positive allosteric modulator

V-0219 is a positive allosteric modulator of GLP-1 and can be used in studies about obesity-associated diabetes.

BMT-145027 is a positive allosteric modulator of mGluR5 without inherent agonist activity (EC50 = 47 nM).

CPPHA, a positive allosteric modulator of glutamate receptors mGluR5 and mGluR1, is commonly used in development for central nervous system diseases.

Tecalcet Hydrochloride (R-568 hydrochloride) is an allosteric and positive modulator of the calcium-sensing receptor(CaSR). Tecalcet Hydrochloride increases the sensitivity to the activation of extracellular Ca2+.

S 18986 is a selective, orally active, brain-penetrant positive allosteric modulator of AMPA-type receptors that enhances cognition in rodents by inducing the release of noradrenaline and acetylcholine in the rat hippocampus, subsequently improving object-recognition memory.

Positive allosteric modulator of GABAA receptors

JNJ-39393406 is an α7 nicotinic acetylcholine receptor positive allosteric modulator for the study of tobacco dependence and Alzheimer's disease.

GNE-8324 is a GluN2A selective positive allosteric modulator that selectively enhances NMDAR-mediated synaptic responses in inhibitory, but not excitatory, neurons.GNE-8324 is used in the study of neurological disorders.

VU0364770 (VU 0364770)(EC50=1.1 μM), a positive allosteric modulator(PAM) of mGlu4, shows insignificant activity at 68 other receptors, including other mGlu subtypes.

6-Methoxyflavanone (6-MeOF) is a positive allosteric modulator of the GABA response in human recombinant GABA A receptors, exhibiting antianxiety and anti-inflammatory properties, and is used to alleviate cisplatin-induced neuropathic pain.

GNE-5729 is a positive allosteric modulator of NMDAR with the advantage of crossing the blood-brain barrier and being orally available, with EC50 values of 37 nM, 4.7 μM and 9.5 μM for GluN2A, GluN2C and GluN2D, respectively, and can be used for the study of neurological and psychiatric disorders.

E1R is a positive sigma-1 receptor (Sig1R PAM) allosteric modulator. It has a cognition-enhancing activity.

(2R,3S)-E1R (Compound 2c) is an enantiomer of E1R. (2R,3R)-E1R is a sigma-1 receptor positive allosteric modulator for treating cognition and memory disorders.

(2S,3S)-E1R (Compound 2d) is an enantiomer of (2R,3R)-E1R, a sigma-1 receptor positive allosteric modulator for the treatment of cognition memory disorders.

CDPPB is a modulator of mGluR5 positive allosteric(with an EC50 of 27 nM in Chinese hamster ovary cells expressing human mGluR5).

Ro 67-7476 is a positive allosteric modulator of mGlu1 receptors. No activity at human mGlu1 receptors. Potentiates glutamate-induced calcium release with EC 50 of 60.1 nM.

4-CMTB is a selective agonist of FFA2 and GPR43.It also is a positive allosteric modulator (pEC50=6.38).

AZD-8529 mesylate is a highly selective, and orally bioavailable positive allosteric modulator of mGluR2 (EC50: 285 nM). It shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.

VU 0365114 is a positive allosteric modulator of mAChR M5 (EC50: 2.7 μM).

GT 949 is a selective excitatory positive allosteric modulator of amino acid transporter-2 (EAAT2) with an EC50 of 0.26 nM.

Org-26576 is a positive allosteric modulator of the AMPA receptor.

VU0467154 is a positive allosteric modulator of the M4 muscarinic acetylcholine receptor (M4 mAChR).

CX516 (Ampalex), an ampakine and nootropic, acts as an AMPA receptor positive allosteric modulator as a therapy for Alzheimer's disease, schizophrenia and mild cognitive impairment (MCI).

L-838417 D9 (C-21191) is a novel deuterated subtype-selective GABAA positive allosteric modulator, acting as a partial agonist at α2, α3 and α5 subtypes[1].