dynorphin a (1-11)-amide profile

ID Source	ID
PubMed CID	10677974
CHEMBL ID	216640
MeSH ID	M0288950

Synonym
h-tyr-gly-gly-phe-leu-arg-lys-ile-lys-pro-lys-leu-lys-trp-asp-asn-gln-oh
bdbm50033143
CHEMBL216640 ,
htyr-gly-gly-phe-leu-arg-arg-lle-arg-pro-lysnh2
tyr-gly-gly-phe-leu-arg-arg-ile-arg-pro-d-lys-nh2
h-tyr-gly-gly-phe-leu-arg-arg-ile-arg-pro-lys-nh2
bdbm50010704
dyn a(1-11)-nh2
79985-48-1
dynorphin a (1-11) amide
dynorphin a(1-11)amide
PD086271

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Delta-type opioid receptor	Mus musculus (house mouse)	Ki	0.0071	0.0000	0.5393	9.4000	AID149069; AID149080; AID149081; AID431804; AID439354
Delta-type opioid receptor	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.0255	0.0003	0.3887	7.0000	AID149624
Mu-type opioid receptor	Rattus norvegicus (Norway rat)	Ki	0.0019	0.0000	0.3845	8.6000	AID151617; AID431803; AID439353
Kappa-type opioid receptor	Rattus norvegicus (Norway rat)	Ki	0.0004	0.0000	0.1868	3.9500	AID148569; AID431802; AID439352
Mu-type opioid receptor	Homo sapiens (human)	Ki	0.0063	0.0000	0.4197	10.0000	AID150975; AID150979; AID1714329
Delta-type opioid receptor	Homo sapiens (human)	IC50 (µMol)	0.0177	0.0002	0.7521	8.0140	AID149624; AID149740
Delta-type opioid receptor	Homo sapiens (human)	Ki	0.0031	0.0000	0.5978	9.9300	AID148239; AID149069; AID1714330
Kappa-type opioid receptor	Cavia porcellus (domestic guinea pig)	IC50 (µMol)	0.0006	0.0003	0.7123	7.0700	AID148559
Kappa-type opioid receptor	Cavia porcellus (domestic guinea pig)	Ki	0.0001	0.0000	0.2018	6.4240	AID149267
Kappa-type opioid receptor	Homo sapiens (human)	IC50 (µMol)	0.0002	0.0000	1.2011	10.0000	AID1714328
Kappa-type opioid receptor	Homo sapiens (human)	Ki	0.0001	0.0000	0.3624	10.0000	AID148006; AID148010; AID1714328
D(1A) dopamine receptor	Sus scrofa (pig)	Ki	0.0019	0.0005	1.2223	8.8000	AID439353
Mu-type opioid receptor	Cavia porcellus (domestic guinea pig)	IC50 (µMol)	0.0099	0.0002	0.6603	10.0000	AID138853; AID149740
Mu-type opioid receptor	Cavia porcellus (domestic guinea pig)	Ki	0.0007	0.0000	0.2786	9.0000	AID152227
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Kappa-type opioid receptor	Rattus norvegicus (Norway rat)	EC50 (µMol)	0.0004	0.0004	0.0039	0.0180	AID431807
Kappa-type opioid receptor	Homo sapiens (human)	EC50 (µMol)	0.0007	0.0000	0.2244	8.9900	AID149989; AID149993
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	Mu-type opioid receptor	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathway	Mu-type opioid receptor	Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway	Mu-type opioid receptor	Homo sapiens (human)
sensory perception	Mu-type opioid receptor	Homo sapiens (human)
negative regulation of cell population proliferation	Mu-type opioid receptor	Homo sapiens (human)
sensory perception of pain	Mu-type opioid receptor	Homo sapiens (human)
G protein-coupled opioid receptor signaling pathway	Mu-type opioid receptor	Homo sapiens (human)
behavioral response to ethanol	Mu-type opioid receptor	Homo sapiens (human)
positive regulation of neurogenesis	Mu-type opioid receptor	Homo sapiens (human)
negative regulation of Wnt protein secretion	Mu-type opioid receptor	Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascade	Mu-type opioid receptor	Homo sapiens (human)
calcium ion transmembrane transport	Mu-type opioid receptor	Homo sapiens (human)
cellular response to morphine	Mu-type opioid receptor	Homo sapiens (human)
regulation of cellular response to stress	Mu-type opioid receptor	Homo sapiens (human)
regulation of NMDA receptor activity	Mu-type opioid receptor	Homo sapiens (human)
neuropeptide signaling pathway	Mu-type opioid receptor	Homo sapiens (human)
immune response	Delta-type opioid receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Delta-type opioid receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	Delta-type opioid receptor	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	Delta-type opioid receptor	Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway	Delta-type opioid receptor	Homo sapiens (human)
adult locomotory behavior	Delta-type opioid receptor	Homo sapiens (human)
negative regulation of gene expression	Delta-type opioid receptor	Homo sapiens (human)
negative regulation of protein-containing complex assembly	Delta-type opioid receptor	Homo sapiens (human)
positive regulation of CREB transcription factor activity	Delta-type opioid receptor	Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylation	Delta-type opioid receptor	Homo sapiens (human)
response to nicotine	Delta-type opioid receptor	Homo sapiens (human)
G protein-coupled opioid receptor signaling pathway	Delta-type opioid receptor	Homo sapiens (human)
eating behavior	Delta-type opioid receptor	Homo sapiens (human)
regulation of mitochondrial membrane potential	Delta-type opioid receptor	Homo sapiens (human)
regulation of calcium ion transport	Delta-type opioid receptor	Homo sapiens (human)
cellular response to growth factor stimulus	Delta-type opioid receptor	Homo sapiens (human)
cellular response to hypoxia	Delta-type opioid receptor	Homo sapiens (human)
cellular response to toxic substance	Delta-type opioid receptor	Homo sapiens (human)
neuropeptide signaling pathway	Delta-type opioid receptor	Homo sapiens (human)
immune response	Kappa-type opioid receptor	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	Kappa-type opioid receptor	Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway	Kappa-type opioid receptor	Homo sapiens (human)
chemical synaptic transmission	Kappa-type opioid receptor	Homo sapiens (human)
sensory perception	Kappa-type opioid receptor	Homo sapiens (human)
locomotory behavior	Kappa-type opioid receptor	Homo sapiens (human)
