Is Mepyramine a reversible antagonist?

The binding of the H1-antagonist, [3H]-mepyramine, was saturable and of high affinity with a maximum binding capacity of 307 +/- 27 fmol mg-1 protein (n = 14) and with an equilibrium dissociation constant (KD) of 1.5 +/- 0.2 nM (n = 14). The binding was rapid and readily reversible.

Is Mepyramine an antagonist?

Mepyramine, a histamine H1 receptor antagonist, inhibits the metabolic activity of rat and human P450 2D forms.

Is Mepyramine an inverse agonist?

Mepyramine, a histamine H1 receptor inverse agonist, binds preferentially to a G protein-coupled form of the receptor and sequesters G protein. J Biol Chem.

What receptors does mepyramine target?

Mepyramine, also known as pyrilamine, is a first generation antihistamine, targeting the H1 receptor as an inverse agonist. It rapidly permeates the brain often causing drowsiness.

Which medicine contains Mepyramine maleate?

Anthisan bite and sting cream contains the active ingredient mepyramine maleate, which is a type of medicine called an antihistamine.

Is Mepyramine maleate safe in pregnancy?

No significant interactions described. There is no evidence of the safety of mepyramine maleate in human pregnancy, but it has been widely used for many years without apparent ill consequence.

Is competitive antagonist reversible?

Competitive antagonists are sub-classified as reversible (surmountable) or irreversible (insurmountable) competitive antagonists, depending on how they interact with their receptor protein targets.

What is the mechanism of action of mepyramine?

Mepyramine is a histamine H1 receptor inverse agonist. It binds to a G protein-coupled form of the receptor and promotes a G protein-coupled inactive state of the H1 receptor that interferes with the Gq/11-mediated signaling.

Is mepyramine an inverse agonist of histamine?

We found that mepyramine acts as an inverse agonist decreasing the basal spontaneous activity of the gp-H 1 r. Moreover, mepyramine inhibited histamine-induced inositol phosphate (InsP) production and intracellular calcium mobilization with a marked decrease in the maximal response to histamine at high mepyramine concentrations.

Is mepyramine an anticholinergic?

Mepyramine, also known as pyrilamine, is a first generation antihistamine, targeting the H1 receptor. It rapidly permeates the brain often causing drowsiness. It also has anticholinergic properties. However, its anticholinergic potency is negligible compared to its antihistaminergic activity; it has an H1 to muscarinic K…

What is mepyramine cream used for?

Mepyramine. It is used in over-the-counter combination products to treat the common cold and menstrual symptoms. It is also the active ingredient of the topical antihistamine creams Anthisan and Neoantergan, sold for the treatment of insect bites, stings, and nettle rash.