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出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2015/11/25 16:17:29」(JST)
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Conivaptan
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Systematic (IUPAC) name |
N-(4-((4,5-dihydro-2-methylimidazo[4,5-d][1]benzazepin- 6(1H)-yl)carbonyl)phenyl)- (1,1'-biphenyl)-2-carboxamide
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Clinical data |
Trade names |
Vaprisol |
AHFS/Drugs.com |
monograph |
Pregnancy
category |
- US: C (Risk not ruled out)
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Legal status |
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Routes of
administration |
intravenous |
Pharmacokinetic data |
Bioavailability |
N/A |
Identifiers |
CAS Number |
210101-16-9 Y |
ATC code |
C03XA02 |
PubChem |
CID: 151171 |
IUPHAR/BPS |
2203 |
DrugBank |
DB00872 Y |
ChemSpider |
133239 Y |
UNII |
0NJ98Y462X Y |
KEGG |
D01236 N |
ChEBI |
CHEBI:681850 Y |
ChEMBL |
CHEMBL1755 Y |
Chemical data |
Formula |
C32H26N4O2 |
Molecular mass |
498.583 g/mol |
SMILES
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O=C(c2ccccc2c1ccccc1)Nc3ccc(cc3)C(=O)N5c6c(c4nc(nc4CC5)C)cccc6
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InChI
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InChI=1S/C32H26N4O2/c1-21-33-28-19-20-36(29-14-8-7-13-27(29)30(28)34-21)32(38)23-15-17-24(18-16-23)35-31(37)26-12-6-5-11-25(26)22-9-3-2-4-10-22/h2-18H,19-20H2,1H3,(H,33,34)(H,35,37) Y
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Key:IKENVDNFQMCRTR-UHFFFAOYSA-N Y
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N (what is this?) (verify) |
Conivaptan (YM 087, brand name Vaprisol) is a non-peptide inhibitor of antidiuretic hormone (vasopressin receptor antagonist). It was approved in 2004 for hyponatremia (low blood sodium levels) caused by syndrome of inappropriate antidiuretic hormone (SIADH), and there is some evidence it may be effective in heart failure. It is marketed by Cumberland Pharmaceuticals, Inc.
Conivaptan inhibits two of the three subtypes of the vasopressin receptor (V1a and V2). Effectively, it causes iatrogenic nephrogenic diabetes insipidus.
Conivaptan has not been approved by the FDA for the treatment of decompensated congestive heart failure. However, in theory, vasopressin receptor antagonism would be particularly useful in this setting, and an initial study shows that it has some promise.[1]
References
- ^ Udelson JE, Smith WB, Hendrix GH; et al. (November 2001). "Acute hemodynamic effects of conivaptan, a dual V(1A) and V(2) vasopressin receptor antagonist, in patients with advanced heart failure". Circulation 104 (20): 2417–23. doi:10.1161/hc4501.099313. PMID 11705818.
