neurokinin a(4-10) profile

Neurokinin A(4-10) is a hexapeptide fragment of neurokinin A, a neuropeptide involved in various physiological processes, including pain perception, inflammation, and smooth muscle contraction. It exhibits agonist activity at the neurokinin-1 receptor (NK-1R), a G protein-coupled receptor primarily expressed in the central and peripheral nervous systems. This fragment, unlike the full-length neurokinin A, displays a higher selectivity for NK-1R compared to other tachykinin receptors (NK-2R and NK-3R). Research on Neurokinin A(4-10) focuses on its potential as a therapeutic agent for conditions associated with NK-1R activation, such as pain, anxiety, and substance abuse. Studies have shown that Neurokinin A(4-10) can effectively reduce pain perception in animal models, suggesting its potential for pain management. Additionally, its ability to modulate neuronal activity in brain regions associated with anxiety and reward suggests its potential for treating anxiety disorders and substance dependence.'

neurokinin A(4-10): bronchospastic agent [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	122230
CHEMBL ID	126294
MeSH ID	M0158207

Synonym
CHEMBL126294 ,
nka-(4-10)
3-amino-n-(1-{1-[1-({[1-(1-carbamoyl-3-methylsulfanyl-propylcarbamoyl)-3-methyl-butylcarbamoyl]-methyl}-carbamoyl)-2-methyl-propylcarbamoyl]-2-phenyl-ethylcarbamoyl}-2-hydroxy-ethyl)-succinamic acid
bdbm50001451
(3s)-3-amino-4-[[(2s)-1-[[(2s)-1-[[(2s)-1-[[2-[[(2s)-1-[[(2s)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]am
l-methioninamide, l-alpha-aspartyl-l-seryl-l-phenylalanyl-l-valylglycyl-l-leucyl-
neurokinin a(4-10)
HY-P0236
DTXSID50913838
23-amino-17-benzyl-7,10,13,16,19,22-hexahydroxy-5-[hydroxy(imino)methyl]-20-(hydroxymethyl)-8-(2-methylpropyl)-14-(propan-2-yl)-2-thia-6,9,12,15,18,21-hexaazapentacosa-6,9,12,15,18,21-hexaen-25-oic acid
(5s,8s,14s,17s,20s,23s)-23-amino-17-benzyl-5-carbamoyl-20-(hydroxymethyl)-8-isobutyl-14-isopropyl-7,10,13,16,19,22-hexaoxo-2-thia-6,9,12,15,18,21-hexaazapentacosan-25-oic acid
asp-ser-phe-val-gly-leu-met-nh2

Excerpt	Reference	Relevance
"Tachykinin NK2 receptor antagonists could reduce motility and symptoms during gastrointestinal diseases characterized by local inflammation such as diarrhea or colitis; however, how these conditions change pharmacodynamic and pharmacokinetic characteristics of NK2 receptor antagonists is unknown."	( Nepadutant pharmacokinetics and dose-effect relationships as tachykinin NK2 receptor antagonist are altered by intestinal inflammation in rodent models. Bueno, L; Carini, F; Crea, A; Criscuoli, M; D'Aranno, V; Fioramonti, J; Giuliani, S; Lecci, A; Maggi, CA; Marinoni, E; Tramontana, M, 2001)	0.31

Excerpt	Reference	Relevance
" In the castor oil model, the oral/intraduodenal bioavailability of nepadutant was also determined."	( Nepadutant pharmacokinetics and dose-effect relationships as tachykinin NK2 receptor antagonist are altered by intestinal inflammation in rodent models. Bueno, L; Carini, F; Crea, A; Criscuoli, M; D'Aranno, V; Fioramonti, J; Giuliani, S; Lecci, A; Maggi, CA; Marinoni, E; Tramontana, M, 2001)	0.31

