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Dynorphin A (1-10) acetate salt

Names

[ CAS No. ]:
79994-24-4

[ Name ]:
Dynorphin A (1-10) acetate salt

[Synonym ]:
YGGFLRRIRP
dynorphin A fragment 1-10 porcine*sequence
DYNORPHIN A (1-10),PORCINE
DYNORPHIN A (1-10)
dynorphin A,porcine,fragment 1-10
OPIOID AGONIST
H-TYR-GLY-GLY-PHE-LEU-ARG-ARG-ILE-ARG-PRO-OH
TYR-GLY-GLY-PHE-LEU-ARG-ARG-ILE-ARG-PRO

Biological Activity

[Description]:

Dynorphin A (1-10) an endogenous opioid neuropeptide, binds to extracellular loop 2 of the κ-opioid receptor. Dynorphin A (1-10) also blocks NMDA-activated current with an IC50 of 42.0 μM.

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> iGluR
Signaling Pathways >> Neuronal Signaling >> iGluR
Signaling Pathways >> GPCR/G Protein >> Opioid Receptor
Signaling Pathways >> Neuronal Signaling >> Opioid Receptor
Peptides
Research Areas >> Neurological Disease

[Target]

κ-opioid receptor[1] NMDA receptor[2]


[In Vitro]

Dynorphin A (1-10) binds in the transmembrane domain of the κ-receptor[1]. The non-opioid actions of various forms of Dynorphin A (DynA) are examined on N-methyl-D-aspartate (NMDA) receptor channels in isolated rat trigeminal neurons using the whole-cell patch recording technique. All the dynorphins tested blocked NMDA-activated currents. The blocking actions are voltage-independent. The IC50 is 42.0 μM for DynA(1-10). To determine if shorter dynorphins have the similar blocking property, we examined the action of DynA(1-10) at different membrane potentials. DynA(1-10) blocks INMDA to a similar extent as the membrane potentials changed from -80 to +60 mV. Thus, despite a 160-fold difference in the apparent affinities, DynA(1-32) and DynA(1-10) both exert voltage-independent actions on NMDA receptors[2].

[References]

[1]. Paterlini G, et al. Molecular simulation of dynorphin A-(1-10) binding to extracellular loop 2 of the kappa-opioidreceptor. A model for receptor activation. J Med Chem. 1997 Sep 26;40(20):3254-62.

[2]. Chen L, et al. Dynorphin block of N-methyl-D-aspartate channels increases with the peptide length. J Pharmacol Exp Ther. 1998 Mar;284(3):826-31.


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Chemical & Physical Properties

[ Molecular Formula ]:
C57H91N19O12

[ Molecular Weight ]:
1234.45000

[ Exact Mass ]:
1233.71000

[ PSA ]:
522.36000

[ LogP ]:
3.94170

[ Storage condition ]:
2-8℃

MSDS

Click to get detail MSDS

Related Compounds