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. 2023 Aug 24;28(17):6236. doi: 10.3390/molecules28176236

Table 2.

Names, structures, and inhibition constants of cathinones as human 5-HT2AR ligands compiling the TR.

Name
(Number)
P (Mechanism) a
Compound’s
Structure
pKi Ref. Name
(Number)
P (Mechanism) a
Compound’s
Structure
pKi Ref.
Cathinone and its derivatives Naphyrone
(13) FA
graphic file with name molecules-28-06236-i020.jpg 4.96 [34]
Cathinone
(1) AG a
graphic file with name molecules-28-06236-i021.jpg 6.00 [34] MDPV
(14) FA
graphic file with name molecules-28-06236-i022.jpg 4.88 [34]
Flephedrone
(2) AG
graphic file with name molecules-28-06236-i023.jpg 6.00 [34] Pyrovalerone
(15) FA
graphic file with name molecules-28-06236-i024.jpg 4.88 [34]
Mephedrone
(3) AG
graphic file with name molecules-28-06236-i025.jpg 5.68 [34] MDPPP
(16) FA
graphic file with name molecules-28-06236-i026.jpg 4.20 [21]
Methcathinone
(4) AG
graphic file with name molecules-28-06236-i027.jpg 5.23 [34] Benzo[d][1,3]dioxole-based SCs
4-Bromomethcathinone
(5) IA/FA
graphic file with name molecules-28-06236-i028.jpg 5.20 [21] MDBD
(17) AG
graphic file with name molecules-28-06236-i029.jpg 5.20 [34]
3-Bromomethcathinone
(6) IA/FA
graphic file with name molecules-28-06236-i030.jpg 5.00 [21] MDMA
(18) AG
graphic file with name molecules-28-06236-i031.jpg 5.11 [34]
2-Fluoromethcathinone
(7) IA/FA
graphic file with name molecules-28-06236-i032.jpg 5.00 [21] Butylone
(19) AG
graphic file with name molecules-28-06236-i033.jpg 4.88 [34]
2-(Trifluoromethoxy)
-methcathinone
(8) IA/FA
graphic file with name molecules-28-06236-i034.jpg 5.00 [21] Ethylone
(20) AG
graphic file with name molecules-28-06236-i035.jpg 4.88 [34]
Pyrovalerone-based SCs MDEA
(21) AG
graphic file with name molecules-28-06236-i036.jpg 4.88 MDEA
AG (21)
α-PPP
(9) IA/FA
graphic file with name molecules-28-06236-i037.jpg 5.60 [21] Methylone
(22) AG
graphic file with name molecules-28-06236-i038.jpg 4.88 [34]
4-Methyl-α-PPP
(10) IA/FA
graphic file with name molecules-28-06236-i039.jpg 5.50 [21] SCs ’ precursors
4-Bromo-α-PPP
(11) IA/FA
graphic file with name molecules-28-06236-i040.jpg 5.40 [21] Amphetamine
(23) AG
graphic file with name molecules-28-06236-i041.jpg 4.88 [34]
3-Bromo-α-PPP
(12) IA/FA
graphic file with name molecules-28-06236-i042.jpg 5.00 [21] Methamphetamine
(24) AG
graphic file with name molecules-28-06236-i043.jpg 4.88 [34]

a Pharmacology: AG—agonist, IA—inverse agonist, PA—partial agonist, FA—full antagonist.