AEW-541 is a pyrrolo[2,3-d]pyrimidine derivative small molecular weight kinase inhibitor of the IGF-IR IGF-1R/InsR with IC50 of 150 nM/140 nM in cell-free assays, greater potency and selectivity for IGF-1R in a cell-based assay. In vivo, this orally bioavailable compound inhibits IGF-IR signaling in tumor xenografts and significantly reduces the growth of IGF-IR-driven fibrosarcomas. AEW-541 represents a class of selective, small molecule IGF-IR kinase inhibitors with proven in vivo antitumor activity and potential therapeutic application.

(R)-Alprenolol is a less active stereoisomer of antihypertensive beta-blocker alprenolol. Its activity against beta-adrenoreceptor is 100 times lower than the activity of (S)-alprenolol. In a model of ventricular arrhythmias produced by ligation of the left coronary artery, (R)-alprenolol was effective at 15.5 mg/kg, whereas (S)-alprenolol abolished the ventricular arrhythmia by cumulative dose of 7.5 mg/kg.

(S)-Alprenolol is a more active stereoisomer of antihypertensive beta-blocker alprenolol. Its activity against beta-adrenoreceptor is 100 times greater than the activity of (R)-alprenolol. In a model of ventricular arrhythmias produced by ligation of the left coronary artery, (S)-alprenolol was effective at 7.5 mg/kg, whereas (R)-alprenolol abolished the ventricular arrhythmia by cumulative dose of 15.5 mg/kg. As a most active enantiomer of alprenolol, the compound was used as a tool to study beta-adrenergic receptors.

6-alpha-Naloxol is active metabolite of naloxone. 6-alpha-Naloxol was shown to be neutral antagonist at the mu receptor in vitro, with no affect on cAMP levels or GTPitalic gammaS binding, regardless of morphine pretreatment. It elicits withdrawal behaviour and conditioned place aversion in morphine pretreated rodents.

KMD-3241 (Dehydro Silodosin) is a silodosin metabolite (also known as an impurity of Silodosin). Silodosin is a selective antagonsit of alpha-1a adrenergic receptor which was developed by Kissei Pharmaceutical and approved by FDA under the name Rapaflo for the treatment of signs and symptoms associated with benign prostatic hyperplasia. The affnities of silodosin metabolites, KMD-3241, KMD-3289 and KMD-3295, for alpha1A-AR subtype receptor were equal to or lower than that of silodosin.

(1,2,5,6-tetrahydropyridine-4-yl)methylphosphinic acid (TPMPA) is a competitive antagonist of gamma-aminobutyric acid (GABA)C receptors.

4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine (S1RA, E-52862) is an 1-arylpyrazole class of sigma-1 receptor antagonist. Formalin-induced nociception (both phases), capsaicin-induced mechanical hypersensitivity and sciatic nerve injury-induced mechanical and thermal hypersensitivity were dose-dependently inhibited by systemic administration of S1RA. Occupancy of sigma-1 receptors in the CNS was significantly correlated with the antinociceptive effects. As a mechanistic correlate, electrophysiological recordings demonstrated that pharmacological antagonism of sigma-1 receptors attenuated the wind-up responses in spinal cords sensitized by repetitive nociceptive stimulation. Esteve is developing E 52862 for the treatment of several pain indications, including diabetic neuropathies, chemotherapy-induced neuropathic pain, postherpetic neuralgia, postoperative pain. Phase II development of this first-in-class agent is underway in Romania, Spain and Greece.