DAMGO - CAS 78123-71-4
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
Molecular Weight:
Opioid Receptor
DAMGO is a highly selective peptide agonist of the μ opioid receptor.
Brife Description:
μ opioid receptor
[D-Ala2, NMe-Phe4, Gly-ol5]-enkephalin
Canonical SMILES:
1.Dual effects of DAMGO [D-Ala2,N-Me-Phe4,Gly5-ol]-enkephalin and CTAP (D-Phe-Cys-Tyr-D-Trp-Arg-Thr-Pen-Thr-NH2) on adenylyl cyclase activity: implications for mu-opioid receptor Gs coupling.
Szücs M;Boda K;Gintzler AR J Pharmacol Exp Ther. 2004 Jul;310(1):256-62. Epub 2004 Mar 2.
The mu-opioid receptor (MOR) couples to multiple G proteins, of which coupling to Gs has long been debated. As expected, in opioid naive Chinese hamster ovary cells expressing recombinant MOR, the predominant action of [D-Ala2,N-Me-Phe4,Gly5-ol]-enkephalin (DAMGO) is inhibitory. However, inactivation of Gi/Go proteins via pertussis toxin (PTX) unmasks its ability to facilitate forskolin activation of adenylyl cyclase (AC) activity. Tolerance develops to this effect of DAMGO, which can also be attenuated by cholera toxin (CTX). The latter suggests G mediation. D-Phe-Cys-Tyr-D-Trp-Arg-Thr-Pen-Thr-NH2 (CTAP), previously considered to be a neutral MOR antagonist, also produces a facilitation of forskolin (FSK) activation of AC that is augmented by chronic morphine. Facilitative effects of CTAP in naive as well as its augmentation in tolerant membranes are both substantially reduced by CTX. This suggests that not only Gs mediation but also G(salpha)-linked signaling is critical to the chronic morphine-induced enhanced facilitative action of CTAP. Interestingly, the (augmented) CTAP facilitation of FSK-stimulated AC activity that is observed in opioid tolerant (but not in naive) membranes is also sensitive to PTX.
2.Two delta opioid receptor subtypes are functional in single ventral tegmental area neurons, and can interact with the mu opioid receptor.
Margolis EB;Fujita W;Devi LA;Fields HL Neuropharmacology. 2017 Sep 1;123:420-432. doi: 10.1016/j.neuropharm.2017.06.019. Epub 2017 Jun 21.
The mu and delta opioid receptors (MOR and DOR) are highly homologous members of the opioid family of GPCRs. There is evidence that MOR and DOR interact, however the extent to which these interactions occur in vivo and affect synaptic function is unknown. There are two stable DOR subtypes: DPDPE sensitive (DOR1) and deltorphin II sensitive (DOR2); both agonists are blocked by DOR selective antagonists. Robust motivational effects are produced by local actions of both MOR and DOR ligands in the ventral tegmental area (VTA). Here we demonstrate that a majority of both dopaminergic and non-dopaminergic VTA neurons express combinations of functional DOR1, DOR2, and/or MOR, and that within a single VTA neuron, DOR1, DOR2, and MOR agonists can differentially couple to downstream signaling pathways. As reported for the MOR agonist DAMGO, DPDPE and deltorphin II produced either a predominant K;+; dependent hyperpolarization or a Ca;v;2.1 mediated depolarization in different neurons. In some neurons DPDPE and deltorphin II produced opposite responses. Excitation, inhibition, or no effect by DAMGO did not predict the response to DPDPE or deltorphin II, arguing against a MOR-DOR interaction generating DOR subtypes.
3.The biological consequences of replacing D-Ala in biphalin with amphiphilic α-alkylserines.
Frączak O;Lasota A;Leśniak A;Lipkowski AW;Olma A Chem Biol Drug Des. 2014 Aug;84(2):199-205. doi: 10.1111/cbdd.12305. Epub 2014 Mar 24.
Biphalin, a synthetic opioid peptide with a broad affinity for all opioid receptors (δ, μ, and κ) and high antinociceptive activity, has been under extensive study as a potential analgesic drug. This study presents the synthesis and biological properties of four new analogues of biphalin containing amphiphilic α-alkylserines in position 2 and 2'. The incorporation of bulky α,α-disubstituted amino acids in the peptide chain using standard peptide chemistry is often unsuccessful. We synthesized depsipeptides, and then, the desired peptides were obtained by internal O,N-migration of the acyl residue from the hydroxyl to the amino group under mild basic conditions. The potency and selectivity of the new analogues were evaluated by a competitive receptor-binding assay in the rat brain using [(3)H]DAMGO (a μ ligand) and [(3)H]DELT (a δ ligand). Their binding affinity is strongly dependent on the chirality of α-alkylserine, as analogues containing (R)-α-alkylserines displayed higher μ receptor affinity and selectivity than those incorporating the (S)-isomers.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Opioid Receptor Products

CAS 371980-94-8 SB 612111 hydrochloride

SB 612111 hydrochloride
(CAS: 371980-94-8)

SB 612111 hydrochloride is a selective NOP receptor antagonist (Ki = 0.33, 57.6, 160.5 and 2109 nM for NOP, μ-, κ- and δ-receptors, respectively). SB 612111 exh...

CAS 89352-67-0 ICI 174,864

ICI 174,864
(CAS: 89352-67-0)

ICI 174,864 is a potent and highly selective δ opioid antagonist. It shows partial agonist in vitro activity at δ receptors at high concentrations.

CAS 1355244-02-8 ML 190

ML 190
(CAS: 1355244-02-8)

ML 190 is a κ opioid receptor antagonist with IC50 value of 120 nM.

CAS 170098-38-1 Alvimopan dihydrate

Alvimopan dihydrate
(CAS: 170098-38-1)

Alvimopan dihydrate is a novel, orally available peripherally restricted opioid antagonist with low systemic absorption. It accelerates the gastrointestinal rec...

CAS 34140-59-5 Trimebutine Maleate

Trimebutine Maleate
(CAS: 34140-59-5)

Trimebutine is an opioid receptor agonist used as spasmolytic agent abdominal pain.

CAS 122752-16-3 Deltorphin 2

Deltorphin 2
(CAS: 122752-16-3)

Deltorphin 2, an anion transporting peptid, is a selective peptide agonist for theδ opioid receptor.

CAS 113158-35-3 Nor-Binaltorphimine dihydrochloride

Nor-Binaltorphimine dihydrochloride
(CAS: 113158-35-3)

Nor-Binaltorphimine dihydrochloride is a potent and selective kappa opioid receptor antagonist.

CAS 83397-56-2 PL 017

PL 017
(CAS: 83397-56-2)

PL 017, a morphiceptin analog, is a selective μ opioid receptor agonist (IC50= 5.5 and > 10000 nM for inhibition of 125I-FK 33,824 and 125I-DADLE binding to μ a...

Chemical Structure

CAS 78123-71-4 DAMGO

Quick Inquiry

Verification code

Featured Items