sensory perception of pain	Kappa-type opioid receptor	Homo sapiens (human)
adenylate cyclase-inhibiting opioid receptor signaling pathway	Kappa-type opioid receptor	Homo sapiens (human)
response to insulin	Kappa-type opioid receptor	Homo sapiens (human)
positive regulation of dopamine secretion	Kappa-type opioid receptor	Homo sapiens (human)
negative regulation of luteinizing hormone secretion	Kappa-type opioid receptor	Homo sapiens (human)
response to nicotine	Kappa-type opioid receptor	Homo sapiens (human)
G protein-coupled opioid receptor signaling pathway	Kappa-type opioid receptor	Homo sapiens (human)
maternal behavior	Kappa-type opioid receptor	Homo sapiens (human)
eating behavior	Kappa-type opioid receptor	Homo sapiens (human)
response to estrogen	Kappa-type opioid receptor	Homo sapiens (human)
estrous cycle	Kappa-type opioid receptor	Homo sapiens (human)
response to ethanol	Kappa-type opioid receptor	Homo sapiens (human)
regulation of saliva secretion	Kappa-type opioid receptor	Homo sapiens (human)
behavioral response to cocaine	Kappa-type opioid receptor	Homo sapiens (human)
sensory perception of temperature stimulus	Kappa-type opioid receptor	Homo sapiens (human)
defense response to virus	Kappa-type opioid receptor	Homo sapiens (human)
cellular response to lipopolysaccharide	Kappa-type opioid receptor	Homo sapiens (human)
cellular response to glucose stimulus	Kappa-type opioid receptor	Homo sapiens (human)
positive regulation of p38MAPK cascade	Kappa-type opioid receptor	Homo sapiens (human)
positive regulation of potassium ion transmembrane transport	Kappa-type opioid receptor	Homo sapiens (human)
response to acrylamide	Kappa-type opioid receptor	Homo sapiens (human)
positive regulation of eating behavior	Kappa-type opioid receptor	Homo sapiens (human)
conditioned place preference	Kappa-type opioid receptor	Homo sapiens (human)
neuropeptide signaling pathway	Kappa-type opioid receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
G-protein alpha-subunit binding	Mu-type opioid receptor	Homo sapiens (human)
G protein-coupled receptor activity	Mu-type opioid receptor	Homo sapiens (human)
beta-endorphin receptor activity	Mu-type opioid receptor	Homo sapiens (human)
voltage-gated calcium channel activity	Mu-type opioid receptor	Homo sapiens (human)
protein binding	Mu-type opioid receptor	Homo sapiens (human)
morphine receptor activity	Mu-type opioid receptor	Homo sapiens (human)
G-protein beta-subunit binding	Mu-type opioid receptor	Homo sapiens (human)
neuropeptide binding	Mu-type opioid receptor	Homo sapiens (human)
G protein-coupled opioid receptor activity	Delta-type opioid receptor	Homo sapiens (human)
protein binding	Delta-type opioid receptor	Homo sapiens (human)
receptor serine/threonine kinase binding	Delta-type opioid receptor	Homo sapiens (human)
G protein-coupled enkephalin receptor activity	Delta-type opioid receptor	Homo sapiens (human)
neuropeptide binding	Delta-type opioid receptor	Homo sapiens (human)
G protein-coupled opioid receptor activity	Kappa-type opioid receptor	Homo sapiens (human)
protein binding	Kappa-type opioid receptor	Homo sapiens (human)
receptor serine/threonine kinase binding	Kappa-type opioid receptor	Homo sapiens (human)
dynorphin receptor activity	Kappa-type opioid receptor	Homo sapiens (human)
neuropeptide binding	Kappa-type opioid receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
endosome	Mu-type opioid receptor	Homo sapiens (human)
endoplasmic reticulum	Mu-type opioid receptor	Homo sapiens (human)
Golgi apparatus	Mu-type opioid receptor	Homo sapiens (human)
plasma membrane	Mu-type opioid receptor	Homo sapiens (human)
axon	Mu-type opioid receptor	Homo sapiens (human)
dendrite	Mu-type opioid receptor	Homo sapiens (human)
perikaryon	Mu-type opioid receptor	Homo sapiens (human)
synapse	Mu-type opioid receptor	Homo sapiens (human)
plasma membrane	Mu-type opioid receptor	Homo sapiens (human)
neuron projection	Mu-type opioid receptor	Homo sapiens (human)
plasma membrane	Delta-type opioid receptor	Homo sapiens (human)
synaptic vesicle membrane	Delta-type opioid receptor	Homo sapiens (human)
dendrite membrane	Delta-type opioid receptor	Homo sapiens (human)
presynaptic membrane	Delta-type opioid receptor	Homo sapiens (human)
axon terminus	Delta-type opioid receptor	Homo sapiens (human)
spine apparatus	Delta-type opioid receptor	Homo sapiens (human)
postsynaptic density membrane	Delta-type opioid receptor	Homo sapiens (human)
neuronal dense core vesicle	Delta-type opioid receptor	Homo sapiens (human)
plasma membrane	Delta-type opioid receptor	Homo sapiens (human)
neuron projection	Delta-type opioid receptor	Homo sapiens (human)
nucleoplasm	Kappa-type opioid receptor	Homo sapiens (human)
mitochondrion	Kappa-type opioid receptor	Homo sapiens (human)
cytosol	Kappa-type opioid receptor	Homo sapiens (human)
plasma membrane	Kappa-type opioid receptor	Homo sapiens (human)
membrane	Kappa-type opioid receptor	Homo sapiens (human)
sarcoplasmic reticulum	Kappa-type opioid receptor	Homo sapiens (human)
T-tubule	Kappa-type opioid receptor	Homo sapiens (human)
dendrite	Kappa-type opioid receptor	Homo sapiens (human)
synaptic vesicle membrane	Kappa-type opioid receptor	Homo sapiens (human)
presynaptic membrane	Kappa-type opioid receptor	Homo sapiens (human)
perikaryon	Kappa-type opioid receptor	Homo sapiens (human)
axon terminus	Kappa-type opioid receptor	Homo sapiens (human)
postsynaptic membrane	Kappa-type opioid receptor	Homo sapiens (human)
plasma membrane	Kappa-type opioid receptor	Homo sapiens (human)
neuron projection	Kappa-type opioid receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (84)

