塩酸プラルモレリン

関: pralmorelin

WordNet

a complex consisting of an organic base in association with hydrogen chloride

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/09/10 15:22:00」(JST)

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Pralmorelin (INN) (brand name GHRP Kaken 100; former developmental code names KP-102, GPA-748, WAY-GPA-748), also known as pralmorelin hydrochloride (JAN) and pralmorelin dihydrochloride (USAN), as well as, notably, growth hormone-releasing peptide 2 (GHRP-2), is a growth hormone secretagogue (GHS) used as a diagnostic agent that is marketed by Kaken Pharmaceutical in Japan in a single-dose formulation for the assessment of growth hormone deficiency (GHD).^[1]^[2]^[3]

Pralmorelin is an orally-active, synthetic peptide drug, specifically, an analogue of met-enkephalin, with the amino acid sequence D-Ala-D-(β-naphthyl)-Ala-Ala-Trp-D-Phe-Lys-NH₂.^[2]^[4] It acts as a ghrelin/growth hormone secretagogue receptor (GHSR) agonist, and was the first of this class of drugs to be introduced clinically.^[2]^[3] Acute administration of the drug markedly increases the levels of plasma growth hormone (GH)^[4]^[5] and reliably induces sensations of hunger and increases food intake in humans.^[6]

Pralmorelin was also under investigation for the treatment of GHD and short stature (pituitary dwarfism), and made it to phase II clinical trials for these indications, but was ultimately never marketed for them.^[4] This may be because the ability of pralmorelin to increase plasma GH levels is significantly lower in people with GHD relative to healthy individuals.^[4]

References

^ Graul, Ann I.; Prous, J.R. (2006). "The Year's New Drugs: A Historical and Research Perspective on the 41 New Products that Reached their First Markets in 2005". Drug News & Perspectives (Prous Science) 19 (1): 33. ISSN 0214-0934.
^ ^a ^b ^c Moulin, Aline; Brunel, Luc; Verdie, Pascal; Gavara, Laurent; Martinez, Jean; Fehrentz, Jean-Alain (2014). "Ghrelin Receptor Ligands: Design and Synthesis of Pseudopeptides and Peptidomimetics". Current Chemical Biology 7 (3): 254–270. doi:10.2174/2212796807999131128125920. ISSN 2212-7968.
^ ^a ^b J. Larry Jameson; Leslie J. De Groot (25 February 2015). Endocrinology: Adult and Pediatric: Expert Consult - Online. Elsevier Health Sciences. pp. 1366–. ISBN 978-0-323-32195-2.
^ ^a ^b ^c ^d Adis Editorial (2004). "Pralmorelin". Drugs in R & D (Springer International Publishing) 5 (4): 236–239. doi:10.2165/00126839-200405040-00011.
^ Furuta S, Shimada O, Doi N, Ukai K, Nakagawa T, Watanabe J, Imaizumi M (2004). "General pharmacology of KP-102 (GHRP-2), a potent growth hormone-releasing peptide". Arzneimittelforschung 54 (12): 868–80. doi:10.1055/s-0031-1297042. PMID 15646371.
^ Müller, T.D.; Nogueiras, R.; Andermann, M.L.; Andrews, Z.B.; Anker, S.D.; Argente, J.; Batterham, R.L.; Benoit, S.C.; Bowers, C.Y.; Broglio, F.; Casanueva, F.F.; D'Alessio, D.; Depoortere, I.; Geliebter, A.; Ghigo, E.; Cole, P.A.; Cowley, M.; Cummings, D.E.; Dagher, A.; Diano, S.; Dickson, S.L.; Diéguez, C.; Granata, R.; Grill, H.J.; Grove, K.; Habegger, K.M.; Heppner, K.; Heiman, M.L.; Holsen, L.; Holst, B.; Inui, A.; Jansson, J.O.; Kirchner, H.; Korbonits, M.; Laferrère, B.; LeRoux, C.W.; Lopez, M.; Morin, S.; Nakazato, M.; Nass, R.; Perez-Tilve, D.; Pfluger, P.T.; Schwartz, T.W.; Seeley, R.J.; Sleeman, M.; Sun, Y.; Sussel, L.; Tong, J.; Thorner, M.O.; van der Lely, A.J.; van der Ploeg, L.H.T.; Zigman, J.M.; Kojima, M.; Kangawa, K.; Smith, R.G.; Horvath, T.; Tschöp, M.H. (2015). "Ghrelin". Molecular Metabolism 4 (6): 437–460. doi:10.1016/j.molmet.2015.03.005. ISSN 2212-8778.

