Berbamine is a natural product extracted from Phellodendron amurense. It acts as a calcium channel blocker and possesses anti-tumor, immunomodulatory, and cardiovascular effects.

Phenoxybenzamine hydrochloride (NCI-c01661) is the hydrochloride salt form of phenoxybenzamine, a synthetic, dibenzamine alpha-adrenergic antagonist with antihypertensive and vasodilatory properties. Phenoxybenzamine non-selectively and irreversibly blocks the postsynaptic alpha-adrenergic receptor in smooth muscle, thereby preventing vasoconstriction, relieving vasospasms, and decreasing peripheral resistance. Reflex tachycardia may occur and may be enhanced by blockade of alpha-2 receptors which enhances norepinephrine release. Phenoxybenzamine is reasonably anticipated to be a human carcinogen.

Calmidazolium chloride (R 24571) is a calmodulin (CaMK) antagonist with a Kd of 3 nM, which inhibits CaM-dependent phosphodiesterase (IC50 = 0.15 μM) and calmodulin-induced activation of erythrocyte Ca2+-transporting ATPase (IC50 = 0.35 μM). It also induces apoptosis in certain cancer cell lines.

Dibucaine (Cinchocaine), a local anesthetic of the amide type, is now usually used for surface anesthesia.

Promethazine (Proazamine) is an analogue of anti-glaucoma prostaglandin (PG) .

Nifedipine (Procardia) is a dihydropyridine calcium channel blocking agent. Nifedipine inhibits the transmembrane influx of extracellular calcium ions into myocardial and vascular smooth muscle cells, causing dilatation of the main coronary and systemic arteries and decreasing myocardial contractility. This agent also inhibits the drug efflux pump P-glycoprotein which is overexpressed in some multi-drug resistant tumors and may improve the efficacy of some antineoplastic agents.

Tanshinone IIA sulfonate sodium (Tanshinone IIA sodium sulfonate) is a water-soluble derivative of tanshinone IIA extracted from Savia miltiorrhiza; a potent negative allosteric modulator of the human purinergic receptor P2X7. Tanshinone IIA sulfonate sodium (12.5 μM) inhibits hypoxia-induced PKG and PPAR-γ downregulation in PASMCs and distal pulmonary arteries of rats.

STO-609 is a specific and cell-permeable inhibitor of the Ca2+/calmodulin-dependent protein kinase kinase (CaM-KK) for recombinant CaM-KKα/KKβ (Ki: 80/15 ng/mL).