Assay ID	Title	Year	Journal	Article
AID78860	Binding affinity against smooth muscle tissue of Guinea pig ileum	1995	Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18	Synthesis using a Fmoc-based strategy and biological activities of some reduced peptide bond pseudopeptide analogues of dynorphin A1.
AID152227	Binding affinity was measured on mu opioid receptor	2001	Journal of medicinal chemistry, Sep-13, Volume: 44, Issue:19	[2',6'-Dimethyltyrosine]dynorphin A(1-11)-NH2 analogues lacking an N-terminal amino group: potent and selective kappa opioid antagonists.
AID150248	Opioid receptors antagonist activity in smooth-muscle tissue mouse vas deferens (MVD) in presence of CTAP	1990	Journal of medicinal chemistry, Jul, Volume: 33, Issue:7	Design and synthesis of highly potent and selective cyclic dynorphin A analogues.
AID439354	Displacement of [3H]DPDPE from mouse delta opioid receptor expressed in CHO cells	2009	Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21	The effects of C-terminal modifications on the opioid activity of [N-benzylTyr(1)]dynorphin A-(1-11) analogues.
AID231479	Ratio between IC50 of GPI and GPB	1996	Journal of medicinal chemistry, Jun-21, Volume: 39, Issue:13	Effects of modifications of residues in position 3 of dynorphin A(1-11)-NH2 on kappa receptor selectivity and potency.
AID149989	Effective concentration for half-maximal stimulation was determined by [35S]GTP-gamma-S, assay	2003	Journal of medicinal chemistry, May-22, Volume: 46, Issue:11	Structure-activity relationships of dynorphin a analogues modified in the address sequence.
AID148006	In vitro binding affinity towards human Opioid receptor kappa 1 on CHO cell membranes using [3H]diprenorphine displacement.	2003	Journal of medicinal chemistry, May-22, Volume: 46, Issue:11	Structure-activity relationships of dynorphin a analogues modified in the address sequence.
AID78867	Evaluated for its ability to inhibit the electrically evoked contraction of the guinea pig ileum(GPI).	1996	Journal of medicinal chemistry, Jun-21, Volume: 39, Issue:13	Effects of modifications of residues in position 3 of dynorphin A(1-11)-NH2 on kappa receptor selectivity and potency.
AID148239	Binding affinity towards cloned human Opioid receptor delta 1 in CHO cell membranes.	2000	Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14	[Pro(3)]Dyn A(1-11)-NH(2): a dynorphin analogue with high selectivity for the kappa opioid receptor.
AID149624	Binding affinity at delta opioid receptor in guinea pig brain by [3H]c[D-Pen2, p-Cl-Phe4, D-Pen5]-enkephalin displacement.	1994	Journal of medicinal chemistry, Nov-11, Volume: 37, Issue:23	Design, synthesis, and biological properties of highly potent cyclic dynorphin A analogues. Analogues cyclized between positions 5 and 11.
AID431808	Agonist activity at rat cloned kappa opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by scintillation counting relative to Dyn A-(1-13)NH2	2009	Journal of medicinal chemistry, Sep-24, Volume: 52, Issue:18	Design, synthesis, and pharmacological activities of dynorphin A analogues cyclized by ring-closing metathesis.
AID439352	Displacement of [3H]diprenorphine from rat kappa opioid receptor expressed in CHO cells	2009	Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21	The effects of C-terminal modifications on the opioid activity of [N-benzylTyr(1)]dynorphin A-(1-11) analogues.
AID148554	Binding affinity against Opioid receptor kappa 1 in guinea pig brain homogenate using [3H]- U-69593 as radioligand	1990	Journal of medicinal chemistry, Jul, Volume: 33, Issue:7	Design and synthesis of highly potent and selective cyclic dynorphin A analogues.
AID149746	Inhibition of binding [3H]DAMGO at Opioid receptor mu 1 of guinea pig brain membrane (GPB) homogenates.	1996	Journal of medicinal chemistry, Jun-21, Volume: 39, Issue:13	Effects of modifications of residues in position 3 of dynorphin A(1-11)-NH2 on kappa receptor selectivity and potency.
AID1714334	Toxicity in mouse HN9.10 cells expressing human KOR assessed as cell viability at 1 mM after 24 hrs by XTT assay	2016	Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22	Structure-Activity Relationships of [des-Arg
AID150249	Opioid receptors antagonist activity in smooth-muscle tissue mouse vas deferens (MVD) in presence of ICI	1990	Journal of medicinal chemistry, Jul, Volume: 33, Issue:7	Design and synthesis of highly potent and selective cyclic dynorphin A analogues.
AID1714328	Displacement of [3H]U69,593 from human KOR expressed in mouse HN9.10 cell membranes incubated for 2 hrs by liquid scintillation counting based radioligand competition assay	2016	Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22	Structure-Activity Relationships of [des-Arg
