mglu1

Ro0711401 is an agonist of mGlu1 receptor.

L-Glutamic acid monosodium salt (MSG) (Monosodium glutamate) is an activator of mGlu1 receptor.

VU 0469650 is a potent and selective negative allosteric modulator of mGluR1 (IC50 = 99 nM).

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.

DCG-IV is an effective agonist of class II mGluR. DCG-IV has anticonvulsant and neuroprotective effects. The EC50 of mGlu2R and mGlu3R are 0.35 and 0.09 μM, respectively. DCG-IV is also a competitive antagonist of Group I (IC50: mGlu1 / 5R = 389/630 μM) a

VU6033685 is an orally effective positive allosteric modulator (PAM) of mGlu1, capable of positively modulating human mGlu1 and mGlu5, with EC50 values of 39 nM and 3960 nM, respectively. Additionally, VU6033685 inhibits CYP1A2, CYP2C9, and CYP2D6 with IC50 values of 26, 22.3, and 23.8 μM. It reverses amphetamine-induced hyperactivity in rats and protects against MK-801-induced cognitive deficits. VU6033685 demonstrates favorable pharmacokinetic properties in rats, with an oral bioavailability of 42.8%.

A-841720 is a potent, selective, and non-competitive antagonist of the mGlu1 receptor, exhibiting an IC 50 value of 10 nM specifically for the human mGlu1 receptor. It demonstrates a 34-fold greater selectivity for mGlu1 over mGlu5 (IC 50 of 342 nM), with negligible activity across a spectrum of other neurotransmitter receptors, ion channels, and transporters. Additionally, A-841720 possesses analgesic potential within a certain dose range [1] [2].

mGlu1-selective antagonist

LY 456236 hydrochloride (MPMQ hydrochloride) is an mGlu1 receptor antagonist with an ic50 value of 143 nM. LY456236 has selective, non-competitive and oral activity, and can inhibit the hydrolysis of inositol phosphate with IC50 of 0.145 μM. LY 456236 hydrochloride inhibited EGFR with IC50 of 0.91 μM.

Positive allosteric modulator of mGlu1 receptors

TC-N 22A is a strong, selective, oral active mGlu4 forward allosteric regulator (PAM) that can cross the blood-brain barrier. EC50 expression of TC-N 22A in BHK cells expressing human mGlu4 was 9 nM. TC-N 22A showed very low activity against mGlu 1, 2, 3, 5, and 7 receptors in excitation and forward allosteric models (EC50 >10 μM). TC-N 22A can be used in the study of central nervous system diseases.

metabotropic glutamate receptor type 1 (mGlu1) antagonist

Selective mGlu1 antagonist

mGlu1 receptor antagonist

A-794282 is a selective and potent mGlu1 receptor antagonist with analgesic activity and may be useful in the study of neurologic disorders.

R214127 is a new type of mGlu1 receptor high-affinity radioligand.

VU0486321 is a potent mGlu1 PAM with moderate rat PK (CLp = 13.3. mL/min/kg,t1/2 = 54 min), good free fraction (human fu = 0.05, rat fu =0.03) and excellent CNS penetration (Kp = 1.02).

(S)-4CPG ((S)-4-Carboxyphenylglycine) is a competitive mGlu1 receptor antagonist that attenuates nociceptive hypersensitivity and nociceptive abnormalities associated with sciatic nerve constriction injuries in rats, and may be used in the study of neurological disorders.

JNJ16259685 (TN.T 16259685) is a selective mGluR1 antagonist, and inhibits the synaptic activation of mGluR1 in a concentration-dependent manner with IC50 of 19 nM.

YM-202074 is a high affinity, selective metabotropic glutamate receptor type 1 (mGlu1) antagonist. YM-202074 binds an allosteric site of the rat mGlu1 receptor with a Ki of 4.8 nM. It inhibits mGlu1-mediated inositol phosphates production (IC50 = 8.6 nM in rat cerebellar granule cells).

YM 298198 Hydrochloride is a non-competitive antagonist with high affinity and selectivity for mGlu1 receptors (Ki = 19 nM). YM 298198 Hydrochloride is inactive at other mGlu receptor subtypes (mGlu2-7), ionotropic receptors and glutamate transporters (IC50 > 10 μM). It inhibits glutamate-induced IP production more potently than CPCCOEt (IC50 values are 16 nM and 6.3 μM respectively).

FITM is a potent negative allosteric modulator of mGlu1 receptor(Ki : 2.5 nM).

VU6004909 is a potent mGlu5 receptor orthosteric modulator (EC50:25.7nM) that reverses MK801-induced cortical activity enhancement and cognitive dysfunction, and can be used in the study of neurological disorders.