Deltorphin I TFA

Names

[ CAS No. ]:
122752-15-2

[ Name ]:
Deltorphin I TFA

[Synonym ]:
H-Tyr-D-Ala-Phe-Asp-Val-Val-Gly-NH2
deltorphin I
Deltorphin C
Tyr-D-Ala-Phe-Asp-Val-Val-Cly-NH2

Biological Activity

[Description]:

Deltorphin I is a δ-opioid receptor agonist with high affinity and selectivity.

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Opioid Receptor
Signaling Pathways >> Neuronal Signaling >> Opioid Receptor
Research Areas >> Neurological Disease
Peptides

[Target]

δ-opioid receptor[1]


[In Vivo]

Twice daily administration of Deltorphin I (20μg/mouse) for 4 days produces tolerance to Deltorphin I analgesia, as shown by the decrease in the analgesic response. The peak analgesic response to Deltorphin I (20 μg/mouse) at 10 min after injections is decreased from 8.36±0.28 s (the 1st day) to 4.53±0.14 s (the 4th day) markedly. Concurrent treatment of Melatonin (0.5, 1 and 2.5 mg/kg) and Deltorphin I (20 μg/mouse) twice daily for 4 days can attenuate the tolerance to Deltorphin I analgesia (P<0.05, <0.05 and <0.05), and this effect is dose dependent[1].

[Animal admin]

Mice[1] Male Kunming mice (20.0±1.0 g) are used. In order to investigate the chronic effect of Melatonin on opioid receptor agonist analgesia, 18, 17, 16 and 21 mice are treated with Melatonin (0, 0.5, 1 and 2.5 mg/kg, respectively) twice daily for 4 days. On the 5th day, 8, 8, 8 and 9 mice are administered with Endomorphin-1 18 μg/mouse (corresponding to 0, 0.5, 1 and 2.5 mg/kg Melatonin, respectively), while 10, 9, 8 and 12 mice are administered with Deltorphin I 20 μg/mouse (corresponding to 0, 0.5, 1 and 2.5 mg/kg Melatonin, respectively). Subsequently tail-flick latency is measured at 10 min interval within 60 min[1].

[References]

[1]. Dai X, et al. Melatonin attenuates the development of antinociceptive tolerance to delta-, but not to mu-opioid receptor agonist in mice. Behav Brain Res. 2007 Aug 22;182(1):21-7.


[Related Small Molecules]

PZM-21 | Loperamide hydrochloride | Oliceridine hydrochloride | ADL5859 HCl | JDTic (dihydrochloride) | Naltrindole hydrochloride | LY-2456302 | JTC-801 | Matrine | Met-Enkephalin acetate salt | Cebranopadol | Leu-Enkephalin | DAMGO | Sinomenine HCl | SR17018

Chemical & Physical Properties

[ Density]:
1.284g/cm3

[ Boiling Point ]:
1242.4ºC at 760mmHg

[ Molecular Formula ]:
C37H52N8O10

[ Molecular Weight ]:
768.85600

[ Flash Point ]:
705.2ºC

[ Exact Mass ]:
768.38100

[ PSA ]:
301.24000

[ LogP ]:
2.08280

[ Vapour Pressure ]:
0mmHg at 25°C

[ Index of Refraction ]:
1.578

[ Storage condition ]:
2-8℃

Synthetic Route

Precursor & DownStream


Related Compounds