AID228314	Compound was evaluated for opioid receptor selectivity, expressed as Ki ratio (kappa/mu/delta); 1/14/44	2004	Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2	Synthesis and opioid activity of side-chain-to-side-chain cyclic dynorphin A-(1-11) amide analogues cyclized between positions 2 and 5. 1. Substitutions in position 3.
AID149740	Inhibition of [3H]DAMGO binding to Opioid receptor mu 1 of guinea pig brain membrane homogenates	1996	Journal of medicinal chemistry, Mar-01, Volume: 39, Issue:5	Design, synthesis, and biological activities of cyclic lactam peptide analogues of dynorphine A(1-11)-NH2.
AID149732	Binding affinity against Opioid receptor mu 1 in guinea pig brain homogenate using [3H]- PL-17 as radioligand	1990	Journal of medicinal chemistry, Jul, Volume: 33, Issue:7	Design and synthesis of highly potent and selective cyclic dynorphin A analogues.
AID239268	Inhibition of [3H]diprenorphine binding to kappa opioid receptor expressed in CHO cells	2005	Journal of medicinal chemistry, Jul-14, Volume: 48, Issue:14	[Nalpha-benzylTyr1,cyclo(D-Asp5,Dap8)]- dynorphin A-(1-11)NH2 cyclized in the "address" domain is a novel kappa-opioid receptor antagonist.
AID152409	Opioid receptors antagonist activity in smooth-muscle tissue of guinea pig ileum (GPI) in presence of CTAP	1990	Journal of medicinal chemistry, Jul, Volume: 33, Issue:7	Design and synthesis of highly potent and selective cyclic dynorphin A analogues.
AID232456	Selectivity ratio between delta and kappa opioid receptor from guinea pig brain homogenate	1996	Journal of medicinal chemistry, Jun-21, Volume: 39, Issue:13	Effects of modifications of residues in position 3 of dynorphin A(1-11)-NH2 on kappa receptor selectivity and potency.
AID439353	Displacement of [3H]DAMGO from rat mu opioid receptor expressed in CHO cells	2009	Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21	The effects of C-terminal modifications on the opioid activity of [N-benzylTyr(1)]dynorphin A-(1-11) analogues.
AID149731	Binding affinity against Opioid receptor mu 1 from Guinea pig brain homogenate using [3H]DAMGO	1995	Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18	Synthesis using a Fmoc-based strategy and biological activities of some reduced peptide bond pseudopeptide analogues of dynorphin A1.
AID151617	Binding affinity towards Opioid receptor mu 1 expressed in CHO cells was determined by using[3H]DAMGO as radioligand	2004	Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2	Synthesis and opioid activity of side-chain-to-side-chain cyclic dynorphin A-(1-11) amide analogues cyclized between positions 2 and 5. 1. Substitutions in position 3.
AID239551	Inhibition of [3H]-DPDPE (cyclo[D-Pen2,D-Pen5]enkep halin) binding to delta opioid receptor expressed in CHO cells	2005	Journal of medicinal chemistry, Jul-14, Volume: 48, Issue:14	[Nalpha-benzylTyr1,cyclo(D-Asp5,Dap8)]- dynorphin A-(1-11)NH2 cyclized in the "address" domain is a novel kappa-opioid receptor antagonist.
AID1714333	Half life in rat plasma by RP-HPLC analysis	2016	Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22	Structure-Activity Relationships of [des-Arg
AID1714330	Displacement of [3H]deltorphin-II from human DOR expressed in CHO cell membranes incubated for 2 hrs by liquid scintillation counting based radioligand competition assay	2016	Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22	Structure-Activity Relationships of [des-Arg
AID149993	Human kOpioid receptor kappa 1 mediated stimulation of [35S]- GTPgammaS binding in CHO cells (Agonist potency).	2000	Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14	[Pro(3)]Dyn A(1-11)-NH(2): a dynorphin analogue with high selectivity for the kappa opioid receptor.
AID148010	Binding affinity towards cloned human Opioid receptor kappa 1 in CHO cell membranes.	2000	Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14	[Pro(3)]Dyn A(1-11)-NH(2): a dynorphin analogue with high selectivity for the kappa opioid receptor.
AID431805	Selectivity ratio of Ki for rat kappa opioid receptor to Ki for rat mu opioid receptor	2009	Journal of medicinal chemistry, Sep-24, Volume: 52, Issue:18	Design, synthesis, and pharmacological activities of dynorphin A analogues cyclized by ring-closing metathesis.
AID228936	Tested for maximum agonist response at concentration 10 uM, relative to that with standard agonist U50,488.	2000	Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14	[Pro(3)]Dyn A(1-11)-NH(2): a dynorphin analogue with high selectivity for the kappa opioid receptor.
