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Oxytocin acetate
Oxytocin is a positive allosteric modulator of μ opioid receptor (MOR) signaling [1].?
Oxytocin, a 9-amine neuropeptide synthesized in the paraventricular nucleus (PVN) and the supraoptic nucleus of the hypothalamus, is secreted from the posterior pituitary into the systemic circulation, playing an essential role in mammalian labor, lactation, maternal bonding, and social affiliation. Oxytocin has been reported to exert an?analgesic?effect as well [1].?
In hMOR-expressing HEK293 cells, Oxytocin alone showed no direct agonistic effect on human MOR at concentration up to 10-5 M, but treatment with 10-6 M Oxytocin markedly enhanced the MOR signaling stimulated by 10-6 M endomorphin-1, β-endorphin, morphine, fentanyl, as well as DAMGO. Moreover, in the competitive receptor-binding assay, 10-6 M Oxytocin did not alter the affinity of endomorphin-1 or morphine for MOR [1]. ?
Intracerebroventricular Oxytocin administration (0.2 μg) robustly increased medial nucleus accumbens shell (NAcSh) neuron mean firing rate in rats, but did not do so after rats were repeatedly treated with morphine [2].?
References:
[1]. Meguro Y, Miyano K, Hirayama S, et al. Neuropeptide oxytocin enhances μ opioid receptor signaling as a positive allosteric modulator. Journal of Pharmacological Sciences, 2018, 137(1): 67-75.
[2]. Moaddab M, Hyland B I, Brown C H. Oxytocin excites nucleus accumbens shell neurons in vivo. Molecular and Cellular Neuroscience, 2015, 68: 323-330.
- 1. Justin G Meyerowitz, Michael J Robertson, et al. "The oxytocin signaling complex reveals a molecular switch for cation dependence." Nat Struct Mol Biol. 2022 Mar;29(3):274-281. PMID: 35241813
- 2. Lin CH, Tsai CC, et al. "Oxytocin maintains lung histological and functional integrity to confer protection in heat stroke." Sci Rep. 2019 Dec 5;9(1):18390. PMID:31804535
- 3. An X, Sun X, et al. "Protective effect of oxytocin on LPS-induced acute lung injury in mice." Sci Rep. 2019 Feb 26;9(1):2836. PMID:30808956
Storage | Store at -20°C |
M.Wt | 1067.25 |
Cas No. | 6233-83-6 |
Formula | C45H70N12O14S2 |
Synonyms | α-Hypophamine acetate; Oxytocic hormone acetate |
Solubility | ≥182.8 mg/mL in DMSO; ≥14.93 mg/mL in EtOH; ≥44.1 mg/mL in H2O |
Chemical Name | rac-(R)-N-((R)-1-((2-amino-2-oxoethyl)amino)-4-methyl-1-oxopentan-2-yl)-1-((4S,7R,10R,13R,16R,19S)-19-amino-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-13-((R)-sec-butyl)-16-(4-hydroxybenzyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentaazacyclo |
SDF | Download SDF |
Canonical SMILES | O=C([C@H]1N(C([C@H](CSSC[C@@H]2N)NC([C@H](CC(N)=O)NC([C@H](CCC(N)=O)NC([C@H]([C@@H](C)CC)NC([C@H](CC(C=C3)=CC=C3O)NC2=O)=O)=O)=O)=O)=O)CCC1)N[C@H](C(NCC(N)=O)=O)CC(C)C.OC(C)=O |
Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Cell experiment:[1] | |
Cell lines |
Human Embryonic Kidney 293 (HEK293) cells stably expressing human μ opioid receptor (hMOR) |
Reaction Conditions |
10-10 ~ 10-5 M oxytocin |
Applications |
In hMOR-expressing HEK293 cells, oxytocin alone showed no direct agonistic effect on hMOR at concentration up to 10-5 M, but treatment with 10-6 M oxytocin markedly enhanced the MOR signaling stimulated by 10-6 M endomorphin-1, β-endorphin, morphine, fentanyl, as well as DAMGO. Neuropeptide oxytocin could enhance MOR signaling as a positive allosteric modulator. |
Animal experiment:[2] | |
Animal models |
Adult male Wistar rats aged 6 ~ 8 weeks and weighing 250 ~ 300 g |
Dosage form |
0.2 μg Intracerebroventricular administration |
Applications |
Intracerebroventricular oxytocin administration (0.2 μg) robustly increased medial nucleus accumbens shell (NAcSh) neuron mean firing rate in rats, but did not do so after rats were repeatedly treated with morphine. |
Note |
The technical data provided above is for reference only. |
References: 1. Meguro Y, Miyano K, Hirayama S, et al. Neuropeptide oxytocin enhances μ opioid receptor signaling as a positive allosteric modulator. Journal of Pharmacological Sciences, 2018, 137(1): 67-75. 2. Moaddab M, Hyland B I, Brown C H. Oxytocin excites nucleus accumbens shell neurons in vivo. Molecular and Cellular Neuroscience, 2015, 68: 323-330. |
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