Excerpt	Relevance	Reference
" Thus, we have compared the actions of the selective neurokinin 1 (NK1) (CP-99,994) and neurokinin 2 (NK2) (SR-48,968) receptor antagonists against dose-response curves (DRC) induced by intravenously administered substance P (SP), neurokinin A (NKA), neurokinin B (NKB), beta Ala8-NKA (4-10),Sar9-Met(O2)11SP, and single dose (intravenous) challenge with resiniferatoxin (RTX), a capsaicin-like sensory neurotoxin, leukotriene D4 (LTD4) and antigen."	( NK1 and NK2 receptors mediate tachykinin and resiniferatoxin-induced bronchospasm in guinea pigs. Champion, E; Foulon, DM; Jones, TR; Masson, P; Rodger, IW, 1993)	0.29

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Substance-K receptor	Mesocricetus auratus (golden hamster)	IC50 (µMol)	0.0060	0.0010	0.0353	0.1480	AID211530
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Assay ID	Title	Year	Journal	Article
AID211530	Competitive inhibition of [125I]NKA binding to hamster urinary bladder Tachykinin receptor 2	1992	Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21	A new class of high affinity ligands for the neurokinin A NK2 receptor: psi (CH2NR) reduced peptide bond analogues of neurokinin A4-10.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	4 (12.90)	18.7374
1990's	22 (70.97)	18.2507
2000's	5 (16.13)	29.6817
2010's	0 (0.00)	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	34 (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
dimethyl sulfoxide Dimethyl Sulfoxide: A highly polar organic liquid, that is used widely as a chemical solvent. Because of its ability to penetrate biological membranes, it is used as a vehicle for topical application of pharmaceuticals. It is also used to protect tissue during CRYOPRESERVATION. Dimethyl sulfoxide shows a range of pharmacological activity including analgesia and anti-inflammation.. dimethyl sulfoxide : A 2-carbon sulfoxide in which the sulfur atom has two methyl substituents.	1.97	1	sulfoxide; volatile organic compound	alkylating agent; antidote; Escherichia coli metabolite; geroprotector; MRI contrast agent; non-narcotic analgesic; polar aprotic solvent; radical scavenger
histamine [no description available]	2.68	3	aralkylamino compound; imidazoles	human metabolite; mouse metabolite; neurotransmitter
guanethidine Guanethidine: An antihypertensive agent that acts by inhibiting selectively transmission in post-ganglionic adrenergic nerves. It is believed to act mainly by preventing the release of norepinephrine at nerve endings and causes depletion of norepinephrine in peripheral sympathetic nerve terminals as well as in tissues.. guanethidine : A member of the class of guanidines in which one of the hydrogens of the amino group has been replaced by a 2-azocan-1-ylethyl group.. guanethidine sulfate : A organic sulfate salt composed of two molecules of guanethidine and one of sulfuric acid.	1.98	1	azocanes; guanidines	adrenergic antagonist; antihypertensive agent; sympatholytic agent
isoproterenol Isoproterenol: Isopropyl analog of EPINEPHRINE; beta-sympathomimetic that acts on the heart, bronchi, skeletal muscle, alimentary tract, etc. It is used mainly as bronchodilator and heart stimulant.. isoprenaline : A secondary amino compound that is noradrenaline in which one of the hydrogens attached to the nitrogen is replaced by an isopropyl group. A sympathomimetic acting almost exclusively on beta-adrenergic receptors, it is used (mainly as the hydrochloride salt) as a bronghodilator and heart stimulant for the management of a variety of cardiac disorders.	2.39	2	catechols; secondary alcohol; secondary amino compound	beta-adrenergic agonist; bronchodilator agent; cardiotonic drug; sympathomimetic agent
potassium chloride Potassium Chloride: A white crystal or crystalline powder used in BUFFERS; FERTILIZERS; and EXPLOSIVES. It can be used to replenish ELECTROLYTES and restore WATER-ELECTROLYTE BALANCE in treating HYPOKALEMIA.. potassium chloride : A metal chloride salt with a K(+) counterion.	1.98	1	inorganic chloride; inorganic potassium salt; potassium salt	fertilizer
propranolol Propranolol: A widely used non-cardioselective beta-adrenergic antagonist. Propranolol has been used for MYOCARDIAL INFARCTION; ARRHYTHMIA; ANGINA PECTORIS; HYPERTENSION; HYPERTHYROIDISM; MIGRAINE; PHEOCHROMOCYTOMA; and ANXIETY but adverse effects instigate replacement by newer drugs.. propranolol : A propanolamine that is propan-2-ol substituted by a propan-2-ylamino group at position 1 and a naphthalen-1-yloxy group at position 3.	1.98	1	naphthalenes; propanolamine; secondary amine	anti-arrhythmia drug; antihypertensive agent; anxiolytic drug; beta-adrenergic antagonist; environmental contaminant; human blood serum metabolite; vasodilator agent; xenobiotic