AID148152	Agonist activity towards human Opioid receptor kappa 1 mediated [35S]GTP-gamma-S, binding at 10 uM	2003	Journal of medicinal chemistry, May-22, Volume: 46, Issue:11	Structure-activity relationships of dynorphin a analogues modified in the address sequence.
AID234291	Selectivity as ratio of IC50 for delta and mu opioid receptors	1995	Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18	Synthesis using a Fmoc-based strategy and biological activities of some reduced peptide bond pseudopeptide analogues of dynorphin A1.
AID150250	Opioid receptors antagonist activity in smooth-muscle tissue mouse vas deferens (MVD) in presence of NLX	1990	Journal of medicinal chemistry, Jul, Volume: 33, Issue:7	Design and synthesis of highly potent and selective cyclic dynorphin A analogues.
AID149080	Binding affinity towards opioid receptor delta 1 expressed in CHO cells was determined by using [3H]DPDPE as radioligand	2004	Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2	Synthesis and opioid activity of side-chain-to-side-chain cyclic dynorphin A-(1-11) amide analogues cyclized between positions 2 and 5. 1. Substitutions in position 3.
AID228161	Binding affinity towards human kappa,mu,delta receptors was calculated as the ratio; 1/95/54	2003	Journal of medicinal chemistry, May-22, Volume: 46, Issue:11	Structure-activity relationships of dynorphin a analogues modified in the address sequence.
AID76213	Inhibitory concentration of compound was measured in guinea pig ileum(GPI) assay	2001	Journal of medicinal chemistry, Sep-13, Volume: 44, Issue:19	[2',6'-Dimethyltyrosine]dynorphin A(1-11)-NH2 analogues lacking an N-terminal amino group: potent and selective kappa opioid antagonists.
AID431804	Displacement of [3H]DPDPE from mouse delta opioid receptor expressed in CHO cells	2009	Journal of medicinal chemistry, Sep-24, Volume: 52, Issue:18	Design, synthesis, and pharmacological activities of dynorphin A analogues cyclized by ring-closing metathesis.
AID150979	Binding affinity towards cloned human Opioid receptor mu 1 in CHO cell membranes.	2000	Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14	[Pro(3)]Dyn A(1-11)-NH(2): a dynorphin analogue with high selectivity for the kappa opioid receptor.
AID234292	Selectivity as ratio of IC50 for mu and kappa opioid receptors	1995	Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18	Synthesis using a Fmoc-based strategy and biological activities of some reduced peptide bond pseudopeptide analogues of dynorphin A1.
AID229312	Ratio of IC50 for central and peripheral kappa opioid receptor binding in giunea pig	1995	Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18	Synthesis using a Fmoc-based strategy and biological activities of some reduced peptide bond pseudopeptide analogues of dynorphin A1.
AID234969	Relative binding to delta and kappa opioid receptors (ratio of IC50)	1996	Journal of medicinal chemistry, Mar-01, Volume: 39, Issue:5	Design, synthesis, and biological activities of cyclic lactam peptide analogues of dynorphine A(1-11)-NH2.
AID149267	Binding affinity was measured on opioid receptor kappa 1	2001	Journal of medicinal chemistry, Sep-13, Volume: 44, Issue:19	[2',6'-Dimethyltyrosine]dynorphin A(1-11)-NH2 analogues lacking an N-terminal amino group: potent and selective kappa opioid antagonists.
AID149631	Compound was tested for the inhibition of binding of [3H]c[D-Pen2,p-Cl-Phe4,D-Pen5]enkephalin to Opioid receptor delta 1 in plasma membrane homogenates of the guinea pig brain	1996	Journal of medicinal chemistry, Mar-01, Volume: 39, Issue:5	Design, synthesis, and biological activities of cyclic lactam peptide analogues of dynorphine A(1-11)-NH2.
AID231670	Central (GPB) and Peripheral (GPI) Nervous Systems Selectivity at kappa Opioid Receptor	1996	Journal of medicinal chemistry, Mar-01, Volume: 39, Issue:5	Design, synthesis, and biological activities of cyclic lactam peptide analogues of dynorphine A(1-11)-NH2.
AID234970	Relative binding to mu and kappa opioid receptors (ratio of IC50)	1996	Journal of medicinal chemistry, Mar-01, Volume: 39, Issue:5	Design, synthesis, and biological activities of cyclic lactam peptide analogues of dynorphine A(1-11)-NH2.
AID231737	Ratio between mouse vas deferens and guinea pig ileum	2001	Journal of medicinal chemistry, Sep-13, Volume: 44, Issue:19	[2',6'-Dimethyltyrosine]dynorphin A(1-11)-NH2 analogues lacking an N-terminal amino group: potent and selective kappa opioid antagonists.
