Table 1 Anti-inflammatory marker inhibition and receptor activation parameters of eVDs and epoxy-eVDs.

From: Anti-inflammatory dopamine- and serotonin-based endocannabinoid epoxides reciprocally regulate cannabinoid receptors and the TRPV1 channel

 

NO production IC50 (μM)

IL-6 expression IC50 (μM)

TRPV1 % activationa

TRPV1 EC50 (IC50)b

CB1 % activationc

CB1 EC50b

CB2 % activationc

CB2 EC50b

NADA

0.909 ± 0.076

0.507 ± 0.065

83.8 ± 13.6

962 ± 249

83.9 ± 9.2

0.045 ± 0.01

---

DNBd

14’,15’-epoNADA

0.888 ± 0.135

0.807 ± 0.440

79.7 ± 9.8

156 ± 36

92.3 ± 11.2

0.080 ± 0.03

---

DNBd

NA5HT

2.14 ± 0.06

1.06 ± 0.49

---

(7,650 ± 1,300)

---

DNBd

19.2 ± 3.4

8.80 ± 5.57

14’,15’-epoNA5HT

2.07 ± 0.18

1.56 ± 0.22

23.6 ± 4.4 ---

120 ± 27 (254 ± 38)

99.9 ± 13.1

16.5 ± 11.7

---

DNBd

  1. aPercent activation compared to the Bmaxc of CAP.
  2. bnM.
  3. cPercent activation compared to the Bmaxc of CP-55940.
  4. dDNB: does not activate. Compounds upto 1 μM in concentration do not agonize the receptor and do not antagonize 50 nM of CP-55940.