thymidine [no description available]	1.97	1	pyrimidine 2'-deoxyribonucleoside	Escherichia coli metabolite; human metabolite; metabolite; mouse metabolite
carbachol Carbachol: A slowly hydrolyzed CHOLINERGIC AGONIST that acts at both MUSCARINIC RECEPTORS and NICOTINIC RECEPTORS.	2.38	2	ammonium salt; carbamate ester	cardiotonic drug; miotic; muscarinic agonist; nicotinic acetylcholine receptor agonist; non-narcotic analgesic
methacholine chloride Methacholine Chloride: A quaternary ammonium parasympathomimetic agent with the muscarinic actions of ACETYLCHOLINE. It is hydrolyzed by ACETYLCHOLINESTERASE at a considerably slower rate than ACETYLCHOLINE and is more resistant to hydrolysis by nonspecific CHOLINESTERASES so that its actions are more prolonged. It is used as a parasympathomimetic bronchoconstrictor agent and as a diagnostic aid for bronchial asthma. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1116)	2	1	quaternary ammonium salt
tryptophan Tryptophan: An essential amino acid that is necessary for normal growth in infants and for NITROGEN balance in adults. It is a precursor of INDOLE ALKALOIDS in plants. It is a precursor of SEROTONIN (hence its use as an antidepressant and sleep aid). It can be a precursor to NIACIN, albeit inefficiently, in mammals.. tryptophan : An alpha-amino acid that is alanine bearing an indol-3-yl substituent at position 3.	1.97	1	erythrose 4-phosphate/phosphoenolpyruvate family amino acid; L-alpha-amino acid zwitterion; L-alpha-amino acid; proteinogenic amino acid; tryptophan zwitterion; tryptophan	antidepressant; Escherichia coli metabolite; human metabolite; micronutrient; mouse metabolite; nutraceutical; plant metabolite; Saccharomyces cerevisiae metabolite
pyrrolidonecarboxylic acid Pyrrolidonecarboxylic Acid: A cyclized derivative of L-GLUTAMIC ACID. Elevated blood levels may be associated with problems of GLUTAMINE or GLUTATHIONE metabolism.. 5-oxo-L-proline : An optically active form of 5-oxoproline having L-configuration.	2.39	2	5-oxoproline; L-proline derivative; non-proteinogenic L-alpha-amino acid	algal metabolite
phenyl acetate phenyl acetate: The ester formed between phenol and acetic acid. Don't confuse with phenylacetic acid derivatives listed under PHENYLACETATES.. phenyl acetate : An acetate ester obtained by the formal condensation of phenol with acetic acid.	2	1	benzenes; phenyl acetates
substance p [no description available]	3.99	14	peptide	neurokinin-1 receptor agonist; neurotransmitter; vasodilator agent
cp 96345 CP 96345: structure given in first source; potent nonpeptide antagonist of the substance P (NK1) receptor; CP 96344 is enantiomer of CP 96345	3.23	6
sr 48968 SR 48968: structure given in first source; neurokinin A antagonist; tachykinin receptor antagonist; SR 48965 is the inactive R-enantiomer of SR 48968	3.24	6
senktide [no description available]	2.67	3
gr 73632 GR 73632: neurokinin receptor agonist	1.97	1
substance p, methyl ester- substance P, methyl ester-: COOH-terminal amide of substance P replaced with methyl ester	1.97	1
neurokinin a (4-10), beta-ala(8)- neurokinin A (4-10), beta-Ala(8)-: selective NK-2 tachykinin receptor	2.38	2
neurokinin a(4-10), tyr(5)-trp(6,8,9)-lys(10)- neurokinin A(4-10), Tyr(5)-Trp(6,8,9)-Lys(10)-: tachykinin receptor antagonist	2.67	3
substance p, pro(9)- substance P, Pro(9)-: RN given refers to the (L-Pro)-isomer; RN for cpd without isomeric designation not available 3/91	2.67	3
substance p, sar(9)-met(o2)(11)- substance P, Sar(9)-Met(O2)(11)-: a neurokinin-1 receptor agonist	3.23	6
atropine tropan-3alpha-yl 3-hydroxy-2-phenylpropanoate : A tropane alkaloid that is (1R,5)-8-methyl-8-azabicyclo[3.2.1]octane substituted by a (3-hydroxy-2-phenylpropanoyl)oxy group at position 3.	2.38	2
bradykinin [no description available]	2	1	oligopeptide	human blood serum metabolite; vasodilator agent
amastatin amastatin: structure; inhibits aminopeptidase. amastatin : A tetrapeptide comprising (2S,3R)-3-amino-2-hydroxy-5-methylhexanoyl, L-valyl, L-valyl and L-aspartic acid units joined in sequence	1.98	1	tetrapeptide	EC 3.4.11.* (aminopeptidase) inhibitor; protease inhibitor
