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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- CAS No.: 222545-63-3
- Formula: C21H25N3
- Molecular Weight:319.44
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Storage:
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Biological Activity
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Biological Activity
Description
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H1 Receptor |
H4 receptor |
In Vitro
Methylhistaprodifen relaxes isolated rat aorta with a pEC50 of 6.8 and an intrinsic activity of 0.61[2].
Methylhistaprodifen is a potent H1 receptor agonist in guinea pig aortic rings, with a pEC50 of 7.40 and a relative potency of 410% compared with histamine[4].
Methylhistaprodifen produces potent H1 receptor-mediated endothelium-dependent relaxation in rat aortic rings, with a pEC50 of 6.80 and a relative potency of 2825% compared with histamine[4].
Methylhistaprodifen contracts endothelium-denuded guinea pig aorta as a partial agonist with a pEC50 of 6.31 and a relative potency of 458 times that of histamine[5].
Methylhistaprodifen contracts endothelium-denuded guinea pig aorta precontracted with PGF2α, with a pEC50 of 7.11 and a relative potency of 410 times that of histamine[5].
Methylhistaprodifen relaxes endothelium-intact rat aortic rings with a pEC50 of 6.80 and a relative potency of 2825-fold versus histamine[5].
Methylhistaprodifen acts as an inverse agonist at hH4R, with a pEC50 of 5.20 and an Emax of -0.93[1].
Methylhistaprodifen (compound 6) contracts isolated guinea pig ileum with a pEC50 of 7.2 and an intrinsic activity of 0.99, indicating potent full H1 receptor agonism[2].
Methylhistaprodifen (150 μM) is a full H1 receptor agonist with a Ca2+ imaging EC50 of 28 μM in cultured Swiss Webster mouse PO/AH neurons[3].
Methylhistaprodifen (150 μM) is a full H1 receptor agonist that activates an inward current in cultured Swiss Webster mouse PO/AH neurons, with an EC50 of 32 μM[3].
Methylhistaprodifen is a full H1 receptor agonist with an EC50 of 31 μM in cultured C57/Bl6 mouse PO/AH neurons[3].
Methylhistaprodifen (compound 7) (30 µM) is a potent H1 receptor agonist in guinea pig ileum, with a pEC50 of 7.24 and a relative potency of 343% compared with histamine[4].
Methylhistaprodifen (compound 13) (30 µM) is a highly potent H1 receptor agonist in guinea pig ileum, with a pEC50 of 7.24 and a relative potency of 343-fold versus histamine[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 222545-63-3
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Molecular Weight 319.44
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Formula C21H25N3
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SMILES
CNCCC1=CN=C(CCC(C2=CC=CC=C2)C3=CC=CC=C3)N1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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]
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Methylhistaprodifen Related Classifications
HY-187962 Related Classifications
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