subtype

BIBO3304 TFA is an effective, orally active, and selective neuropeptide Y (NPY) Y1 receptor antagonist (IC50:0.38 and 0.72 nM for the human and the rat Y1 receptor).

GFB-8438 is a potent and subtype selective inhibitor of TRPC5(IC50s of 0.18 and 0.29 μM of hTRPC5 and hTRPC4, respectively).

Flindokalner (BMS-204352) is a potassium channel modulator and a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. It is also a positive modulator of large conductance calcium-activated K channels (BKca) and displays negative modulatory activity at Kv7.1 channels (Ki = 3.7 μM). Additionally, Flindokalner acts as a negative modulator of GABAA receptors and demonstrates anxiolytic efficacy in vivo.

Luzindole (N-0774) is a selective melatonin receptor antagonist that inhibits experimental autoimmune encephalomyelitis and exhibits antidepressant-like activity. It preferentially targets MT2 (Mel1b) over MT1 (Mel1a), with Ki values of 10.2 nM for human MT2 and 158 nM for MT1.

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

Difamilast is an inhibitor of phosphodiesterase IV.

Radioprotectin-1 is a selective agonist of LPA2 with EC50 of 25 nM for murine LPA2 GPCR and exerts radioprotective and radiomitigative action.

Camonagrel is a compound with inhibitory effects on Prostaglandin E2 (PGE2).

ETHYL 2-AMINO-4-METHYL-5-PHENYLTHIOPHENE-3-CARBOXYLATE targets the prostaglandin E2 receptor EP2 subtype (human)

HEMADO is a potent and selective agonist of the adenosine A3 receptor [Ki: 1.1 nM at the human A3 subtype].

Afloqualone (HQ-495) is a quinazolinone family GABAergic drug that acts as an agonist of the β subtype of the GABAa receptor, exhibiting sedative and muscle-relaxant effects.

PP7 is a potent inhibitor of PB1-PB2 interaction(IC50 of 8.6 μM).

(R)-Terazosin is an active R-enantiomer of Terazosin and a potent antagonist of α1-adrenoceptor [(α1a, α1b, and α1d-adrenoceptor] with Ki values of 6.51 nM, 1.01 nM, and 1.97 nM, respectively).

Ozanimod (RPC-1063) (RPC1063) is a specific oral S1P Receptor 1 modulator. Ozanimod has been used in trials studying the treatment of Crohn's Disease, Ulcerative Colitis, Multiple Sclerosis, and Relapsing Multiple Sclerosis.

Sotagliflozin (LP-802034) is an orally bioavailable inhibitor of the sodium-glucose co-transporter subtype 1 (SGLT1) and 2 (SGLT2), with potential antihyperglycemic activity.

Rivanicline 2HCl is a selective neuronal nicotinic receptor inhibitor with a high affinity for the α4β2 subtype.

UB 165 fumarate is an agonist of the nAChR, a partial agonist of the α4β2 subtype, and a full agonist of the α3β2 subtype, with a Ki value of 0.27 nM for binding to [3H]-nicotine measured in rat brain.

SIB 1553A is an orally available and selective agonist of nicotinic acetylcholine receptors (nAChRs), which are subtype-selective ligands for nicotinic acetylcholine receptors.SIB-1553A is a cognitive enhancer that may be used in the study of neurodegenerative-related diseases such as Alzheimer's disease.

BMY-27709 is an influenza virus growth inhibitor with an IC50 value of 3-8 μM against A/WSN/33 virus growth and demonstrates inhibitory activity against certain subtypes of influenza viruses. BMY-27709 acts early in H1 and H2 virus infections by inhibiting hemagglutinin proteins but has no effect on H3 subtype viruses and influenza B/Lee/40 viruses.

ONO-8713 is a selective prostaglandin E receptor subtype EP1 antagonist used to study diseases of the biblical system and metabolism-related diseases.

Cyclazosin HCl is a subtype-selective α-adrenergic receptor antagonist that competitively antagonizes norepinephrine-induced α(1B)-adrenergic receptor contraction and can be used to study non-arteritic ischemic optic neuropathy and other neurological diseases.

SSR 180 is a potent and subtype-selective α7 agonist with applications in the study of Alzheimer;s disease and schizophrenia.

Clozapine (HF 1854) is a tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A/2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity.

Moxonidine (BDF5895) is a selective agonist at the imidazoline receptor subtype 1, acting as an antihypertensive drug.