AID138853	Binding affinity at mu opioid receptor in guinea pig brain by [3H]DAMGO displacement.	1994	Journal of medicinal chemistry, Nov-11, Volume: 37, Issue:23	Design, synthesis, and biological properties of highly potent cyclic dynorphin A analogues. Analogues cyclized between positions 5 and 11.
AID75890	Ability to inhibit the electrically evoked contraction of the guinea pig ileum	1996	Journal of medicinal chemistry, Mar-01, Volume: 39, Issue:5	Design, synthesis, and biological activities of cyclic lactam peptide analogues of dynorphine A(1-11)-NH2.
AID1714329	Displacement of [3H]diprenorphine from human MOR expressed in mouse NG108-15 cell membranes incubated for 2 hrs by liquid scintillation counting based radioligand competition assay	2016	Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22	Structure-Activity Relationships of [des-Arg
AID431802	Displacement of [3H]Diprenorphine from rat kappa opioid receptor expressed in CHO cells	2009	Journal of medicinal chemistry, Sep-24, Volume: 52, Issue:18	Design, synthesis, and pharmacological activities of dynorphin A analogues cyclized by ring-closing metathesis.
AID232460	Selectivity ratio between mu and kappa opioid receptor from guinea pig brain homogenate	1996	Journal of medicinal chemistry, Jun-21, Volume: 39, Issue:13	Effects of modifications of residues in position 3 of dynorphin A(1-11)-NH2 on kappa receptor selectivity and potency.
AID150975	In vitro binding affinity to human Opioid receptor mu 1 on CHO cell membranes using [3H]diprenorphine displacement.	2003	Journal of medicinal chemistry, May-22, Volume: 46, Issue:11	Structure-activity relationships of dynorphin a analogues modified in the address sequence.
AID223364	Tested for antagonist activity in guinea pig ileum by (GPI) assay.	2000	Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14	[Pro(3)]Dyn A(1-11)-NH(2): a dynorphin analogue with high selectivity for the kappa opioid receptor.
AID431807	Agonist activity at rat cloned kappa opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by scintillation counting	2009	Journal of medicinal chemistry, Sep-24, Volume: 52, Issue:18	Design, synthesis, and pharmacological activities of dynorphin A analogues cyclized by ring-closing metathesis.
AID149069	In vitro binding affinity to human Opioid receptor delta 1 on CHO cell membranes using [3H]diprenorphine displacement.	2003	Journal of medicinal chemistry, May-22, Volume: 46, Issue:11	Structure-activity relationships of dynorphin a analogues modified in the address sequence.
AID148677	Inhibition of [3H]U-69593 binding to Opioid receptor kappa 1 of plasma membrane homogenates of guinea pig brain	1996	Journal of medicinal chemistry, Mar-01, Volume: 39, Issue:5	Design, synthesis, and biological activities of cyclic lactam peptide analogues of dynorphine A(1-11)-NH2.
AID239536	Inhibition of [3H]DAMGO ([D-Ala2,NMePhe4,glyol]-enkephalin) binding to mu opioid receptor expressed in CHO cells	2005	Journal of medicinal chemistry, Jul-14, Volume: 48, Issue:14	[Nalpha-benzylTyr1,cyclo(D-Asp5,Dap8)]- dynorphin A-(1-11)NH2 cyclized in the "address" domain is a novel kappa-opioid receptor antagonist.
AID439355	Selectivity ratio of Ki for rat kappa opioid receptor to Ki for rat mu opioid receptor	2009	Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21	The effects of C-terminal modifications on the opioid activity of [N-benzylTyr(1)]dynorphin A-(1-11) analogues.
AID232185	Ratio of guinea pig brain Vs peripheral guinea pig ileum selectivies at kappa and mu opioid receptor	1990	Journal of medicinal chemistry, Jul, Volume: 33, Issue:7	Design and synthesis of highly potent and selective cyclic dynorphin A analogues.
AID231674	Ratio between Kappa receptor, Mu receptor and Delta receptor; 1/8/155	2001	Journal of medicinal chemistry, Sep-13, Volume: 44, Issue:19	[2',6'-Dimethyltyrosine]dynorphin A(1-11)-NH2 analogues lacking an N-terminal amino group: potent and selective kappa opioid antagonists.
AID150247	Opioid receptors antagonist activity in smooth-muscle tissue mouse vas deferens (MVD)	1990	Journal of medicinal chemistry, Jul, Volume: 33, Issue:7	Design and synthesis of highly potent and selective cyclic dynorphin A analogues.
AID149620	Binding affinity against delta opioid receptor of Guinea pig brain homogenate using [3H]c[D-Pen2,p-Cl-Phe4,D-Pen5]enkephalin	1995	Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18	Synthesis using a Fmoc-based strategy and biological activities of some reduced peptide bond pseudopeptide analogues of dynorphin A1.
AID152408	Opioid receptors antagonist activity in smooth-muscle tissue of guinea pig ileum (GPI)	1990	Journal of medicinal chemistry, Jul, Volume: 33, Issue:7	Design and synthesis of highly potent and selective cyclic dynorphin A analogues.