Antihypertensives: diuretics (C03)
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Sulfonamides
(and etacrynic acid) |
CA inhibitors (at PT) |
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Loop (Na-K-Cl at AL) |
- Furosemide#
- Bumetanide
- Etacrynic acid
- Etozoline
- Muzolimine
- Piretanide
- Tienilic acid
- Torasemide
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Thiazides (Na-Cl at DCT,
Calcium-sparing) |
- Altizide
- Bendroflumethiazide
- Chlorothiazide
- Cyclopenthiazide
- Cyclothiazide
- Epitizide
- Hydrochlorothiazide#
- Hydroflumethiazide
- Mebutizide
- Methyclothiazide
- Polythiazide
- Trichlormethiazide
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Thiazide-likes (primarily DCT) |
- Quinethazone
- Clopamide
- Chlortalidone
- Mefruside
- Clofenamide
- Metolazone
- Meticrane
- Xipamide
- Indapamide
- Clorexolone
- Fenquizone
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Potassium-sparing (at CD) |
ESC blockers |
- Amiloride#
- Triamterene
- Benzamil
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Aldosterone antagonists |
- Spironolactone#
- Eplerenone
- Potassium canrenoate
- Canrenone
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Osmotic diuretics (PT, DL) |
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Vasopressin receptor inhibitors
(DCT and CD) |
- Vaptans: Conivaptan
- Mozavaptan
- Satavaptan
- Tolvaptan
- Others: Demeclocycline
- Lithium carbonate
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Other |
- ethanol, isopropanol, 2M2B
- mercurial diuretic (Mersalyl, Meralluride)
- Theobromine
- Cicletanine
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- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
Index of the circulatory system
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Description |
- Anatomy
- Arteries
- head and neck
- arms
- chest
- abdomen
- legs
- Veins
- head and neck
- arms
- chest
- abdomen and pelvis
- legs
- Development
- Cells
- Physiology
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Disease |
- Congenital
- Neoplasms and cancer
- Lymphatic vessels
- Injury
- Vasculitis
- Other
- Symptoms and signs
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Treatment |
- Procedures
- Drugs
- beta blockers
- channel blockers
- diuretics
- nonsympatholytic vasodilatory antihypertensives
- peripheral vasodilators
- renin–angiotensin system
- sympatholytic antihypertensives
- vasoprotectives
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Neuropeptidergics
|
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CGRP |
- Agonists: Amylin
- CGRP
- Pramlintide
- Antagonists: BI 44370 TA
- BMS-927711
- CGRP (8-37)
- MK-3207
- Olcegepant
- Rimegepant
- SB-268262
- Telcagepant
- Ubrogepant
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Cholecystokinin |
CCKA
|
- Agonists: Cholecystokinin
- CCK-4
- Antagonists: Amiglumide
- Asperlicin
- Devazepide
- Dexloxiglumide
- Lintitript
- Lorglumide
- Loxiglumide
- Pranazepide
- Proglumide
- Tarazepide
- Tomoglumide
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CCKB
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- Agonists: Cholecystokinin
- CCK-4
- Gastrin
- Antagonists: CI-988 (PD-134,308)
- Itriglumide
- L-365,360
- Netazepide
- Proglumide
- Spiroglumide
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Unsorted
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- Antagonists: Nastorazepide
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CRH |
CRF1
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- Agonists: Cortagine
- Corticorelin
- Corticotropin releasing hormone
- Sauvagine
- Stressin I
- Urocortin
- Antagonists: Antalarmin
- Astressin-B
- CP-154,526
- Emicerfont
- Hypericin
- LWH-234
- NBI-27914
- Pexacerfont
- R-121,919
- TS-041
- Verucerfont
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CRF2
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- Agonists: Corticorelin
- Corticotropin releasing hormone
- Sauvagine
- Urocortin
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Galanin |
GAL1
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- Agonists: Galanin
- Galanin (1-15)
- Galanin-like peptide
- Galmic
- Galnon
- Antagonists: C7
- Dithiepine-1,1,4,4-tetroxide
- Galantide (M15)
- M32
- M35
- M40
- SCH-202596
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GAL2
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- Agonists: Galanin
- Galanin (1-15)
- Galanin (2-11)
- Galanin-like peptide
- Galmic
- Galnon
- J18
- Antagonists: C7
- Galantide (M15)
- M32
- M35
- M40
- M871
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GAL3
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- Agonists: Galanin
- Galanin (1-15)
- Galmic
- Galnon
- Antagonists: C7
- Galantide (M15)
