potentiator

Bradykinin potentiator-5 is a peptide inflammatory mediator, causes blood vessels to dilate (enlarge), and therefore causes blood pressure to fall.

NMDA receptor potentiator-1 (Compound 1368) is a subunit-selective NMDA receptor enhancer with IC50 values of 4 μM and 5 μM for NR2C and NR2D expression, respectively.

Bradykinin Potentiator C, a potent inhibitor of angiotensin-converting enzyme (ACE) with an inhibitory concentration (IC 50) of 7.1 μM for rabbit lung ACE, is regarded as a prototype for functional peptides [1].

Bradykinin Potentiator B (also known as Bradykinin Potentiating Peptide B), derived from the venom of Agkistrodon halys blomhoffi, serves as a potent ACE inhibitor. It effectively inhibits the activity of bradykinin inhibitory peptidase [1].

OV-potentiator-28 is a potentiator of cancer virotherapy. OV-potentiator-28 significantly enhances virus replication-associated luciferase expression, specifically in tumors.

LY450108 is a potentiator of the AMPA receptor that can be used in Parkinson's disease studies.

Chromenone 1 is a potent potentiator of osteogenic bone morphogenetic protein (BMP). Chromenone 1 induces a pronounced, kinase-independent, negative TGFβ feedback that enhances nuclear BMP-Smad signaling outputs.

Ivacaftor (VX-770) (VX-770) is a potentiator of CFTR targeting G551D-CFTR (EC50: 100 nM) and F508del-CFTR (EC50: 25 nM) in Fisher rat thyroid cells, respectively.

NG-012, a nerve growth factor (NGF) potentiator, was isolated from the culture broth of Penicillium verruculosum F-4542. It enhances neurite outgrowth as induced by NGF in the rat pheochromocytoma cell line (PC12) [1].

SPR741, formerly NAB741 (12), is a cationic peptide derived from polymyxin B and is one such potentiator molecule that is under development for the treatment of serious Gram-negative bacterial infections.

Indiplon is a short-acting hypnotic with high-affinity allosteric potentiator of GABAA responses that demonstrates preference for alpha1 subunit-containing GABAA receptors.

Icenticaftor (QBW251) is an orally active potentiator of CFTR channel.

Dirocaftor (PTI-808) is a CFTR potentiator that augments CFTR protein function via the activation of chloride channels. Dirocaftor holds potential utility for research pertaining to cystic fibrosis (CF).

HBT1 is an AMPA receptor potentiator that induces production of brain-derived neurotrophic factor (BDNF) and exhibits little agonistic effect in primary neurons. HBT1 binds to ligand-binding domain of AMPA-R in glutamate dependent manner.

CIQ is a subunit-selective potentiator of NMDA receptors containing the NR2C or NR2D subunit. EC50 value: 2.7 μM for NR2C and 2.8 μM for NR2D.

Mip-IN-1 (S,S-28i) is a novel inhibitor derived from rapamycin targeting the macrophage infectivity potentiator (Mip) proteins. It exhibits potent anti-enzymatic effects against Mip proteins from Neisseria meningitidis and Neisseria gonorrhoeae, significantly enhancing macrophage bactericidal efficacy [1].

VU-29 is a positive allosteric mGlu5 receptor modulator with EC50=9 nM and Ki=244 nM for rmGluR5. It is selective for mGluR5 relative to other mGluR subtypes (EC50: rmGluR1/rmGluR2=557 nM/1.5 μM; hmGluR4=154 nM).

Cinepazide is a vasodilator used for the treatment of cardiovascular, cerebrovascular, and peripheral vascular diseases. Cinepazide acts as a potentiator of adenosine A2 receptors.

TAK-137 is a novel AMPA receptor potentiator with little agonistic effect, producing antidepressant-like effect without causing psychotomimetic effects.

SPR741 TFA (NAB741 TFA), a cationic peptide derived from polymyxin B, acts as a potentiator molecule that enhances the permeability of Gram-negative bacteria's outer membrane, thereby facilitating the treatment of severe Gram-negative bacterial infections. This compound effectively inhibits multidrug-resistant Gram-negative bacteria and, when combined with antibiotics, broadens their spectrum of activity [1] [2].

VU10010 (VU 10010) is allosteric potentiator of M4 acetylcholine receptors.

TG3-95-1 is an EP2 allosteric potentiator agent.

