How Do Melanocortin Agonists Work?

Reviewed on 10/6/2021

HOW DO MELANOCORTIN AGONISTS WORK?

Melanocortin receptor (MCR) agonists are neuropeptides used to treat hypoactive sexual desire disorder (HSDD-having no sex drive or a low sex drive) and obesity. Melanocortins are a group of peptide hormones that are essential for certain functions such as sexual response, steroidogenesis (synthesis of steroid hormones), and regulating skin pigmentation. Melanocortins include adrenocorticotropin hormone (ACTH) and different forms of melanocyte-stimulating hormone. MCR agonists mimic the effects of melanocortins. They also exhibit anti-inflammatory properties.

MCRs are a family of five seven-transmembrane G-protein-coupled receptors. MCR agonists act by binding and nonselectively activating most of the receptor subtypes, such as MC1R, MC4R, MC3R, MC5R, and MC2R, or by specifically activating receptor MC4R.

  • MC1R is expressed on melanocytes; binding to this receptor leads to melanin expression and increased pigmentation of the skin and hair. Melanocortin MC1R is also expressed on leukocytes where it may mediate the anti-inflammatory property. 
  • MC2R is the adrenocortical ACTH receptor expressed in the adrenal cortex zona reticularis and zona fasciculata, where it mediates the effects of ACTH on steroid secretion. 
  • MC3R is identified in several areas of the central nervous system and peripheral tissues and is involved in maintaining energy balance.
  • MC4R is expressed in neurons present in several areas of the central nervous system and regulates both food intake and sexual function.
  • MC5R is expressed in numerous human peripheral tissues and is mainly involved in exocrine function, particularly sebaceous gland secretion.

HOW ARE MELANOCORTIN AGONISTS USED?

Melanocortin agonists are administered as subcutaneous injections to treat:

  • HSDD
  • Obesity
 

WHAT ARE SIDE EFFECTS OF MELANOCORTIN AGONISTS? 

Side effects of melanocortin agonists include:

 

The information contained herein is not intended to cover all possible side effects, precautions, warnings, drug interactions, allergic reactions, or adverse effects. Check with your doctor or pharmacist to make sure these drugs do not cause any harm when you take them along with other medicines. Never stop taking your medication and never change your dose or frequency without consulting your doctor.

SLIDESHOW

Erectile Dysfunction (ED) Causes and Treatment See Slideshow

WHAT ARE NAMES OF MELANOCORTIN AGONISTS?

Generic and brand names of melanocortin agonists include:

References
https://reference.medscape.com/drugs/melanocortin-agonists

Health Solutions From Our Sponsors