- GalR3ant
- HT-2157
- M32
- M35
- M40
- SNAP-37889
- SNAP-398299
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Ghrelin/GHS |
- Agonists: Adenosine
- Alexamorelin
- Anamorelin
- Capromorelin
- CP-464709
- Cortistatin-14
- Examorelin (hexarelin)
- Ghrelin (lenomorelin)
- GHRP-1
- GHRP-3
- GHRP-4
- GHRP-5
- GHRP-6
- Ibutamoren (MK-677)
- Ipamorelin
- L-692,585
- LY-426410
- LY-444711
- Macimorelin
- Pralmorelin (GHRP-2)
- Relamorelin
- SM-130,686
- Tabimorelin
- Ulimorelin
- Antagonists: A-778,193
- Cortistatin-8
- (D-Lys3)-GHRP-6
- YIL-781
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MCH |
MCH1
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- Agonists: Melanin concentrating hormone
- Antagonists: ATC-0065
- ATC-0175
- GW-803,430
- NGD-4715
- SNAP-7941
- SNAP-94847
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MCH2
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- Agonists: Melanin concentrating hormone
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Melanocortin |
MC1
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- Agonists: α-MSH
- β-MSH
- γ-MSH
- ACTH (corticotropin)
- Afamelanotide
- BMS-470,539
- Bremelanotide
- HS-014
- HS-024
- Melanotan II
- Modimelanotide
- PL-8177
- SHU-8914
- SHU-9005
- SHU-9119
- SNAP-7941
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MC2
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- Agonists: ACTH (corticotropin)
- Alsactide
- Codactide
- Giractide
- Norleusactide (pentacosactride)
- Seractide
- Tetracosactide (tetracosactrin, cosyntropin)
- Tosactide (octacosactrin)
- Tricosactide
- Tridecactide
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MC3
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- Agonists: α-MSH
- β-MSH
- γ-MSH
- ACTH (corticotropin)
- Afamelanotide
- Bremelanotide
- Melanotan II
- Modimelanotide
- PG-931
- Antagonists: AGRP
- ASIP
- HS-014
- ML-00253764
- PG-106
- SHU-8914
- SHU-9005
- SHU-9119
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MC4
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- Agonists: α-MSH
- β-MSH
- γ-MSH
- ACTH (corticotropin)
- Afamelanotide
- AZD2820
- BIM-22493
- Bremelanotide
- LY-2112688
- Melanotan II
- MK-0493
- Modimelanotide
- PF-00446687
- PG-931
- PL-6983
- Ro 27-3225
- Setmelanotide
- THIQ
- Antagonists: AGRP
- ASIP
- HS-014
- HS-024
- HS-131
- JKC-363
- MCL-0020
- MCL-0042
- MCL-0129
- ML-00253764
- MPB-10
- SHU-8914
- SHU-9005
- SHU-9119
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MC5
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- Agonists: α-MSH
- β-MSH
- γ-MSH
- ACTH (corticotropin)
- Afamelanotide
- Bremelanotide
- HS-014
- HS-024
- Melanotan II
- Modimelanotide
- SHU-8914
- SHU-9005
- SHU-9119
- Antagonists: ASIP
- ML-00253764
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Unsorted
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- Agonists: Alsactide
- Codactide
- Giractide
- Norleusactide (pentacosactride)
- Seractide
- Tetracosactide (tetracosactrin, cosyntropin)
- Tosactide (octacosactrin)
- Tricosactide
- Tridecactide
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Neuropeptide FF |
- Agonists: Neuropeptide AF
- Neuropeptide FF
- Neuropeptide SF (RFRP-1)
- Neuropeptide VF (RFRP-3)
- Antagonists: BIBP-3226
- RF9
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Neuropeptide S |
- Antagonists: ML-154
- SHA-68
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Neuropeptide Y |
Y1
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- Agonists: Neuropeptide Y
- Peptide YY
- Antagonists: BIBO-3304
- BIBP-3226
- BVD-10
- GR-231,118
- PD-160,170
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Y2
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- Agonists: 2-Thiouridine 5'-triphosphate
- Neuropeptide Y
- Neuropeptide Y (13-36)
- Peptide YY
- Peptide YY (3-36)
- Antagonists: BIIE-0246
- JNJ-5207787
- SF-11
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Y4
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- Agonists: GR-231,118
- Neuropeptide Y
- Pancreatic polypeptide
- Peptide YY
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Y5
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- Agonists: BWX-46
- Neuropeptide Y
- Peptide YY
- Antagonists: CGP-71683
- FMS-586
- L-152,804
- Lu AA-33810
- MK-0557
- NTNCB
- Velneperit (S-2367)
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Neurotensin |
NTS1
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- Agonists: Neurotensin
- Neuromedin N
- Antagonists: Meclinertant
- SR-142,948
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NTS2
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- Antagonists: Levocabastine
- SR-142,948
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Opioid |
See here instead.
