Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C11H15N5O5 |
| Molecular Weight | 297.2673 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 4 / 4 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=NC2=C(N=CN2[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)C(N)=N1
InChI
InChIKey=AJACDNCVEGIBNA-KQYNXXCUSA-N
InChI=1S/C11H15N5O5/c1-20-11-14-8(12)5-9(15-11)16(3-13-5)10-7(19)6(18)4(2-17)21-10/h3-4,6-7,10,17-19H,2H2,1H3,(H2,12,14,15)/t4-,6-,7-,10-/m1/s1
| Molecular Formula | C11H15N5O5 |
| Molecular Weight | 297.2673 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 4 / 4 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
Approval Year
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 12:04:34 GMT 2023
by
admin
on
Sat Dec 16 12:04:34 GMT 2023
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| Record UNII |
E47DV78P45
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| Record Status |
Validated (UNII)
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| Record Version |
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E47DV78P45
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24723-77-1
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9796227
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DTXSID001316127
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36899
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admin on Sat Dec 16 12:04:34 GMT 2023 , Edited by admin on Sat Dec 16 12:04:34 GMT 2023
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ACTIVE MOIETY |
Biovitrum has completed a first phase 2 study in patients with neuropathic pain. The candidate drug, BVT.115959, is a pH-selective A2A-receptor agonist for the treatment of pain. The results of this first patient study is promising as it shows a high level of safety and tolerability, as well as a positive treatment effect that increased over time. The most important finding in this first phase 2 study is that the unique candidate drug BVT.115959 is very safe and tolerable. Moreover, a positive treatment effect that increased over time was observed although the analysis of the primary variable was not statistically significant. Further analysis of the efficacy data showed statistical significance. The conclusion of these observations is that BVT.115959 has a clear opportunity to show good efficacy and few side-effects in further studies.
BVT.115959 decreases inflammation by activating the adenosine receptor 2A in injured tissue. As a consequence of this, BVT.115959 has a potential to fulfil a great medical need to treat chronic pain without giving rise to central nervous system derived side effects.
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ACTIVE MOIETY |
In contrast, spongosine has demonstrated a diverse bioactivity profile including anti-inflammatory activity, analgesic and vasodilation properties. Investigations into unusual nucleoside production by T. crypta-associated microorganisms using mass spectrometric and spectroscopic techniques has identified a spongosine-producing strain of Vibrio harveyi and several structurally related compounds from multiple strains. These results support a microbial source for the unusual nucleosides originally found in this marine invertebrate, and fermentation of these strains may abrogate the need for sponge collection to acquire these valuable metabolites.
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ACTIVE MOIETY |
Originator: Cambridge Biotechnology; Developer: Swedish Orphan Biovitrum; Class: Analgesic
Mechanism of Action: Adenosine A2 receptor agonist; Highest Development Phase: Discontinued for Inflammatory pain, Neuropathic pain; Most Recent Events: 14 Jan 2010 Biovitrum has merged with Swedish Orphan to form Swedish Orphan Biovitrum, 07 Apr 2008 Efficacy data from a phase II trial in Neuropathic pain released by Biovitrum, 14 Dec 2007 Biovitrum completes a phase II trial in Neuropathic pain in the Czech Republic, Germany and South Africa
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