcolepsy: studies in orexin-/- mice and patients..  Neurobiol Dis,  30  (1): (74-83).  [PMID:18295497] [10.1021/op500134e]
3. Celanire S, Wijtmans M, Talaga P, Leurs R, de Esch IJ.  (2005)  Keynote review: histamine H3 receptor antagonists reach out for the clinic..  Drug Discov Today,  10  (23-24): (1613-27).  [PMID:16376822] [10.1021/op500134e]
4. Stocking EM, Letavic MA.  (2008)  Histamine H3 antagonists as wake-promoting and pro-cognitive agents..  Curr Top Med Chem,  8  (11): (988-1002).  [PMID:18673168] [10.1021/op500134e]
5. Pierson PD, Fettes A, Freichel C, Gatti-McArthur S, Hertel C, Huwyler J, Mohr P, Nakagawa T, Nettekoven M, Plancher JM et al..  (2009)  5-hydroxyindole-2-carboxylic acid amides: novel histamine-3 receptor inverse agonists for the treatment of obesity..  J Med Chem,  52  (13): (3855-68).  [PMID:19456097] [10.1021/op500134e]
6. Ligneau X, Landais L, Perrin D, Piriou J, Uguen M, Denis E, Robert P, Parmentier R, Anaclet C, Lin JS et al..  (2007)  Brain histamine and schizophrenia: potential therapeutic applications of H3-receptor inverse agonists studied with BF2.649..  Biochem Pharmacol,  73  (8): (1215-24).  [PMID:17343831] [10.1021/op500134e]
7. Łazewska D, Kuder K, Ligneau X, Camelin JC, Schunack W, Stark H, Kieć-Kononowicz K.  (2009)  Diether derivatives of homo- or substituted piperidines as non-imidazole histamine H3 receptor ligands..  Bioorg Med Chem,  17  (8): (3037-42).  [PMID:19329325] [10.1021/op500134e]
8. Schwartz JC.  (2011)  The histamine H3 receptor: from discovery to clinical trials with pitolisant..  Br J Pharmacol,  163  (4): (713-21).  [PMID:21615387] [10.1021/op500134e]
9. Kollb-Sielecka M, Demolis P, Emmerich J, Markey G, Salmonson T, Haas M.  (2017)  The European Medicines Agency review of pitolisant for treatment of narcolepsy: summary of the scientific assessment by the Committee for Medicinal Products for Human Use..  Sleep Med,  33  (13): (125-129).  [PMID:28449891] [10.1021/op500134e]
10. Szakacs Z, Dauvilliers Y, Mikhaylov V, Poverennova I, Krylov S, Jankovic S, Sonka K, Lehert P, Lecomte I, Lecomte JM et al..  (2017)  Safety and efficacy of pitolisant on cataplexy in patients with narcolepsy: a randomised, double-blind, placebo-controlled trial..  Lancet Neurol,  16  (3): (200-207).  [PMID:28129985] [10.1021/op500134e]

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