penetrate

Octocrylene (Octocrilene) is used as an ingredient in sunscreens and cosmetics. This organic compound can penetrate into the skin where it acts as a photosensitizer. This results in an increased production of free radicals under illumination.

Ebastine (Kestine) (trade names Evastin, Kestine, Ebastel, Aleva) is a non-sedating H1 antihistamine. It does not penetrate the blood-brain barrier and thus allows an effective block of the H1 receptor in peripheral tissue without a central side effect, i. e not causing sedation or drowsiness.

Keratin hydrolyzed is a processed form of keratin that allows it to penetrate the hair cuticle.

LY2940094 (LY-2940094) decreases ethanol self-administration in animal models. LY2940094 is an effective, selective, and orally available nociceptin receptor antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM).

IU1(IC50=4.7 μ M), a reversible, specific human USP14 proteasome inhibitor, can penetrate the cell.

VU0361737 (ML-128) is a specific positive allosteric modulator (PAM) of the mGlu4 receptor with an EC50 of 240 nM for human receptors and 110 nM for rat receptors. It exhibits weak activity at mGlu5 and mGlu8 receptors and is inactive at mGlu1, mGlu2, mGlu3, mGlu6, and mGlu7 receptors. The compound can penetrate the CNS.

A 1070722 is a potent and selective GSK-3 inhibitor, exhibiting high affinity for both GSK-3α (Ki = 0.6 nM) and GSK-3β (Ki = 0.6 nM). It can penetrate the blood-brain barrier (BBB) and accumulate in brain regions, indicating potential use as a PET radiotracer for quantifying GSK-3 in the brain.

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.

Frakefamide, a potent analgesic, functions as a peripheral active μ-selective receptor agonist and cannot penetrate the blood-brain barrier to enter the central nervous system.

ICA-105665 (PF-04895162) is a potent and orally active opener of neuronal Kv7.2 7.3 and Kv7.3 7.5 potassium channels. ICA-105665 had low cytotoxic potential in human hepatocytes but inhibited liver mitochondrial function and bile salt export protein (BSEP) transport (IC50 of 311 μM). ICA-105665 can penetrate the central nervous system (CNS) and has antiseizure effects [1][2][3][4].

Phosphoenolpyruvic acid tricyclohexylammonium salt (PEP 3 CHA) is a functional carbohydrate metabolite with cytoprotective and anti-oxidative activity. Phosphoenolpyruvic acid tricyclohexylammonium salt is able to penetrate the cell membrane.

SB-277011 dihydrochloride is a potent, selective, orally bioavailable and brain penetrate antagonist of dopamine D3 receptor(pKis of 8.0, 6.0, <5.2 and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively).

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.

Lactacystin is a natural non-peptide proteasome inhibitor and highly specific anticancer drug that controls the UPS of cellular protein turnover and inhibits alkaline cell proliferation, and is able to be used as a model for studying dementia, induces neurite outgrowth and transiently elevated levels of cAMP, inhibits angiogenesis, triggers apoptosis in glioma cells, and can penetrate the blood-brain barrier (BBB).

D5R Agonist 1 (Compound 5j) is a selective, orally active partial agonist of the D5 receptor that can penetrate the blood-brain barrier (EC50: 269.7 nM). It has been demonstrated to enhance cognitive abilities in a scopolamine-induced amnesia model.

RTI-122 is an effective GPR88 agonist with good metabolic stability (half-life of 5.8 hours in mice) and a cAMP EC50 of 11 nM. It can penetrate the blood-brain barrier and is utilized in research related to excessive drinking.

MZ82, a derivative of Ko 143, is a potent inhibitor of ATP-binding cassette sub-family G member 2 (ABCG2 BCRP), with an IC50 of approximately 23 nM. Compared to Ko 143, MZ82 exhibits significantly enhanced metabolic stability in liver microsomes and shows marked improvement in mice, along with the ability to penetrate the brain.

Zotiraciclib (also known as TG02 and SB1317) is an innovative small-molecule compound with potent inhibitory effects on CDK, JAK2, and FLT3. By inhibiting cyclin-dependent kinase 9 (CDK9) and depleting Myc, it serves as a treatment for cancers that can penetrate the blood-brain barrier. Zotiraciclib is one of the numerous CDK inhibitors under investigation; other compounds targeting CDK9, utilized for treating acute myeloid leukemia, include alvocidib and atuveciclib. Myc overexpression is a known factor in many cancers, with 80% of glioblastomas exhibiting this characteristic.

SKQ1, also known as Visomitin or plastoquinonyl decyltriphenyl phosphonium (PDTP), is a potent mitochondrial-targeted antioxidant. As the active pharmaceutical ingredient (API) in Visomitin eye drops, SKQ1 exhibits various biomedical activities: (1) prevents impairment of long-term potentiation in rat hippocampal slices caused by amyloid β-protein; (2) reverses aging-related biomarkers in rats; (3) slows age-related degenerative changes in the retinas and choroid of Wistar and OXYS rats; (4) extends the lifespan of male rodents in LP or SPF conditions. SKQ1 can penetrate cell membranes and is proposed for use in anti-aging therapies. Clinical trials for SKQ1 are currently underway in Russia to treat glaucoma. For convenience, SKQ1 is provided as an ethanol-water (1:1, v v) solution at a concentration of 200 mg mL.

Ir(III) Octaethylporphine chloride is a synthetic porphyrin primarily used as a potent catalyst for intramolecular C-H insertion. Additionally, Ir(III) Octaethylporphine chloride participates in C-O bond cleavage reactions of primary alcohols. When combined with histidine-functionalized peptides, this compound can penetrate cells and sense intracellular O2 concentration.

TNIR7-1A is a fused cycloheptatriene-BODIPY derivative that is optimized for near-infrared (NIR) imaging characteristics (Ex Em = 600 774 nm in PBS) and exhibits high affinity and specificity for neurofibrillary tangles (NFT) in vitro. Additionally, TNIR7-1A can effectively penetrate the blood-brain barrier.

DBPR116 is a prodrug of BPRMU191 that can penetrate the blood-brain barrier. It significantly enhances the delivery efficiency of drugs targeting the central nervous system. When combined with the antagonist Naltrexone, DBPR116 demonstrates superior safety and analgesic effects compared to morphine in various in vivo pharmacological studies, including thermal pain models, cancer pain models, constipation, sedation, psychological dependence, heart rate, and respiratory frequency. As a strategy for peripheral administration, DBPR116 effectively alleviates pain while reducing adverse effects, showing promise as a safer opioid analgesic.

ASM-IN-3 (Compound 21b) is a selective acid sphingomyelinase (ASM) inhibitor that can penetrate the blood-brain barrier, with an IC50 of 3.37 μM against purified human ASM. By inhibiting ASM activity in the hippocampus and promoting neurogenesis, ASM-IN-3 alleviates depressive-like behavior in reserpine-induced depressive rats.

Lu 25-077 is a pharmacologically active N-demethylated metabolite of Lu 25-109 that can penetrate the blood-brain barrier. Lu 25-109 functions as a partial M1 agonist and an M2 M3 antagonist. Lu 25-077 is applicable in neuroscience research.