222545-63-3
Chemical Structure
Methylhistaprodifen
- CAS No.: 222545-63-3
- Formula:C21H25N3
- Molecular Weight:319.44
InChIKey: YMVWDVNGNLXSKR-UHFFFAOYSA-N
SMILES: CNCCC1=CN=C(CCC(C2=CC=CC=C2)C3=CC=CC=C3)N1
Biological Activity: Methylhistaprodifen is a selective histamine H1 receptor agonist. Methylhistaprodifen also exhibits inverse agonist activity at the H4 receptor. Methylhistaprodifen partially activates recombinant H1 receptor subtypes through Gq-mediated GTP hydrolysis, and activates H1 signaling, smooth muscle contraction, and vasodilation. Methylhistaprodifen is a full agonist at the mouse H1 receptor, elicits Ca2+ release with a slow response decay, and stabilizes the inactive H4 receptor conformation to reduce constitutive G protein signaling[1][2][3][4][5].
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Methylhistaprodifen | Methylhistaprodifen is a selective histamine H1 receptor agonist. Methylhistaprodifen also exhibits inverse agonist activity at the H4 receptor. Methylhistaprodifen partially activates recombinant H1 receptor subtypes through Gq-mediated GTP hydrolysis, and activates H1 signaling, smooth muscle contraction, and vasodilation. Methylhistaprodifen is a full agonist at the mouse H1 receptor, elicits Ca2+ release with a slow response decay, and stabilizes the inactive H4 receptor conformation to reduce constitutive G protein signaling. | |||||||||||||||||||||
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References
- [1]. Deml KF, et al. Interactions of histamine H1-receptor agonists and antagonists with the human histamine H4-receptor. Mol Pharmacol. 2009 Nov;76(5):1019-30.
- [2]. Pertz HH, et al. Structure-activity relationships of histamine H1-receptor agonists. Mini reviews in medicinal chemistry. 2004 Nov;4(9):935-40. [Content Brief]
- [3]. Tabarean IV, et al. Functional pharmacology of H1 histamine receptors expressed in mouse preoptic/anterior hypothalamic neurons. British journal of pharmacology. 2013 Sep;170(2):415-25.
- [4]. Elz S, et al. Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H(1)-receptor agonists. Journal of medicinal chemistry. 2000 Mar 23;43(6):1071-84. [Content Brief]