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English Journal

Physiologically based pharmacokinetic model for pralmorelin hydrochloride in rats.

Nasu R1, Kumagai Y, Kogetsu H, Tsujimoto M, Ohtani H, Sawada Y.Author information 1Graduate School of Pharmaceutical Sciences, The University of Tokyo, 3-14-15 Hongo, Tokyo 113-0033, Japan.AbstractPralmorelin hydrochloride (pralmorelin), consisting of six amino acid residues, is a growth hormone-releasing peptide. The aim of this study is to analyze the pharmacokinetics of pralmorelin after intravenous bolus administration to rats, and to develop a physiologically based pharmacokinetic (PB-PK) model to describe and predict the concentrations of pralmorelin in blood and tissues. Pralmorelin (3 mg/kg) was administered intravenously to 24 Sprague-Dawley rats. Groups of three rats were sacrificed by decapitation at each designated time point (up to 4 h), and plasma and tissues (brain, lung, heart, liver, kidney, small intestine, muscle, adipose, and skin) were collected. Bile was also pooled until decapitation. The concentration of pralmorelin in samples was determined by liquid chromatography-tandem mass spectrometry. Plasma concentrations of pralmorelin declined rapidly in a biexponential manner. Biliary excretion of pralmorelin was so rapid that 80% of the dose was recovered unchanged in the bile within 1 h after administration. The distribution parameters in each tissue were obtained by using a hybrid model and an integration plot. They revealed that the distribution of pralmorelin into liver was blood flow-limited, and its distribution was permeability-limited in all other tissues. The PB-PK model developed in this study well described the time courses of pralmorelin concentration in the blood and tissues of rats.
Drug metabolism and disposition: the biological fate of chemicals.Drug Metab Dispos.2005 Oct;33(10):1488-94. Epub 2005 Jul 20.
Pralmorelin hydrochloride (pralmorelin), consisting of six amino acid residues, is a growth hormone-releasing peptide. The aim of this study is to analyze the pharmacokinetics of pralmorelin after intravenous bolus administration to rats, and to develop a physiologically based pharmacokinetic (PB-PK
PMID 16033952

Gateways to clinical trials.

Bayés M1, Rabasseda X, Prous JR.Author information 1Prous Science, Barcelona, Spain. mbayes@prous.comAbstractGateways to Clinical Trials is a guide to the most recent clinical trials in current literature and congresses. The data in the following tables has been retrieved from the Clinical Studies Knowledge Area of Prous Science Integrity, the drug discovery and development portal, http://integrity.prous.com. This issue focuses on the following selection of drugs: Abetimus sodium, adalimumab, alefacept, alemtuzumab, almotriptan, AMGN-0007, anakinra, anti-CTLA-4 Mab, L-arginine hydrochloride, arzoxifene hydrochloride, astemizole, atazanavir sulfate, atlizumab; Belimumab, BG-9928, binodenoson, bosentan, botulinum toxin type B, bovine lactoferrin, BufferGel; Caspofungin acetate, ciclesonide,cilomilast, ciluprevir, clofarabine, CVT-3146; Darbepoetin alfa, desloratadine, diflomotecan, doripenem, dronedarone hydrochloride, drotrecogin alfa (activated), DT388-GM-CSF, duloxetine hydrochloride, E-5564, efalizumab, enfuvirtide, esomeprazole magnesium, estradiol acetate, ETC-642, exenatide, exisulind, ezetimib; Febuxostat; Gallium maltolate, ganirelix acetate, garenoxacin mesilate, gefitinib; H11, HuMax; IL-15, IDD-1, IGIV-C, imatinib mesylate, ISIS-14803, ITF-1697, ivabradine hydrochloride; KRN-5500; L-365260, levetiracetam, levosimendan, licofelone, linezolid, LJP-1082, lopinavir lumiracoxib; MCC-478, melatonin, morphine hydrochloride, morphine-6-glucuronide, moxidectin; N-Acetylcarnosine, natalizumab, NM-702, NNC-05-1869, NSC-703940; Ocinaplon OM-89, omalizumab, omeprazole/ sodium bicarbonate, OPC-28326, ospemifene; PEG-filgrastim peginterferon alfa-2a, pegsunercept, pirfenidone, pralmorelin, pregabalin; Recombinant glucagon-like peptide-1 (7-36) amide, repifermin, RSD-1235; S-8184, selodenoson, sodium dichloroacetate, suberanilohydroxamic acid; TAS-102, terfenadine, teriparatide, tipranavir troxacitabine; Ximelagatran; YM-337.
Methods and findings in experimental and clinical pharmacology.Methods Find Exp Clin Pharmacol.2003 Dec;25(10):831-55.
Gateways to Clinical Trials is a guide to the most recent clinical trials in current literature and congresses. The data in the following tables has been retrieved from the Clinical Studies Knowledge Area of Prous Science Integrity, the drug discovery and development portal, http://integrity.prous.c
PMID 14735233

