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Chemical Structure| 33458-93-4 Chemical Structure| 33458-93-4

Structure of AH 6809
CAS No.: 33458-93-4

Chemical Structure| 33458-93-4

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AH 6809 is an EP and DP receptor antagonist with nearly equal affinity for the cloned human EP1, EP2, EP3-III, and DP1 receptors.

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Product Details of AH 6809

CAS No. :33458-93-4
Formula : C17H14O5
M.W : 298.29
SMILES Code : O=C(C1=CC(C2=O)=C(OC3=C2C=CC(OC(C)C)=C3)C=C1)O
MDL No. :MFCD08056083
InChI Key :AQFFXPQJLZFABJ-UHFFFAOYSA-N
Pubchem ID :119461

Safety of AH 6809

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319-H335
Precautionary Statements:P261-P264-P271-P280-P302+P352-P304+P340-P305+P351+P338-P312-P332+P313

Related Pathways of AH 6809

GPCR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
mouse bladder smooth muscle cells 10 μM AH-6809 (10 μM) significantly reduced the PGE2 (50 μM)-induced change in bladder smooth muscle tone (by 23.7 ±4.4%) but had no significant effect on the frequency of phasic contractions (reduced by 9.7 ±4.7%). Br J Pharmacol. 2012 Jan;165(2):401-13
guinea-pig tracheal smooth muscle 10 μM 30 min To assess the effect of AH-6809 on insulin-induced contractions, results showed AH-6809 strongly reduced insulin-induced contractions Br J Pharmacol. 2007 Jan;150(2):136-42
guinea-pig tracheal smooth muscle 0.2-5 μM 15 min pre-incubation Antagonized contraction by 17-phenyl-ω-trinor PGE2, pA2=7.35 Br J Pharmacol. 1992 Feb;105(2):271-8
guinea-pig ileum longitudinal smooth muscle 2 μM Blocked EP1 receptor-mediated contraction, pA2=7.08 Br J Pharmacol. 1992 Feb;105(2):271-8
human umbilical vein rings 1 μM 30 min To evaluate the effect of AH 6809 on PGF2a-induced contraction responses, results showed AH 6809 did not exhibit antagonistic effects Br J Pharmacol. 2003 Aug;139(8):1409-16
adult pig brain microvessel membranes 10 µM 30 min AH6809, as an EP1 receptor antagonist, significantly inhibited the binding of [3H]-PGE2 to adult pig brain microvessel membranes by 82-91%. Br J Pharmacol. 1994 May;112(1):59-64
newborn pig brain microvessel membranes 10 µM 30 min AH6809, as an EP1 receptor antagonist, significantly inhibited the binding of [3H]-PGE2 to newborn pig brain microvessel membranes by 82-91%. Br J Pharmacol. 1994 May;112(1):59-64
guinea-pig trachea epithelium-intact strips 10 μM 20 min To evaluate the effect of EP1/EP2 receptor antagonist on bradykinin-induced relaxation, results showed AH 6809 did not significantly affect BK-induced relaxation. Br J Pharmacol. 2005 Jul;145(6):740-50
Guinea-pig tracheal cholinergic nerves 10 μM 30 min To evaluate the effect of AH 6809 on the inhibition of EFS-induced [3H]ACh release by 8-iso-PGE1 and 8-iso-PGE2. Results showed AH 6809 itself had no significant inhibitory effect on cholinergic transmission and did not antagonize the inhibitory actions of 8-iso-PGE1 or 8-iso-PGE2. Br J Pharmacol. 2004 Feb;141(4):600-9
guinea pig tracheal smooth muscle cells 10 µM 30 min To investigate the effect of AH-6809 on growth factor-induced contractions, results showed AH-6809 almost completely abolished growth factor-induced contractions Respir Res. 2005 Jul 27;6(1):85
Rabbit pulmonary smooth muscle cells (PSMC) 3 μM To investigate the antagonistic effect of AH 6809 on EP1 receptors and its impact on iloprost-induced vasodilation. Results showed that AH 6809 significantly enhanced the vasodilatory effect of iloprost. Respir Res. 2007 Jan 26;8(1):4

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rats Freely moving rats Continuous infusion into the third ventricle 2.1, 6.3, or 21 pmol/min From 2300 to 0500 hr During the infusion at 21 pmol/min, wakefulness decreased to 82%, and SWS and PS increased to 122% and 161%, of the respective baseline values. These changes can be explained by AH 6809 antagonizing the endogenous PGE2 that acts to augment wakefulness in the brain. Proc Natl Acad Sci U S A. 1989 Jul;86(14):5666-9

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.35mL

0.67mL

0.34mL

16.76mL

3.35mL

1.68mL

33.52mL

6.70mL

3.35mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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