capsaicin ALGRX-4975: an injectable capsaicin (TRPV1 receptor agonist) formulation for longlasting pain relief. capsaicinoid : A family of aromatic fatty amides produced as secondary metabolites by chilli peppers.	2.68	3	capsaicinoid	non-narcotic analgesic; TRPV1 agonist; voltage-gated sodium channel blocker
neurokinin a (3-10), lysyl(3)-glycyl(8)-r-lactam-leucine(9)- neurokinin A (3-10), lysyl(3)-glycyl(8)-R-lactam-leucine(9)-: neurokinin receptor agonist	1.97	1
asp-ser-phe-val-gly-leu-ch2nh-leu-nh2 [no description available]	1.98	1
ovalbumin Ovalbumin: An albumin obtained from the white of eggs. It is a member of the serpin superfamily.	2	1
dinoprost Dinoprost: A naturally occurring prostaglandin that has oxytocic, luteolytic, and abortifacient activities. Due to its vasocontractile properties, the compound has a variety of other biological actions.. prostaglandin F2alpha : A prostaglandins Falpha that is prosta-5,13-dien-1-oic acid substituted by hydroxy groups at positions 9, 11 and 15. It is a naturally occurring prostaglandin used to induce labor.	1.98	1	monocarboxylic acid; prostaglandins Falpha	human metabolite; mouse metabolite
cp 99994 3-(2-methoxybenzylamino)-2-phenylpiperidine: selective NK(1) receptor antagonist; CP-100263 is the inactive enantiomer	1.98	1
neurokinin a Neurokinin A: A mammalian neuropeptide of 10 amino acids that belongs to the tachykinin family. It is similar in structure and action to SUBSTANCE P and NEUROKININ B with the ability to excite neurons, dilate blood vessels, and contract smooth muscles, such as those in the BRONCHI.	4.75	31
neurokinin b Neurokinin B: A mammalian neuropeptide of 10 amino acids that belongs to the tachykinin family. It is similar in structure and action to SUBSTANCE P and NEUROKININ A with the ability to excite neurons, dilate blood vessels, and contract smooth muscles, such as those in the URINARY BLADDER and UTERUS.	3.07	5	polypeptide
resiniferatoxin resiniferatoxin: phorbol related diterpene ester; potent agonist of vanilloid TRPV1 receptors. resiniferatoxin : A heteropentacyclic compound found in Euphorbia poissonii with molecular formula C37H40O9. It is an agonist of the transient receptor potential cation channel subfamily V member 1 (TrpV1).	1.98	1	carboxylic ester; diterpenoid; enone; monomethoxybenzene; organic heteropentacyclic compound; ortho ester; phenols; tertiary alpha-hydroxy ketone	analgesic; neurotoxin; plant metabolite; TRPV1 agonist
tetrodotoxin Tetrodotoxin: An aminoperhydroquinazoline poison found mainly in the liver and ovaries of fishes in the order TETRAODONTIFORMES, which are eaten. The toxin causes paresthesia and paralysis through interference with neuromuscular conduction.. tetrodotoxin : A quinazoline alkaloid that is a marine toxin isolated from fish such as puffer fish. It has been shown to exhibit potential neutotoxicity due to its ability to block voltage-gated sodium channels.	1.97	1	azatetracycloalkane; oxatetracycloalkane; quinazoline alkaloid	animal metabolite; bacterial metabolite; marine metabolite; neurotoxin; voltage-gated sodium channel blocker
men 11420 [no description available]	2	1
tachykinin neuropeptide gamma tachykinin neuropeptide gamma: potentiates substance P-induced salivation; lacks residues (3-17) of neuropeptide K; derived from gamma-preprotachykinin	1.98	1
septide [no description available]	2.39	2
neurokinin a (4-10), tyr(5)-trp(6,8,9)-arg(10)- [no description available]	1.97	1
piperidines Piperidines: A family of hexahydropyridines.	3.24	6
vasoactive intestinal peptide Vasoactive Intestinal Peptide: A highly basic, 28 amino acid neuropeptide released from intestinal mucosa. It has a wide range of biological actions affecting the cardiovascular, gastrointestinal, and respiratory systems and is neuroprotective. It binds special receptors (RECEPTORS, VASOACTIVE INTESTINAL PEPTIDE).	2	1
cyclic gmp Cyclic GMP: Guanosine cyclic 3',5'-(hydrogen phosphate). A guanine nucleotide containing one phosphate group which is esterified to the sugar moiety in both the 3'- and 5'-positions. It is a cellular regulatory agent and has been described as a second messenger. Its levels increase in response to a variety of hormones, including acetylcholine, insulin, and oxytocin and it has been found to activate specific protein kinases. (From Merck Index, 11th ed). 3',5'-cyclic GMP : A 3',5'-cyclic purine nucleotide in which the purine nucleobase is specified as guanidine.	2	1	3',5'-cyclic purine nucleotide; guanyl ribonucleotide	Escherichia coli metabolite; human metabolite; mouse metabolite; plant metabolite; Saccharomyces cerevisiae metabolite