Gateways to clinical trials.

Bayes M1, Rabasseda X, Prous JR.Author information 1mbayes@prous.comAbstractGateways to Clinical Trials is a guide to the most recent clinical trials in current literature and congresses. The data in the following tables can be retrieved from the Clinical Studies knowledge area of Prous Science Integrity, the drug discovery and development portal, http://integrity.prous.com. This issue focuses on the following selection of drugs: Abacavir sulfate, abarelix, abciximab, acarbose, alefacept, alteplase, amisulpride, amoxicillin trihydrate, apomorphine hydrochloride, aprepitant, argatroban monohydrate, aspirin, atenolol; Betamethasone dipropionate, betamethasone valerate, bicalutamide, bleomycin sulfate; Calcium carbonate, candesartan cilexetil, celecoxib, cetirizine hydrochloride, cisplatin, clarithromycin, clavulanate potassium, clomethiazole edisilate, clopidogrel hydrogensulfate, cyclophosphamide, chorionic gonadotropin (human); Dalteparin sodium, desloratadine, dexamethasone, doxorubicin, DPC-083; Efalizumab, efavirenz, enoxaparin sodium, eprosartan mesilate, etanercept, etoposide, ezetimibe; Faropenem daloxate, fenofibrate, fluocinolone acetonide, flutamide, fluvastatin sodium, follitropin beta, fondaparinux sodium; Gabapentin, glibenclamide, goserelin, granisetron hydrochloride; Haloperidol, hydrochlorothiazide; Imiquimod, interferon beta-1a, irbesartan, iseganan hydrochloride; L-758298, lamivudine, lanoteplase, leflunomide, leuprorelin acetate, loratadine, losartan potassium; Melagatran, metformin hydrochloride, methotrexate, metronidazole, micafungin sodium, mitoxantrone hydrochloride; Nelfinavir mesilate, neutral insulin injection, nizatidine; Olopatadine hydrochloride, omeprazole, ondansetron hydrochloride; Pamidronate sodium, paracetamol, paroxetine hydrochloride, perindopril, pimecrolimus, pioglitazone hydrochloride, piroxicam, pleconaril, pralmorelin, pravastatin sodium, prednisolone, prednisone, propofol; Raloxifene hydrochloride, ranpirnase, remifentanil hydrochloride, risedronate sodium, risperidone, rofecoxib, ropinirole hydrochloride, rosuvastatin calcium; Sevoflurane, sildenafil citrate, simvastatin, somatropin; Tacrolimus, tamoxifen citrate, telmisartan, temozolomide, thiopental sodium, tinzaparin sodium, tirofiban hydrochloride, treosulfan, triamcinolone acetonide; Urokinase; Valsartan, vardenafil, vincristine; Warfarin sodium; Ximelagatran; Zidovudine.
Methods and findings in experimental and clinical pharmacology.Methods Find Exp Clin Pharmacol.2002 May;24(4):217-48.
Gateways to Clinical Trials is a guide to the most recent clinical trials in current literature and congresses. The data in the following tables can be retrieved from the Clinical Studies knowledge area of Prous Science Integrity, the drug discovery and development portal, http://integrity.prous.com
PMID 12092009