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Orexin |
OX1
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- Agonists: Orexin-A
- Orexin-B
- Antagonists: ACT-335827
- ACT-462206
- Almorexant
- Filorexant
- Lemborexant
- SB-334,867
- SB-408,124
- SB-649,868
- Suvorexant
- TCS-1102
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OX2
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- Agonists: Orexin-A
- Orexin-B
- SB-668,875
- Antagonists: ACT-335827
- ACT-462206
- Almorexant
- EMPA
- Filorexant
- JNJ-10397049
- JNJ-42847922
- Lemborexant
- MK-1064
- SB-649,868
- Suvorexant
- TCS-1102
- TCS-OX2-29
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Oxytocin |
- Agonists: Aspartocin
- Carbetocin
- Cargutocin
- Demoxytocin
- Lipo-oxytocin-1
- Merotocin
- Nacartocin
- Oxytocin
- TC OT 39
- TGOT
- Vasotocin (argiprestocin)
- WAY-267,464
- Antagonists: Atosiban
- Barusiban
- Epelsiban
- Erlosiban
- L-368,899
- L-371,257
- L-372,662
- OBE001
- Retosiban
- SSR-126,768
- Tocinoic acid
- WAY-162,720
- Metabolism inhibitors: Amastatin
- Bestatin (ubenimex)
- EDTA
- L-Methionine
- Leupeptin
- o-Phenanthroline
- Phosphoramidon
- Puromycin
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Tachykinin |
NK1
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- Antagonists: Aprepitant
- Befetupitant
- Burapitant
- Casopitant
- CI-1021
- CP-96,345
- CP-99,994
- CP-122,721
- Dapitant
- Ezlopitant
- Figopitant
- FK-888
- Fosaprepitant
- Fosnetupitant
- GR-203,040
- GW-597,599
- HSP-117
- L-733,060
- L-741,671
- L-743,310
- L-758,298
- Lanepitant
- LY-306,740
- Maropitant
- Netupitant
- NKP-608
- Nolpitantium besilate
- Orvepitant
- Rolapitant
- RP-67,580
- SDZ NKT 343
- Serlopitant
- Telmapitant
- Tradipitant
- Vestipitant
- Vofopitant
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NK2
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- Antagonists: GR-159,897
- Ibodutant
- Nepadutant
- Saredutant
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NK3
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- Antagonists: Osanetant
- Talnetant
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Vasopressin |
V1A
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- Agonists: Felypressin
- Lypressin
- Ornipressin
- Selepressin
- Terlipressin
- Vasopressin (argipressin)
- Vasotocin (argiprestocin)
- Antagonists: Atosiban
- Conivaptan
- FR-218944
- JNJ-17079166
- JNJ-17308616
- LY-307174
- PF-184563
- Relcovaptan
- RG7314
- SRX246
- SRX251
- TC OT 39
- WAY-267,464
- YM-218
- YM-471
- YM-35471
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V1B
|
- Agonists: Desmopressin
- Felypressin
- Lypressin
- Ornipressin
- Terlipressin
- Vasopressin (argipressin)
- Vasotocin (argiprestocin)
- Antagonists: ABT-436
- Nelivaptan
- ORG-52186
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V2
|
- Agonists: Desmopressin
- Felypressin
- Lypressin
- Ornipressin
- TC OT 39
- Terlipressin
- Vasopressin (argipressin)
- Vasotocin (argiprestocin)
- Antagonists: Conivaptan
- JNJ-17079166
- Lixivaptan
- Mozavaptan
- RWJ-351647
- Satavaptan
- Tolvaptan
- YM-471
- YM-35471
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Unsorted
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- Antagonists: Ribuvaptan
- RWJ-339489
- VMAX-367
- VMAX-372
- VMAX-382
- YM-222546
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See also: Peptidergics
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UpToDate Contents
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English Journal
- Hypertension in mice with transgenic activation of the brain renin-angiotensin system is vasopressin dependent.
