What is the Origin of Ipamorelin Selectivity?

Ipamorelin is a synthetic pentapeptide developed in the late 20th century, emerging from research into Growth Hormone Secretagogues (GHSs). The term "selectivity" is a pharmacological descriptor used to define the precision of a drug's action on a specific receptor subtype, which is a key metric in drug development for minimizing off-target side effects.

What is the Mechanism of Ipamorelin Selectivity?

The selective mechanism of Ipamorelin involves its unique binding profile to the GHSR in the pituitary and hypothalamus. Upon binding, it mimics the action of ghrelin, stimulating the somatotroph cells to release GH. Crucially, its structure prevents it from activating the molecular pathways that lead to the co-secretion of ACTH and cortisol, a side effect seen with older GHS compounds. This specific action allows for a more physiological, pulsatile release of GH without the associated elevation in stress hormones.

Ipamorelin Selectivity

Meaning

Ipamorelin Selectivity refers to the specific, targeted action of the growth hormone-releasing peptide Ipamorelin, which acts as a highly selective agonist at the ghrelin receptor, also known as the Growth Hormone Secretagogue Receptor (GHSR). This high degree of selectivity allows Ipamorelin to stimulate the pituitary gland to release Growth Hormone (GH) with minimal or no significant effect on the release of other pituitary hormones, such as Prolactin or Cortisol. This characteristic provides a cleaner physiological signal compared to less selective secretagogues.