blood brain barrier

Elamipretide (MTP-131) is a mitochondria-targeted antioxidant tetrapeptide (D-Arg-dimethylTyr-Lys-Phe-NH2) that reduces toxic reactive oxygen species (ROS) production and stabilizes cardiolipin, with blood-brain-barrier permeability. It is a potential therapeutic agent in the rare disease of Barnes syndrome.

Carbetocin is an obstetric drug used to control postpartum hemorrhage and bleeding after giving birth.

TAT-Gap19 acetate is a specific inhibitor of connexin43 hemichannel (Cx43 HC). TAT-Gap19 acetate traverses the blood-brain barrier and alleviates liver fibrosis in mice. TAT-Gap19 acetate does not inhibit the corresponding Cx43 GJCs.

Rabies Virus Glycoprotein (TFA), a 29-amino acid-derived cell-penetrating peptide from the Rabies Virus Glycoprotein, can cross the blood-brain barrier (BBB) and enter brain cells.

Certain chronic neurologic disorders, such as Parkinson's disease, are caused by an insufficiency of the neurotransmitter dopamine secondary to the degeneration of substantia nigra dopaminergic neurons. N-(α-Linolenoyl) tyrosine (NALT) is a simple α-amide conjugate between the ω-3 essential fatty acid α-linolenate and the amino acid tyrosine. α-Linolenate is an important precursor to docosahexaenoic acid (DHA), a prominent brain polyunsaturated fatty acid, while tyrosine is the metabolic precursor for neuronal dopamine synthesis. NALT was prepared as a method for enhancing central nervous system (CNS) dopamine content by facilitated transport of the tyrosine precursor across the blood-brain barrier. In experimental rat models of dopamine insufficiency, NALT increased CNS dopamine levels and exhibited an activity profile consistent with an anti-Parkinson's therapeutic agent.

TAT-Gap19 TFA, a Cx mimetic peptide and specific connexin43 hemichannel (Cx43 HC) inhibitor, does not inhibit corresponding Cx43 gap junction channels (GJCs). It crosses the blood-brain barrier and has shown efficacy in alleviating liver fibrosis in mice [1] [2] [3].

γ-Fibrinogen377-395 TFA is an inhibitory peptide derived from fibrinogen, which also functions as a fibrinogen epitope. It effectively blocks microglial activation and impedes fibrin-Mac-1 interactions in vitro. Additionally, it exhibits in vivo efficacy by suppressing experimental autoimmune encephalomyelitis (EAE) in mice. This compound has applications in researching multiple sclerosis (MS) and other neuroinflammatory diseases linked to blood-brain barrier disruption and microglial activation [1].

Galanin-B2 (NAX-5055) demonstrates activity in epilepsy models and possesses the ability to penetrate the blood-brain barrier [1].

Tat-QFNP12 is a peptide that combines a transcriptional transactivator (Tat) transmembrane domain with an inhibitor targeting the interaction between N-Myc downstream regulated gene 2 (NDRG2) and protein phosphatase Mg2+/Mn2+ dependent 1A (PPM1A). This compound effectively mitigates blood-brain barrier endothelial tight junction disruption caused by elevated levels of matrix metalloproteinase-9 (MMP-9), alleviates cerebral edema, and promotes spontaneous activity along with symmetric limb movement in a mouse model of subarachnoid hemorrhage induced by endovascular puncture. These benefits are observed at a dosage of 20 mg/kg.

LSKL TFA (H-Leu-Ser-Lys-Leu-NH2 TFA) is a LAP-TGFβ derivative and a TGF-β1 antagonist that can cross the blood-brain barrier, inhibits the binding of TSP-1 to LAP and reduces renal interstitial fibrosis and liver fibrosis, inhibits subarachnoid fibrosis by inhibiting TSP-1-mediated TGF-β1 activity, prevents the occurrence of chronic hydrocephalus and improves long-term neurocognitive deficits after subarachnoid hemorrhage.

