1082954-71-9 Usage
Description
(±)-(7aR,11aR)-5,6,7a,8,9,10,11,11a-Octahydro-4-(1-piperazinyl)-benzofuran[2,3-h]quinazolin-2-amine is a complex organic compound with a unique molecular structure. It is characterized by its octahydro-benzofuran[2,3-h]quinazolin-2-amine core, which is further modified by a 1-piperazinyl group. (±)-(7aR,11aR)-5,6,7a,8,9,10,11,11a-Octahydro-4-(1-piperazinyl)-benzofuran[2,3-h]quinazolin-2-amine exhibits chiral centers at the 7a and 11a positions, leading to the (±) designation. Its specific properties and potential applications are yet to be fully explored, but its structural features suggest it may have interesting biological activities.
Uses
Used in Pharmaceutical Industry:
(±)-(7aR,11aR)-5,6,7a,8,9,10,11,11a-Octahydro-4-(1-piperazinyl)-benzofuran[2,3-h]quinazolin-2-amine is used as a potential therapeutic agent for various diseases due to its unique molecular structure and the presence of bioactive functional groups. Its specific application and mechanism of action are still under investigation.
Used in Research and Development:
In the field of medicinal chemistry and drug discovery, (±)-(7aR,11aR)-5,6,7a,8,9,10,11,11a-Octahydro-4-(1-piperazinyl)-benzofuran[2,3-h]quinazolin-2-amine serves as a valuable compound for research purposes. It can be used to study the structure-activity relationships of various biological targets and to develop new drugs with improved efficacy and selectivity.
Used in H4 Receptor Antagonism:
(±)-(7aR,11aR)-5,6,7a,8,9,10,11,11a-Octahydro-4-(1-piperazinyl)-benzofuran[2,3-h]quinazolin-2-amine has been identified as an H4 receptor antagonist. It is being studied for its potential role in modulating the H4 receptor, which is implicated in various diseases. By targeting the H4 receptor, this compound may offer a new avenue for the treatment of conditions such as allergies, inflammatory disorders, and certain cancers.
Please note that the provided materials do not specify the exact applications of (±)-(7aR,11aR)-5,6,7a,8,9,10,11,11a-Octahydro-4-(1-piperazinyl)-benzofuran[2,3-h]quinazolin-2-amine. The uses listed above are inferred based on its structural features and potential biological activities. Further research and development are necessary to fully understand its applications and benefits in various industries.
Biological Activity
a987306,cis-4-(piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quin- azolin-2-amine[1], is a selective and potent h4 receptor antagonist [2].h4r is one of 4 known g-protein-coupled receptors (h1, h2, h3 and h4 receptors) of histamine. it is for mediating some physiological functions of histamine [3].in a cell-based ca2+-flux functional assay, a 987306 had no activation to the receptor, but blocked the h4r activation induced by endogenous histamine. a 987306 potently decreased histamine-mediated binding between rat h4-receptor-containing membranes and gtp-γ-[35s] with a kb of 6 nm [3].in sprague-dawley rats, after ip injection, a 987306 had a favorable fractional bioavailability (fip/iv =72%), a half-life of 4.7 h and a cmax of 1.73 μm at a tmax of 0.25 h after dosing. after oral dosing, a 987306 had a moderate fractional oral bioavailability (fpo/iv =26%) with a half-life of 3.7 h and a cmax of 0.30 μm at a tmax of 1.5 h after dosing. the plasma protein binding of a 987306 measured in rats was found to be 59% [3].to human h4r and rat h4r, the ki values of a 987306 are 5.8 nm and 3.4 nm, respectively. a 987306 reduced scratch responses in mice with an ed50 of 0.36 μmol/kg. a 987306 was found to be selective and bear an ic50 > 810 nm for over 100 kinases [3].
references
[1]. vanina a. medina and elena s. rivera. histamine receptors and cancer pharmacology. british journal of pharmacology, 2010, 161:755-767.[2]. m.i. strakhova, c.a. cuff, a.m. manelli, et al. in vitro and in vivo characterization of a-940894: a potent histamine h4 receptor antagonist with anti-inflammatory properties. british journal of pharmacology, 2009, 157:44-54.[3]. huaqing liu, robert j. altenbach, tracy l. carr, et al. cis-4-(piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (a-987306), a new histamine h4r antagonist that blocks pain responses against carrageenan-induced hyperalgesia. j. med. chem., 2008, 51:7094-7098.
Check Digit Verification of cas no
The CAS Registry Mumber 1082954-71-9 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,0,8,2,9,5 and 4 respectively; the second part has 2 digits, 7 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 1082954-71:
(9*1)+(8*0)+(7*8)+(6*2)+(5*9)+(4*5)+(3*4)+(2*7)+(1*1)=169
169 % 10 = 9
So 1082954-71-9 is a valid CAS Registry Number.
1082954-71-9Relevant articles and documents
Cis-4-(piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h] quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia
Liu, Huaqing,Altenbach, Robert J.,Carr, Tracy L.,Chandran, Prasant,Hsieh, Gin C.,Lewis, La Geisha R.,Manelli, Arlene M.,Milicic, Ivan,Marsh, Kennan C.,Miller, Thomas R.,Strakhova, Marina I.,Vortherms, Timothy A.,Wakefield, Brian D.,Wetter, Jill M.,Witte, David G.,Honore, Prisca,Esbenshade, Timothy A.,Brioni, Jorge D.,Cowart, Marlon D.
, p. 7094 - 7098 (2008)
cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h] quinazolin-2-amine, 4 (A-987306) is a new histamine H4 antagonist. The compound is potent in H4 receptor binding assays (rat H 4, Ki = 3.4 nM, human H4 Ki = 5.8 nM) and demonstrated potent functional antagonism in vitro at human, rat, and mouse H4 receptors in cell-based FLIPR assays. Compound 4 also demonstrated H4 antagonism in vivo in mice, blocking H 4-agonist induced scratch responses, and showed anti-inflammatory activity in mice in a peritonitis model. Most interesting was the high potency and efficacy of this compound in blocking pain responses, where it showed an ED50 of 42 μmol/kg (ip) in a rat post-carrageenan thermal hyperalgesia model of inflammatory pain.