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★リンクテーブル★

リンク元	「プラルモレリン」「塩酸プラルモレリン」
関連記事	「pralmorelin」「hydrochloride」

「プラルモレリン」

Pralmorelin
Systematic (IUPAC) name
	(2S)-6-Amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2R)-2-aminopropanoyl]amino]-3-naphthalen-2-ylpropanoyl]amino]propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-phenylpropanoyl]amino]hexanamide</nowiki>
Clinical data
Routes of; administration	Oral, intravenous
Identifiers
CAS Registry Number	158861-67-7
PubChem	CID: 6852372
IUPHAR/BPS	1092
ChemSpider	5293451
Synonyms	D-Alanyl-3-(naphthalen-2-yl)-D-alanyl-L-alanyl-L-tryptophyl-D-phenylalanyl-L-lysinamide
Chemical data
Formula	C45H55N9O6
Molecular mass	817.9749 g/mol
	SMILES CC(C(=O)NC(CC1=CC2=CC=CC=C2C=C1)C(=O)NC(C)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NC(CC5=CC=CC=C5)C(=O)NC(CCCCN)C(=O)N)N ;

　　[★]

英: pralmorelin、pralmorelin hydrochloride
関: 塩酸プラルモレリン

「塩酸プラルモレリン」

　　[★]

英: pralmorelin hydrochloride
関: プラルモレリン

「pralmorelin」

　　[★]

プラルモレリン

関: pralmorelin hydrochloride

「hydrochloride」

　　[★] 塩酸塩、ハイドロクロライド　

[Graul2006-1] Graul, Ann I.; Prous, J.R. (2006). "The Year's New Drugs: A Historical and Research Perspective on the 41 New Products that Reached their First Markets in 2005". Drug News & Perspectives (Prous Science) 19 (1): 33. ISSN 0214-0934.

[MoulinBrunel2014-2] Moulin, Aline; Brunel, Luc; Verdie, Pascal; Gavara, Laurent; Martinez, Jean; Fehrentz, Jean-Alain (2014). "Ghrelin Receptor Ligands: Design and Synthesis of Pseudopeptides and Peptidomimetics". Current Chemical Biology 7 (3): 254–270. doi:10.2174/2212796807999131128125920. ISSN 2212-7968.

[JamesonGroot2015-3] J. Larry Jameson; Leslie J. De Groot (25 February 2015). Endocrinology: Adult and Pediatric: Expert Consult - Online. Elsevier Health Sciences. pp. 1366–. ISBN 978-0-323-32195-2.

[AdisEditorial2004-4] Adis Editorial (2004). "Pralmorelin". Drugs in R & D (Springer International Publishing) 5 (4): 236–239. doi:10.2165/00126839-200405040-00011.

[pmid15646371-5] Furuta S, Shimada O, Doi N, Ukai K, Nakagawa T, Watanabe J, Imaizumi M (2004). "General pharmacology of KP-102 (GHRP-2), a potent growth hormone-releasing peptide". Arzneimittelforschung 54 (12): 868–80. doi:10.1055/s-0031-1297042. PMID 15646371.

[M.C3.BCllerNogueiras2015-6] Müller, T.D.; Nogueiras, R.; Andermann, M.L.; Andrews, Z.B.; Anker, S.D.; Argente, J.; Batterham, R.L.; Benoit, S.C.; Bowers, C.Y.; Broglio, F.; Casanueva, F.F.; D'Alessio, D.; Depoortere, I.; Geliebter, A.; Ghigo, E.; Cole, P.A.; Cowley, M.; Cummings, D.E.; Dagher, A.; Diano, S.; Dickson, S.L.; Diéguez, C.; Granata, R.; Grill, H.J.; Grove, K.; Habegger, K.M.; Heppner, K.; Heiman, M.L.; Holsen, L.; Holst, B.; Inui, A.; Jansson, J.O.; Kirchner, H.; Korbonits, M.; Laferrère, B.; LeRoux, C.W.; Lopez, M.; Morin, S.; Nakazato, M.; Nass, R.; Perez-Tilve, D.; Pfluger, P.T.; Schwartz, T.W.; Seeley, R.J.; Sleeman, M.; Sun, Y.; Sussel, L.; Tong, J.; Thorner, M.O.; van der Lely, A.J.; van der Ploeg, L.H.T.; Zigman, J.M.; Kojima, M.; Kangawa, K.; Smith, R.G.; Horvath, T.; Tschöp, M.H. (2015). "Ghrelin". Molecular Metabolism 4 (6): 437–460. doi:10.1016/j.molmet.2015.03.005. ISSN 2212-8778.

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pralmorelin hydrochloride