Difference between revisions of "Transformation of TXA2 to TXB2"

From ISMOC
Jump to: navigation, search
(Parameters)
(Parameters)
Line 132: Line 132:
 
|[3H]IONO NT-126, a TXA z antagonist,
 
|[3H]IONO NT-126, a TXA z antagonist,
 
|<ref name="Nakahata1992”>[http://ac.els-cdn.com/S0006899310800137/1-s2.0-S0006899310800137-main.pdf?_tid=b2ab095e-155f-11e7-94f0-00000aab0f26&acdnat=1490888822_58d1d45dc3238dede94e4a2f15cada82 N Nakahata et al. "The Presence of Thromboxane A2 Receptors in Cultured Astrocytes From Rabbit Brain" Brain Res 583 (1-2), 100-104. 1992 Jun 26]</ref>
 
|<ref name="Nakahata1992”>[http://ac.els-cdn.com/S0006899310800137/1-s2.0-S0006899310800137-main.pdf?_tid=b2ab095e-155f-11e7-94f0-00000aab0f26&acdnat=1490888822_58d1d45dc3238dede94e4a2f15cada82 N Nakahata et al. "The Presence of Thromboxane A2 Receptors in Cultured Astrocytes From Rabbit Brain" Brain Res 583 (1-2), 100-104. 1992 Jun 26]</ref>
 +
|-
 +
|1500 ± 500
 +
|mM
 +
|Temperature: 25°C
 +
In vitro
 +
|Hydroxysulfamic acid
 +
[[File:HSA.PNG ‎|center|500px]]
 +
|<ref name="Littlejohn1989”>[http://www.nrcresearchpress.com/doi/pdf/10.1139/v89-243 D. LITTLEJOHN "The dissociation constant and acid hydrolysis rate of hydroxysulfamic acid"  Can. J. Chem. 67, 1596 (1989).]</ref>
 
|-
 
|-
 
|}
 
|}

Revision as of 10:38, 31 March 2017

Return to overview

Thromboxane A2 is a bioactive molecule which affects vasoactivity and promotes thrombosis. It is unstable due to the epoxide functional group, and as a consequence has a short half-life of 20- 30 seconds. The hydrolysis reaction results in the generation of biologically inactive TXB2.

Reaction

R6 TXA2 - TXB2.jpg

Chemical equation

 FA \rightleftharpoons AA

Rate equation

Parameters

Association Rate Constant (Kf)
Value Units Conditions Substrate Reference
3.7e3 ± 0.1e3 M-1 s-1 NaCl04 (0.1 - 0.2 M)

Temperature: 25°C

3 [1]
8.7e3 M-1 s-1 KCl (1 M)

Temperature: 25°C

3 [1]
1.1e4 ± 0.1e4 M-1 s-1 NaCl04 (0.1 - 0.2 M)

Temperature: 25°C

4 [1]
2.4 e4 M-1 s-1 KCl (1M)

Temperature: 25°C

4 [1]
3.7e3 ± 0.1e3 M-1 s-1 NaCl04 (0.1 - 0.2 M)

Temperature: 25°C

5 [1]
3.6 ± 0.2 M-1 s-1 NaCl04 (0.1 - 0.2 M)

Temperature: 25°C

6 [1]
1.7 ± 0.1 M-1 s-1 NaCl04 (0.1 - 0.2 M)

Temperature: 25°C

7 [1]
26.7 ± 0.9 M-1 s-1 NaCl04 (0.1 - 0.2 M)

Temperature: 25°C

8 [1]
35 M-1 s-1 KCl (1M)

Temperature: 25°C

8 [1]
Dissociation Rate Constant (Kr)
Value Units Conditions Substrate Reference
Dissociation Constant
Value Units Conditions Substrate Reference
0.000038 mM Temperature: 35°C

Vector:Mosquito

Note: "In solution, it undergoes rapid hydrolysis to form TXB2, a stable but physiologically inactive compound." - therefore they used stable analogues.

carbocyclic TXA2 (analogue of TXA2) [2]
0.00000023 mM Temperature: 35°C

Vector:Rabbit cultured astrocytes

Note: "In solution, it undergoes rapid hydrolysis to form TXB2, a stable but physiologically inactive compound." - therefore they used stable analogues.

[3H]IONO NT-126, a TXA z antagonist, [3]
1500 ± 500 mM Temperature: 25°C

In vitro

Hydroxysulfamic acid
HSA.PNG
[4]

Related Reactions

References