SPR741 TFA (NAB741 TFA) is a cationic peptide derived from polymyxin B and is a potentiator molecule.

allosteric potentiator of mGlu5

GLPG1837 (ABBV-974) is an effective CFTR potentiator, with EC50s of 3 nM and 339 nM for F508del and G551D CFTR, respectively.

653-47 acts as a potentiator significantly enhancing the inhibitory activity of 666-15 on the cAMP-response element binding protein (CREB), while it also exhibits mild CREB inhibitory properties itself, with an IC50 value of 26.3 μM [1].

Ivacaftor hydrate is an orally bioavailable CFTR potentiator. It also is used for cystic fibrosis treatment.

5-MPEP is a neutral allosteric site ligand of the metabotropic glutamate receptor subtype 5 (mGlu5), blocking the effects of both the allosteric antagonist MPEP and potentiator CDPPB.

Allosteric potentiator of α7, α4β2 and α4β4 nAChRs

Galanthamine hydrobromide (Galantamine hydrobromide), a long-acting and centrally active AChE inhibitor (IC50:410 nM), is an allosteric potentiator at neuronal nicotinic ACh receptors.

Mibampator (LY451395) is an effective and selective AMPA receptor potentiator.

HUHS2002 is a free fatty acid derivative that works as a potentiator of GluA1 AMPA receptor responses and α7 ACh receptor responses.

Cyclothiazide is a benzothiadiazide that acts as a potentiator of AMPA receptorsthat potently inhibits AMPA receptor desensitization, positively modulating its response to glutamic acid (EC50 = 3.8 M).

SBI-0061869 is a potentiator of metabotropic glutamate receptors. It was used against neurological and psychiatric disorders.

653-47 hydrochloride is a potentiator, significantly potentiates the cAMP-response element binding protein (CREB) inhibitory activity of 666-15. It is also a very weak CREB inhibitor with IC50 of 26.3 μM.

AM1488 is a potent, orally active glycine receptor ( GlyR ) potentiator (hGlyRα3 EC 50 =0.45 μM) [1] [2].

NSC339614 potassium is a selective GluN1/GluN2C and GluN1/GluN2D receptors potentiator.

VU0152099 is a potent and selective M4 mAChR allosteric potentiator(EC50 = 380 ± 93 nM).

DNAC-1 is against Gram-positive and Gram-negative pathogens potentiator of β-lactam activity.

S07-2001 enhances Doxorubicin against cancer cells activity, which can be used as a chemotherapeutic potentiator for cancer drug resistance. S07-2001 is a potent and selective inhibitor of aldo-keto reductase 1C3 (AKR1C3) with an IC 50 value of 2.08 μM [1].

UBP646 is a GluN1/GluN2 receptors potentiator.

Biphenylindanone A is a selective potentiator of human mGluR2 (hmGluR2),and for the treatment of neurological disorders.

LY2607540 is a metabotropic glutamate 2 potentiator with potential anxiolytic/antidepressant properties (EC(50) = 23 and 13 nM, respectively).

CP-628006 is a small molecule CFTR potentiator that effectively restores ATP-dependent channel gating to G551D-CFTR, the mutant form found in cystic fibrosis.

Polygodial (Tadeonal) is an antifungal potentiator and an antibiotic, particularly against Saccharomyces cerevisiae, Candida utilis, and Sclerotinia libertiana.

LY503430 is a AMPA receptor potentiator with oral activity. LY503430 has both nootropic and neuroprotective effects, reducing brain damage caused by 6-hydroxydopamine or MPTP.

KRAS G13D peptide, a 25-mer sequence, is derived from the KRAS activating oncogene mutation and serves as an immune potentiator. This peptide possesses immunogenic properties and can be utilized for the development of a KRAS vaccine.

DETQ, a selective, allosteric, and orally active potentiator of the dopamine D1 receptor (Dopamine Receptor), enhances cAMP production in HEK293 cells expressing the human D1 receptor, achieving an EC50 of 5.8 nM and a K b of 26 nM. It demonstrates approximately 30-fold reduced potency at rat and mouse D1 receptors and shows no activity at the human D5 receptor [1].

Allosteric potentiator at the adenosine A1 receptor

Pesampator (PF-04958242) is a potent, highly selective positive allosteric modulator of the AMPA receptor, also known as an AMPA potentiator, demonstrating an EC50 of 310 nM and a Ki of 170 nM [1].