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.	3.36	7
Bronchospasm [description not available]	2.67	3
Bronchial Spasm Spasmodic contraction of the smooth muscle of the bronchi.	2.67	3
Muscle Relaxation That phase of a muscle twitch during which a muscle returns to a resting position.	2	1
Bronchial Hyperreactivity Tendency of the smooth muscle of the tracheobronchial tree to contract more intensely in response to a given stimulus than it does in the response seen in normal individuals. This condition is present in virtually all symptomatic patients with asthma. The most prominent manifestation of this smooth muscle contraction is a decrease in airway caliber that can be readily measured in the pulmonary function laboratory.	2	1
Enteritis Inflammation of any segment of the SMALL INTESTINE.	2	1
Anesthesia A state characterized by loss of feeling or sensation. This depression of nerve function is usually the result of pharmacologic action and is induced to allow performance of surgery or other painful procedures.	2.67	3
Decerebrate Posturing [description not available]	1.97	1
Tachyarrhythmia [description not available]	1.97	1
Tachycardia Abnormally rapid heartbeat, usually with a HEART RATE above 100 beats per minute for adults. Tachycardia accompanied by disturbance in the cardiac depolarization (cardiac arrhythmia) is called tachyarrhythmia.	1.97	1

neurokinin a(4-10)

Description

Cross-References

Synonyms (12)

Research Excerpts

Pharmacokinetics

Bioavailability

Dosage Studied

Protein Targets (1)

Inhibition Measurements

Bioassays (1)

Research

Studies (31)

Market Indicators

Research Demand Index: 11.37

Study Types