Oxytocin receptor agonist

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Oxytocin, an example of a peptide oxytocin receptor agonist. Oxytocin with labels.png
Oxytocin, an example of a peptide oxytocin receptor agonist.
LIT-001, an example of a small-molecule oxytocin receptor agonist. LIT-001.svg
LIT-001, an example of a small-molecule oxytocin receptor agonist.

An oxytocin receptor agonist is a compound that acts as an agonist of the oxytocin receptor. [1] [2] They include peptides like oxytocin and carbetocin and small-molecules like LIT-001. [1] [2] Peptide oxytocin receptor agonists are used medically to induce labor, promote lactation, and for certain other uses. [3]

Contents

Oxytocin receptor agonists are of theoretical interest for the potential treatment of neuropsychiatric disorders with social symptoms, such as autism, social anxiety, and psychopathy. [1] [2] [4] Small-molecule oxytocin receptor agonists are considered to be more promising for such uses due to better potential pharmacokinetic profiles, such as blood–brain barrier permeability, elimination half-lives, and oral bioavailability. [1] [2]

List of oxytocin receptor agonists

Peptides

Non-peptides

In April 2025, a series of novel and highly potent small-molecule oxytocin receptor agonists with high selectivity over the vasopressin V1A receptor (up to >5,000-fold) were patented and described. [8] [9]

References

  1. 1 2 3 4 Nashar PE, Whitfield AA, Mikusek J, Reekie TA (2022). "The Current Status of Drug Discovery for the Oxytocin Receptor". Oxytocin. Methods Mol Biol. Vol. 2384. pp. 153–174. doi:10.1007/978-1-0716-1759-5_10. ISBN   978-1-0716-1758-8. PMID   34550574. S2CID   239090096.
  2. 1 2 3 4 Gulliver D, Werry E, Reekie TA, Katte TA, Jorgensen W, Kassiou M (January 2019). "Targeting the Oxytocin System: New Pharmacotherapeutic Approaches". Trends Pharmacol Sci. 40 (1): 22–37. doi:10.1016/j.tips.2018.11.001. hdl: 1959.4/unsworks_81554 . PMID   30509888. S2CID   54559394.
  3. ↑ Viero C, Shibuya I, Kitamura N, Verkhratsky A, Fujihara H, Katoh A, Ueta Y, Zingg HH, Chvatal A, Sykova E, Dayanithi G (October 2010). "REVIEW: Oxytocin: Crossing the bridge between basic science and pharmacotherapy". CNS Neurosci Ther. 16 (5): e138–56. doi:10.1111/j.1755-5949.2010.00185.x. PMC   2972642 . PMID   20626426.
  4. ↑ Ferreira-Nascimento S, Freire F, Prata D (2025). "Psychophysiology of facial emotion recognition in psychopathy dimensions and oxytocin's role: A scoping review". PLOS ONE. 20 (7): e0327764. doi: 10.1371/journal.pone.0327764 . PMC   12310049 . PMID   40737230.{{cite journal}}: Check |pmc= value (help)
  5. ↑ Manning M, Stoev S, Chini B, Durroux T, Mouillac B, Guillon G (2008). "Peptide and non-peptide agonists and antagonists for the vasopressin and oxytocin V1a, V1b, V2 and OT receptors: Research tools and potential therapeutic agents☆". Peptide and non-peptide agonists and antagonists for the vasopressin and oxytocin V1a, V1b, V2 and OT receptors: research tools and potential therapeutic agents. Progress in Brain Research. Vol. 170. pp. 473–512. doi:10.1016/S0079-6123(08)00437-8. ISBN   978-0-444-53201-5. PMID   18655903.
  6. ↑ Rahman Z, Resnick L, Rosenzweig-Lipson SJ, Ring RH,"Methods of treatment using oxytocin receptor agonists", US patent application 2007/0117794, published 2007-05-24 , assigned to Wyeth Corp
  7. ↑ Ring RH, Schechter LE, Leonard SK, Dwyer JM, Platt BJ, Graf R, Grauer S, Pulicicchio C, Resnick L, Rahman Z, Sukoff Rizzo SJ, Luo B, Beyer CE, Logue SF, Marquis KL, Hughes ZA, Rosenzweig-Lipson S (January 2010). "Receptor and behavioral pharmacology of WAY-267464, a non-peptide oxytocin receptor agonist". Neuropharmacology. 58 (1): 69–77. doi:10.1016/j.neuropharm.2009.07.016. PMID   19615387. S2CID   8592340.
  8. ↑ Li Y, Liang SH (May 2025). "Novel Nonpeptide as Oxytocin Receptor Agonist". ACS Med Chem Lett. 16 (5): 750–751. doi:10.1021/acsmedchemlett.5c00191. PMC  12067107. PMID   40365388.
  9. ↑ Song Z, Liang SH (May 2025). "Novel Tetrahydrobenzo[b]pyrazolo[3,4-e][1,4]diazepine Compounds as Oxytocin Receptor Agonists for Treating Autism Spectrum Disorders". ACS Med Chem Lett. 16 (5): 752–753. doi:10.1021/acsmedchemlett.5c00190. PMC  12067140. PMID   40365400.


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