- Littlejohn NK, Siel RB Jr, Ketsawatsomkron P, Pelham CJ, Pearson NA, Hilzendeger AM, Buehrer BA, Weidemann BJ, Li H, Davis DR, Thompson AP, Liu X, Cassell MD, Sigmund CD, Grobe JL.SourceDept. of Pharmacology, Roy J. and Lucille A. Carver College of Medicine, Univ. of Iowa, 51 Newton Rd., 2-307 BSB, Iowa City, IA 52242. justin-grobe@uiowa.edu.
- American journal of physiology. Regulatory, integrative and comparative physiology.Am J Physiol Regul Integr Comp Physiol.2013 May;304(10):R818-28. doi: 10.1152/ajpregu.00082.2013. Epub 2013 Mar 27.
- An indispensable role for the brain renin-angiotensin system (RAS) has been documented in most experimental animal models of hypertension. To identify the specific efferent pathway activated by the brain RAS that mediates hypertension, we examined the hypothesis that elevated arginine vasopressin (A
- PMID 23535460
- Pharmacokinetics of intravenous conivaptan in subjects with hepatic or renal impairment.
- Roy MJ, Erdman KA, Abeyratne AT, Plumb LC, Lasseter K, Riff DS, Keirns JJ.SourceAstellas Pharma Global Development, Inc., 1 Astellas Way, Northbrook, IL 60062, USA.
- Clinical pharmacokinetics.Clin Pharmacokinet.2013 May;52(5):385-95. doi: 10.1007/s40262-013-0047-8.
- BACKGROUND: Conivaptan is a non-peptide dual antagonist of vasopressin V1A and V2 receptors that is approved in the United States as an intravenous formulation for the treatment of euvolemic and hypervolemic hyponatremia in hospitalized patients. The pharmacokinetics of intravenous conivaptan had no
- PMID 23456393
- [Conivaptan inhibites cell proliferation and collagen production of cardiac fibroblasts induced by arginine vasopressin].
- Xie Y, Sun Z, Gai L.SourceDepartment of Cardiology, General Hospital of PLA, Beijing 100853, China.
- Xi bao yu fen zi mian yi xue za zhi = Chinese journal of cellular and molecular immunology.Xi Bao Yu Fen Zi Mian Yi Xue Za Zhi.2013 May;29(5):477-80.
- Objective To investigate the effects of arginine vasopressin (AVP) and its receptor antagonist conivaptan (CON) on the proliferation of cardiac fibroblasts (CFs) and the production of collagen I and III. Methods CFs were isolated by collagenase II method and purified with differential attachment and
- PMID 23643265
Japanese Journal
- Therapeutic Potential of Vasopressin-Receptor Antagonists in Heart Failure
- New Topics in Vasopressin Receptors and Approach to Novel Drugs : Research and Development of Conivaptan Hydrochloride (YM087), a Drug for the Treatment of Hyponatremia
- A Novel Vasopressin Dual V_<1A>/V_2 Receptor Antagonist, Conivaptan Hydrochloride, Improves Hyponatremia in Rats with Syndrome of Inappropriate Secretion of Antidiuretic Hormone (SIADH)(Pharmacology)
Related Pictures
![Conivaptan](https://1mg.info/0/1/5/0619.jpg)
![Conivaptan hydrochloride](https://1mg.info/0/1/5/0620.jpg)
![Skeletal formula of conivaptan](https://1mg.info/0/1/5/0621.jpg)
![hedtke80](https://1mg.info/0/1/5/0622.jpg)
![Distribution](https://1mg.info/0/1/5/0623.jpg)
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