Relamorelin (RM-131) TFA, a pentapeptide ghrelin analog, is a potent and selective agonist for the ghrelin growth hormone secretagogue receptor (GHSR), exhibiting a K_i of 0.42 nM for the GHS-1a receptor. This compound can cross the blood-brain barrier and effectively increases growth hormone levels while promoting faster gastric emptying, showing significant research potential for conditions such as cachexia, gastroparesis, and disorders related to gastric intestinal motility [1] [2] [3] [4] [5].

Cyclotraxin B TFA, a cyclic peptide, is a highly potent and selective non-competitive inhibitor of TrkB, effectively impeding BDNF-triggered TrkB activity without altering BDNF binding affinity, with an IC50 of 0.30 nM. It crosses the blood-brain barrier, demonstrating analgesic and anxiolytic-like behavioral effects [1] [2] [3].

CTAP TFA, a potent and highly selective μ opioid receptor antagonist that effectively crosses the blood-brain barrier, exhibits a significant inhibition concentration (IC50) of 3.5 nM. It demonstrates extraordinary selectivity, being over 1200-fold more specific to μ opioid receptors than to δ opioid (IC50 = 4500 nM) and somatostatin receptors. This compound is primarily leveraged for researching L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction [1] [2].

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.

TAT-NEP1-40 TFA, a blood-brain barrier-permeable peptide, safeguards PC12 cells against oxygen and glucose deprivation (OGD) and fosters neurite outgrowth. Additionally, it enhances neurological outcomes post-ischemia by curtailing apoptosis in ischemic cerebral tissues. This compound has utility in investigating central nervous system (CNS) injuries, encompassing axonal regeneration and functional recuperation following a stroke [1].

SARS-CoV-2-IN-34 (S-20-1) is a broad-spectrum pan-coronavirus (CoV) fusion inhibitor that penetrates the blood-brain barrier and exhibits extensive inhibitory activity against both pseudotyped and authentic SARS-CoV-2, as well as pseudotyped variants of concern (VOCs). It shows high affinity for the receptor-binding domain (RBD) in the S1 and the heptad repeat 1 (HR1) domain in the S2 of the SARS-CoV-2 spike (S) protein, making it a valuable tool for infection research [1].

ANG1009 is an anticancer agent that efficiently crosses the blood-brain barrier. It exhibits cytotoxicity against various tumor cells and can induce cell cycle arrest. ANG1009 is applicable for research in brain cancer.

Nemifitide diTFA (INN 00835 diTFA) is a synthetic pentapeptide that can cross the blood-brain barrier and acts as a potent antidepressant, similar to melanocyte suppressor factor (MIF).

HAIYPRH hydrochloride is a targeting ligand that specifically binds to the transferrin receptor (TfR) and facilitates the transport of nanocarriers across the blood-brain barrier [1].

Type A Allatostatin III (allatostatin 3), a neuropeptide capable of crossing the blood-brain barrier and exhibiting reversibility, suppresses hormone production in juvenile female cockroaches, with applications in pesticide research [1].

NNZ 2591, a synthetic analogue of cyclic glycine-proline (cGP), exhibits oral activity and the ability to cross the blood-brain barrier. This compound demonstrates neuroprotective properties following ischemic brain injury and improves motor function in a rat model of Parkinson's disease. NNZ 2591 holds research potential for ischemic brain injury and Angelman syndrome [1] [2] [3].

GluN1 (359-378), an antibody targeting the N-methyl-D-aspartate receptor (NMDAR), can cross the blood-brain barrier and is used in research on immune-based therapies for anti-NMDAR encephalitis [1].

Biphalin TFA is an opioid peptide analog that penetrates the blood-brain barrier (BBB) and encompasses two active enkephalin pharmacophores. It exhibits high affinity for opioid receptors and demonstrates analgesic effects in acute, neuropathic, and chronic animal pain models. Additionally, Biphalin TFA possesses antiviral, antiproliferative, anti-inflammatory, and neuroprotective properties [1].

Substance P (3-11), an SP fragment peptide capable of crossing the blood-brain barrier (BBB), induces contraction in guinea pig ileum and facilitates chemotaxis in human monocytes [1] [2] [5].