Tubulin inhibitor 41 (Compd D19) is a promising lead compound for glioblastoma treatment, known for its ability to penetrate the blood-brain barrier (BBB). It functions as a tubulin inhibitor, inducing G2 M phase arrest, leading to cell apoptosis, and inhibiting the migration of U87 cells [1].
Frakefamide is unable to penetrate the blood-brain-barrier and enter the central nervous system. Frakefamide TFA is a potent analgesic that acts as a peripheral active μ-selective receptor agonist.
Lamivudine (BCH-189) salicylate is an orally active nucleoside reverse transcriptase inhibitor (NRTI) that effectively inhibits the reverse transcriptase activity of both HIV 1 2 and hepatitis B virus. Moreover, it demonstrates the ability to penetrate the central nervous system [1] [2].
WSD0922-FU is a blood-brain-barrier (BBB) penetrable selective inhibitor of epidermal growth factor receptor (EGFR) and various EGFR mutations, including but not limited to the EGFR variant III (EGFRvIII) mutant form, with potential antineoplastic activity. WSD0922-FU is able to penetrate the BBB and specifically targets, binds to and inhibits EGFR and specific EGFR mutations, which prevents EGFR/EGFR mutant-mediated signaling and leads to cell death in EGFR/EGFR mutant-expressing tumor cells. Compared to other EGFR inhibitors that are not able to penetrate the BBB, WSD0922-FU may have therapeutic benefits in brain tumors, such as glioblastoma (GBM) and metastatic CNS tumors.
Frakefamide is a potent analgesic. It acts as a peripheral active μ-selective receptor agonist. Frakefamide is unable to penetrate the blood-brain-barrier and enter the central nervous system.
4-Me-PDTic is a potent and selective Kappa Opioid Receptor Antagonist. 4-Me-PDTic had a Ke = 0.37 nM in a [35S]GTPγS binding assay and was 645- and >8100-fold selective for the κ relative to the μ and δ opioid receptors, respectively. Calculated logBB and CNS (central nervous system) multiparameter optimization (MPO) and low molecular weight values all predict that 4-Me-PDTic will penetrate the brain and pharmacokinetic studies in rats shows that 4-Me-PDTic does indeed penetrate the brain.
Crocin-4, a carotenoid compound found in saffron, possesses potent antioxidant properties and can penetrate the brain. It effectively inhibits the aggregation and deposition of Aβ fibrils, making it useful for Alzheimer's Disease research. Additionally, Crocin-4 demonstrates antitumor and anti-inflammatory activities.
Rho-Kinase-IN-2 (Compound 23) is an orally active and selective inhibitor of Rho Kinase (ROCK), which can penetrate the central nervous system (CNS). It exhibits a high affinity for ROCK2 with an inhibition constant (IC50) of 3 nM. This compound is of potential interest for further investigations in the field of Huntington's disease research [1].
TAT-amide is a cell-penetrating peptide (CPP) that exhibits the ability to enter various cells. CPPs, which are composed of short amino acid sequences, possess the capability to penetrate cell membranes and access intracellular compartments.
Abacavir monosulfate is an orally active, competitive nucleoside reverse transcriptase inhibitor that effectively inhibits HIV replication. Additionally, it exhibits anticancer properties in prostate cancer cell lines, and has the ability to penetrate the blood-brain-barrier and suppress telomerase activity [1] [2] [3].
CB1-IN-2 (Compound 4g) is a potent and selective inhibitor of the CB1 receptor, exhibiting an IC50 value of 0.644 μM. This compound possesses the ability to penetrate the blood-brain barrier and has the potential to induce central nervous system (CNS) side effects similar to Rimonabant [1].
TfR-T12 is a transferrin receptor (TfR) binding peptide that can penetrate the blood-brain barrier (BBB), exhibiting a high binding affinity within the nanomolar (nM) range.
TRPV1 antagonist 3 (Compound 7q) is a highly potent antagonist of the TRPV1 receptor with an IC50 of 2.66 nM against capsaicin. It exhibits selectivity towards its mode of action and is orally bioavailable (with a bioavailability of 60%). Additionally, it can penetrate the central nervous system [1].
CGP 36742 is a selective antagonist of the GABAB receptor that can penetrate the blood-brain barrier after peripheral administration (IC50: 32 μM). It is useful in the treatment of depression.
Phenoprolamine Hydrochloride is an adrenergic α1 receptor antagonist with potent antihypertensive, neuroprotective and cardioprotective effects. Phenoprolamine Hydrochloride inhibits CYP2D and CYP3A activities and down-regulates their mRNA transcription a