AID439356	Selectivity ratio of Ki for rat kappa opioid receptor to Ki for mouse delta opioid receptor	2009	Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21	The effects of C-terminal modifications on the opioid activity of [N-benzylTyr(1)]dynorphin A-(1-11) analogues.
AID149081	Binding affinity was measured on delta opioid receptor	2001	Journal of medicinal chemistry, Sep-13, Volume: 44, Issue:19	[2',6'-Dimethyltyrosine]dynorphin A(1-11)-NH2 analogues lacking an N-terminal amino group: potent and selective kappa opioid antagonists.
AID132829	Inhibitory concentration of compound was measured in mouse vas deferens assay	2001	Journal of medicinal chemistry, Sep-13, Volume: 44, Issue:19	[2',6'-Dimethyltyrosine]dynorphin A(1-11)-NH2 analogues lacking an N-terminal amino group: potent and selective kappa opioid antagonists.
AID431803	Displacement of [3H]DAMGO from rat mu opioid receptor expressed in CHO cells	2009	Journal of medicinal chemistry, Sep-24, Volume: 52, Issue:18	Design, synthesis, and pharmacological activities of dynorphin A analogues cyclized by ring-closing metathesis.
AID243018	Relative binding affinity for kappa and delta opioid receptors	2005	Journal of medicinal chemistry, Jul-14, Volume: 48, Issue:14	[Nalpha-benzylTyr1,cyclo(D-Asp5,Dap8)]- dynorphin A-(1-11)NH2 cyclized in the "address" domain is a novel kappa-opioid receptor antagonist.
AID148559	Binding affinity at kappa opioid receptor in guinea pig brain by [3H]U-69593 displacement.	1994	Journal of medicinal chemistry, Nov-11, Volume: 37, Issue:23	Design, synthesis, and biological properties of highly potent cyclic dynorphin A analogues. Analogues cyclized between positions 5 and 11.
AID234293	Selectivity ratio for Mu and Kappa opioid receptors.	1994	Journal of medicinal chemistry, Nov-11, Volume: 37, Issue:23	Design, synthesis, and biological properties of highly potent cyclic dynorphin A analogues. Analogues cyclized between positions 5 and 11.
AID148553	Binding affinity against Opioid receptor kappa 1 of Guinea pig brain homogenate using [3H]U-69593	1995	Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18	Synthesis using a Fmoc-based strategy and biological activities of some reduced peptide bond pseudopeptide analogues of dynorphin A1.
AID231540	Ratio of binding affinity towards kappa, mu and delta opioid receptor; 1/103/39	2000	Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14	[Pro(3)]Dyn A(1-11)-NH(2): a dynorphin analogue with high selectivity for the kappa opioid receptor.
AID150232	Opioid receptors antagonist activity in smooth-muscle tissue of guinea pig ileum (GPI) in presence of NLX	1990	Journal of medicinal chemistry, Jul, Volume: 33, Issue:7	Design and synthesis of highly potent and selective cyclic dynorphin A analogues.
AID149619	Binding affinity against Opioid receptor delta 1 in guinea pig brain homogenate using [3H]- DPDPE as radioligand	1990	Journal of medicinal chemistry, Jul, Volume: 33, Issue:7	Design and synthesis of highly potent and selective cyclic dynorphin A analogues.
AID243009	Relative binding affinity for kappa and mu opioid receptors	2005	Journal of medicinal chemistry, Jul-14, Volume: 48, Issue:14	[Nalpha-benzylTyr1,cyclo(D-Asp5,Dap8)]- dynorphin A-(1-11)NH2 cyclized in the "address" domain is a novel kappa-opioid receptor antagonist.
AID148682	Inhibition of binding [3H]U-69539 at Opioid receptor kappa 1 of guinea pig brain membrane (GPB) homogenates.	1996	Journal of medicinal chemistry, Jun-21, Volume: 39, Issue:13	Effects of modifications of residues in position 3 of dynorphin A(1-11)-NH2 on kappa receptor selectivity and potency.
AID148569	Binding affinity towards Opioid receptor kappa 1 expressed in CHO cells was determined by using [3H]diprenorphine as radioligand	2004	Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2	Synthesis and opioid activity of side-chain-to-side-chain cyclic dynorphin A-(1-11) amide analogues cyclized between positions 2 and 5. 1. Substitutions in position 3.
AID149618	Agonistic activity towards Opioid receptor delta 1 was determined by evaluating the inhibitory activity towards electrically stimulated mouse vas deferens	1996	Journal of medicinal chemistry, Jun-21, Volume: 39, Issue:13	Effects of modifications of residues in position 3 of dynorphin A(1-11)-NH2 on kappa receptor selectivity and potency.
AID234294	Selectivity ratio for delta and kappa opioid receptors.	1994	Journal of medicinal chemistry, Nov-11, Volume: 37, Issue:23	Design, synthesis, and biological properties of highly potent cyclic dynorphin A analogues. Analogues cyclized between positions 5 and 11.
