The application notes include recommended starting dilutions; optimal dilutions/concentrations should be determined by the end user.
Small HRH1 agonists exhibit similar effects at Human HRH1 and guinea pig HRH1, whereas bulkier 2-phenylhistamines and histaprodifens are up to ~10-fold more potent at guinea pig HRH1 than at Human HRH1.
Several first-generation HRH1 antagonists are ~2-fold, and arpromidine-type HRH1 antagonists up to ~10-fold more potent at guinea pig HRH1 than at Human HRH1.
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Shipped on dry ice. Upon delivery aliquot and store at -80ºC. Avoid freeze / thaw cycles.
In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamine release from adrenal medulla, as well as mediating neurotransmission in the central nervous system.
Belongs to the G-protein coupled receptor 1 family.
Potential sites of phosphorylation in the third cytoplasmic loop may play an important role in regulating signal transduction through the receptor molecule.