. Author manuscript; available in PMC: 2024 May 6.

Published in final edited form as: J Med Chem. 2023 Aug 16;66(16):11027–11039. doi: 10.1021/acs.jmedchem.3c01178

Table 2.

Selected Antitargets and Associated Ligands.

Biological Target	Classification	Associated Deleterious Effects	Mode of Pharmacology	Example Ligand(s)
5-HT_2A	GPCR	Hallucinations, psychedelic-experiences, changes in perception^20–22	Agonism	LSD Psilocin
5-HT _2B	GPCR	Pulmonary arterial hypertension, valve disease ^37,38	Agonism	Fenfluramine Norfenfluramine MDMA
μOR	GPCR	Bradypnea, hypoxemia³⁹	Agonism	Morphine Fentanyl Carfentanil
M₂	GPCR	Reduction in heart rate^23,40	Agonism	Oxotremorine M (non-selective)
hERG	Ion Channel	LQTS^31–36	Inhibition	Cisapride
Ca_V1.2	Ion Channel	LQTS, Brugda Syndrome²⁵	Inhibition	Verapamil (non-selective)
CYP3A4	Cytochrome P40	Various drug-drug interactions^26,41	Inhibition	Mibefradil
MDR1 (ABCB1)	Efflux Pump	Multiple drug resistance (chemotherapy)^42,43	Efflux substrate	Verapamil (inhibitor) Paclitaxel (substrate)