AID431806	Selectivity ratio of Ki for rat kappa opioid receptor to Ki for mouse delta opioid receptor	2009	Journal of medicinal chemistry, Sep-24, Volume: 52, Issue:18	Design, synthesis, and pharmacological activities of dynorphin A analogues cyclized by ring-closing metathesis.
AID78851	Inhibition of electrically induced smooth muscle contraction in guinea pig ileum.	1994	Journal of medicinal chemistry, Nov-11, Volume: 37, Issue:23	Design, synthesis, and biological properties of highly potent cyclic dynorphin A analogues. Analogues cyclized between positions 5 and 11.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	5 (38.46)	18.2507
2000's	7 (53.85)	29.6817
2010's	1 (7.69)	24.3611
2020's	0 (0.00)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	0 (0.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	13 (100.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
enkephalin-leu, arg(6)- [no description available]	2.01	1
enkephalin, leucine Enkephalin, Leucine: One of the endogenous pentapeptides with morphine-like activity. It differs from MET-ENKEPHALIN in the LEUCINE at position 5. Its first four amino acid sequence is identical to the tetrapeptide sequence at the N-terminal of BETA-ENDORPHIN.. Leu-enkephalin : A pentapeptide comprising L-tyrosine, glycine, glycine, L-phenylalanine and L-leucine residues joined in sequence by peptide linkages. It is an endogenous opioid peptide produced in vertebrate species, including rodents, primates and humans that results from decomposition of proenkephalin or dynorphin and exhibits antinociceptive properties.	2.01	1	pentapeptide; peptide zwitterion	analgesic; delta-opioid receptor agonist; human metabolite; mu-opioid receptor agonist; neurotransmitter; rat metabolite
u-50488 3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer: A non-peptide, kappa-opioid receptor agonist which has also been found to stimulate the release of adrenocorticotropin (ADRENOCORTICOTROPIC HORMONE) via the release of hypothalamic arginine vasopressin (ARGININE VASOPRESSIN) and CORTICOTROPIN-RELEASING HORMONE. (From J Pharmacol Exp Ther 1997;280(1):416-21). U50488 : A monocarboxylic acid amide obtained by formal condensation between the carboxy group of 3,4-dichlorophenylacetic acid and the secondary amino group of (1R,2R)-N-methyl-2-(pyrrolidin-1-yl)cyclohexanamine	2.44	2	dichlorobenzene; monocarboxylic acid amide; N-alkylpyrrolidine	analgesic; antitussive; calcium channel blocker; diuretic; kappa-opioid receptor agonist
dynorphin (1-17) [no description available]	2.01	1
dynorphin (1-11) [no description available]	2.48	2
naloxone Naloxone: A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.. naloxone : A synthetic morphinane alkaloid that is morphinone in which the enone double bond has been reduced to a single bond, the hydrogen at position 14 has been replaced by a hydroxy group, and the methyl group attached to the nitrogen has been replaced by an allyl group. A specific opioid antagonist, it is used (commonly as its hydrochloride salt) to reverse the effects of opioids, both following their use of opioids during surgery and in cases of known or suspected opioid overdose.	2.46	2	morphinane alkaloid; organic heteropentacyclic compound; tertiary alcohol	antidote to opioid poisoning; central nervous system depressant; mu-opioid receptor antagonist
norbinaltorphimine norbinaltorphimine: kappa opiate receptor antagonist; structure given in first source	2.7	3	isoquinolines
dynorphin (1-17) [no description available]	2.01	1
dynorphin (1-17) [no description available]	1.97	1
dynorphins dynorphin (1-13): potent opioid peptide; see also record for dynorphin & D-Ala(2)-dynorphin (1-11)	2.13	1

Condition	Relationship Strength	Studies
Muscle Contraction A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.	3.38	7
Ache [description not available]	2.13	1
Pain An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.	2.13	1

dynorphin a (1-11)-amide

Cross-References

Synonyms (12)

Protein Targets (10)

Inhibition Measurements

Activation Measurements

Biological Processes (52)

Molecular Functions (12)

Ceullar Components (23)

Bioassays (84)

Research

Studies (13)

Market Indicators

Research Demand Index: 11.63

Study Types

dynorphin a (1-11)-amide

Cross-References

Synonyms (12)

Protein Targets (10)

Inhibition Measurements

Activation Measurements

Biological Processes (52)

Molecular Functions (12)

Ceullar Components (23)

Bioassays (84)

Research

Studies (13)

Market Indicators

Research Demand Index: 11.63

Study Types

Related Drugs (10)

Related Conditions (3)