222545-59-7
Chemical Structure
Histaprodifen
- CAS No.: 222545-59-7
- Formula:C20H23N3
- Molecular Weight:305.42
InChIKey: BPZGZNLONLANFE-UHFFFAOYSA-N
SMILES: NCCC1=CN=C(CCC(C2=CC=CC=C2)C3=CC=CC=C3)N1
Biological Activity: Histaprodifen is a selective histamine H1 receptor agonist that preferentially recruits β-arrestin2 over β-arrestin1. Histaprodifen activates phosphoinositide signaling and partially stimulates Gq-catalyzed GTP hydrolysis, stimulates astrocyte NGF secretion in a concentration-dependent manner, and produces guinea pig ileum/aorta contraction, rat aorta endothelium-dependent relaxation, and vascular hypotensive effects. Histaprodifen can be used for research on neurological diseases and cardiovascular diseases[1][2][3][4][5][6][7][8][9].
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Histaprodifen | Histaprodifen is a selective histamine H1 receptor agonist that preferentially recruits β-arrestin2 over β-arrestin1. Histaprodifen activates phosphoinositide signaling and partially stimulates Gq-catalyzed GTP hydrolysis, stimulates astrocyte NGF secretion in a concentration-dependent manner, and produces guinea pig ileum/aorta contraction, rat aorta endothelium-dependent relaxation, and vascular hypotensive effects. Histaprodifen can be used for research on neurological diseases and cardiovascular diseases. | |||||||||||||||||||||
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References
- [1]. Lieb S, et al. Label-free versus conventional cellular assays: Functional investigations on the human histamine H1 receptor. Pharmacological research. 2016 Dec 1;114:13-26. [Content Brief]
- [2]. Lipnik-Štangelj M, et al. Activation of histamine H1-receptor enhances neurotrophic factor secretion from cultured astrocytes. Inflammation Research. 2004 May;53(6):245-52. [Content Brief]
- [3]. Straßer A, et al. Pharmacological profile of histaprodifens at four recombinant histamine H1 receptor species isoforms. The Journal of pharmacology and experimental therapeutics. 2008 Jan 1;324(1):60-71. [Content Brief]
- [4]. Deml KF, et al. Interactions of histamine H1-receptor agonists and antagonists with the human histamine H4-receptor. Molecular pharmacology. 2009 Nov 1;76(5):1019-30. [Content Brief]
- [5]. Elz S, et al. Ring-substituted histaprodifen analogues as partial agonists for histamine H1 receptors: synthesis and structure–activity relationships. European journal of medicinal chemistry. 2000 Jan 1;35(1):41-52. [Content Brief]
- [6]. Pertz HH, et al. Structure-activity relationships of histamine H1-receptor agonists. Mini Rev Med Chem. 2004 Nov;4(9):935-40. [Content Brief]
- [7]. Elz S, et al. Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H1-receptor agonists. Journal of medicinal chemistry. 2000 Mar 23;43(6):1071-84. [Content Brief]
- [8]. Menghin S, et al. N α-Imidazolylalkyl and pyridylalkyl derivatives of histaprodifen: synthesis and in vitro evaluation of highly potent histamine H1-receptor agonists. Journal of medicinal chemistry. 2003 Dec 4;46(25):5458-70. [Content Brief]
