168626-94-6 Usage
Description
Different sources of media describe the Description of 168626-94-6 differently. You can refer to the following data:
1. Arginine vasopressin is intimately involved in volume homeostasis, and
elevated levels of arginine vasopressin are responsible for the pathogenesis and
progression of diseases with an imbalance of sodium and water, particularly
congestive heart failure. To restore homeostasis, antagonism of vasopressin
receptors is a practical solution. As such, conivaptan has been developed and
launched as a dual V1a and V2 vasopressin receptor antagonist. As a competitive,
reversible inhibitor of both subtypes, conivaptan can modulate systemic vascular
resistance through the V1a receptor (Ki ? 0.48 nM) distributed in vascular smooth
muscle cells, cardiomyocytes, hepatocytes, and platelets and blocks the renal V2
receptor (Ki ? 3.04 nM) resulting in enhanced diuresis, thereby increasing serum
sodium concentration and reducing total body volume. Currently, the drug is
approved for the management of refractory hyponatremia and potentially lifethreatening
sodium and water imbalance, but it has shown promise as a potential
treatment option for other diseases, such as congestive heart failure, syndrome of
antidiuretic hormone, diabetes insipidus, and liver cirrhosis.
2. Conivaptan is an antagonist of the arginine vasopressin (AVP) receptors V1A and V2 (Kis = 0.48 and 3.04 nM for rat liver V1A and kidney V2, respectively). It also competitively inhibits oxytocin binding to rat uterine oxytocin receptors (Ki = 44 nM) but has no effect on AVP binding to anterior pituitary V1B receptors at concentrations up to 100 μM in a radioligand binding assay. Conivaptan suppresses AVP-induced increases in intracellular calcium in vascular smooth muscle cells (VSMCs) in vitro and the pressor response in pithed rats. Conivaptan (0.01-0.3 mg/kg, i.v.) increases urine output and decreases urine osmolality in dehydrated conscious rats in a dose-dependent manner. It also reduces brain edema and blood-brain barrier disruption in a mouse experimental stroke model.
Chemical Properties
White to Off-White Solid
Originator
Yamanouchi (Japan)
Uses
Different sources of media describe the Uses of 168626-94-6 differently. You can refer to the following data:
1. Conivaptan is a non-peptide inhibitor of antidiuretic hormone (vasopressin receptor antagonist).
2. Used in treatment of congestive heart failure.
Definition
ChEBI: The hydrochloride salt of conivaptan. It is an antagonist for two of the three types of arginine vasopressin (AVP) receptors, V1a and V2, and is used for the treatment of hyponatraemia (low blood sodium levels) cau
ed by syndrome of inappropriate antidiuretic hormone (SIADH).
Brand name
Vaprisol (Astellas).
Check Digit Verification of cas no
The CAS Registry Mumber 168626-94-6 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,6,8,6,2 and 6 respectively; the second part has 2 digits, 9 and 4 respectively.
Calculate Digit Verification of CAS Registry Number 168626-94:
(8*1)+(7*6)+(6*8)+(5*6)+(4*2)+(3*6)+(2*9)+(1*4)=176
176 % 10 = 6
So 168626-94-6 is a valid CAS Registry Number.
InChI:InChI=1/C32H26N4O2.ClH/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);1H
168626-94-6Relevant articles and documents
Preparation method of conivaptan hydrochloride
-
, (2017/08/27)
The invention discloses a preparation method of conivaptan hydrochloride. The preparation method includes: taking aniline (compound I) as a raw material which is subjected to amidation, alkylation, friedel-crafts acylation, nitro reduction, amidation, alpha-chloro, cyclization and salt-forming reaction to obtain the conivaptan hydrochloride. With the method, the aniline is taken as the raw material easy to obtain, and toxic substances of acyl chloride and the like are avoided during amidation. The entire synthesis process is small in pollution and easy to process with the brand new synthesis theory, and reaction conditions of procedures are moderate; the preparation method is moderate in reaction condition of each procedure, simple in operation, high in yield and purity, environment friendly, low in production cost and suitable in industrial production.
A new synthetic route to YM087, an arginine vasopressin antagonist
Tsunoda, Takashi,Tanaka, Akihiro,Mase, Toshiyasu,Sakamoto, Shuichi
, p. 1113 - 1122 (2007/10/03)
A new synthesis of N-{4-[(2-methyl-4,5-dihydroimidazo[4,5-d][1]benzazepin-6(1H)-yl)carbonyl]phenyl} biphenyl-2-carboxamide monohydrochloride (1, YM087) via new imidazobenzazepine intermediates is described. This method remarkably improves the overall yiel
Condensed benzazepine derivative and pharmaceutical composition thereof
-
, (2008/06/13)
This invention relates to nitrogen-containing aromatic 5-membered ring-condensed benzazepine derivatives represented by the general formula (I) STR1 (symbols in the formula have the following meanings; ring B: a nitrogen-containing aromatic 5-membered ring having at least 1 nitrogen atom and optionally one oxygen or sulfur atom, which may optionally have substituent(s), R1 and R2 : these may be the same or different from each other and each represents a hydrogen atom, a halogen atom, a lower alkyl group, an amino group which may optionally be substituted by lower alkyl group(s), or a lower alkoxy group, A: a single bond; a group represented by the formula n: 0 or an integer of from 1 to 3, R3 and R4 : these may be the same or different from each other and each represents a hydrogen atom, a lower alkyl group (provided that R3 and R4 may together form a lower alkylene group having 2 to 7 carbon atoms), and ring C: a benzene ring which may optionally have substituent(s)) and salts thereof; to pharmaceutical compositions which contain these compounds as an active ingredient and to intermediates which are useful in synthesizing these compounds. The compounds of this invention are useful as arginine vasopressin antagonists.
