168626-94-6 Usage
Description
Conivaptan hydrochloride, also known as Vaprisol, is a hydrochloride salt of conivaptan and functions as an antagonist for two of the three types of arginine vasopressin (AVP) receptors, specifically V1a and V2. It is a white to off-white solid and is used for the treatment of hyponatremia (low blood sodium levels) caused by the syndrome of inappropriate antidiuretic hormone (SIADH).
Uses
1. Used in the Treatment of Hyponatremia:
Conivaptan hydrochloride is used as a therapeutic agent for the treatment of hyponatremia, particularly in cases caused by SIADH. It helps to increase serum sodium concentration and reduce total body volume by blocking the renal V2 receptor, resulting in enhanced diuresis.
2. Used in the Treatment of Congestive Heart Failure:
Conivaptan hydrochloride is used as a vasopressin receptor antagonist in the treatment of congestive heart failure. It modulates systemic vascular resistance through the V1a receptor, which is distributed in vascular smooth muscle cells, cardiomyocytes, hepatocytes, and platelets. This action helps to restore volume homeostasis and alleviate the symptoms of congestive heart failure.
3. Used in the Management of Syndrome of Inappropriate Antidiuretic Hormone (SIADH):
Conivaptan hydrochloride is used as a treatment option for SIADH, a condition characterized by an imbalance of sodium and water in the body due to elevated levels of arginine vasopressin. By antagonizing vasopressin receptors, conivaptan hydrochloride helps to restore homeostasis and manage the symptoms associated with SIADH.
4. Used in the Treatment of Other Diseases:
Conivaptan hydrochloride has shown promise as a potential treatment option for other diseases, such as diabetes insipidus and liver cirrhosis. Its dual V1a and V2 vasopressin receptor antagonist properties make it a versatile candidate for further research and development in these areas.
5. Used in Experimental Stroke Models:
Conivaptan hydrochloride is used as a therapeutic agent in mouse experimental stroke models. It has been shown to reduce brain edema and blood-brain barrier disruption, which are critical factors in the progression of stroke and its associated complications.
Originator
Yamanouchi (Japan)
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
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, (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.