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Bromocriptine is a partial agonist of the dopamine D 2 receptor. [ 21 ] [ 22 ] [ 23 ] It also interacts with other dopamine receptors and with various serotonin and adrenergic receptors . [ 21 ] [ 22 ] [ 24 ] Bromocriptine has additionally been found to inhibit the release of glutamate by reversing the GLT1 glutamate transporter .
Prolactin inhibitors are mainly used to treat hyperprolactinemia (high prolactin levels). [1] Agonists of the dopamine D 2 receptor such as bromocriptine and cabergoline are able to strongly suppress pituitary prolactin secretion and thereby decrease circulating prolactin levels, and so are most commonly used as prolactin inhibitors. [1]
[citation needed] Although cabergoline is commonly described principally as a D 2 receptor agonist, it also possesses significant affinity for the dopamine D 3, and D 4, serotonin 5-HT 1A, 5-HT 2A, 5-HT 2B, and 5-HT 2C, and α 2-adrenergic receptors, as well as moderate/low affinity for the dopamine D 1, serotonin 5-HT 7, and α 1-adrenergic ...
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Ergocryptine is an ergopeptine and one of the ergoline alkaloids.It is isolated from ergot or fermentation broth and it serves as starting material for the production of bromocriptine. [1]
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Conversely, BMB-A39a shows minimal or negligible activity in activating the serotonin 5-HT 2B receptor (E max < 20%) and does not activate other serotonin receptors. [ 3 ] [ 4 ] BMB-201 is said to have minimal or absent psychedelic effects due to its reduced serotonin 5-HT 2A receptor intrinsic activity but to potently induce neuroplasticity .
According to the Biopharmaceutics Classification System (BCS) drug substances are classified to four classes upon their solubility and permeability: [1] Class I – high permeability, high solubility. Example: metoprolol, paracetamol [2] Those compounds are well absorbed and their absorption rate is usually higher than excretion.