v1a

LIT-001 improves social interaction in a mouse model of autism.It is the first nonpeptide oxytocin receptor agonist with EC50 of 55 nM and Ki of 226 nM.

L-371,257 is a competitive antagonist of oxytocin receptor with pA2 of 8.4 and Ki of 19 nM. L-371,257 shows a Ki of 3.7 nM for vasopressin receptor 1a.

VNA-932 is an agonist of the vasopressin V2-receptor (IC50: 80.3 nM and 778 nM in human-V2 binding and V1a binding assay).

Xanthone V1a is a useful organic compound for research related to life sciences and the catalog number is T126501.

V1a/V2 antagonist 1 (Compound 18j) is an orally active dual-target antagonist of V1a and V2 receptors, exhibiting high binding affinity toward these receptors [Ki values are hV1a: 0.13 nM, hV2: 0.53 nM, and mV1a: 0.5 nM; IC50 for hV1a is 2.2 nM]. This compound can inhibit oxytocin-induced scratching behavior in mice.

ω-Hexatoxin-Hv1a, a neurotoxin extracted from the venom of the spider Hadronyche versuta, inhibits voltage-gated calcium channels [1] [2].

Furaprofen is an orally available, selective and potent HCV inhibitor with anti-inflammatory activity, inhibits carrageenan-induced paw edema in rats and inhibits cotton pellet-induced granulomas in rats at higher doses.

Daclatasvir dihydrochloride (BMS-790052 dihydrochloride) is an orally available antiviral agent that inhibits the NS5A region of the hepatitis C virus (HCV) and is used in combination with other oral antivirals to treat chronic hepatitis C. Elevations in serum enzyme levels during daclatasvir therapy are uncommon, and it has not been convincingly implicated in cases of clinically apparent liver injury with jaundice.

RG7713 (RO 5028442) has been used in trials studying Autistic Disorder.

Balovaptan (RG7314) is a highly potent and selective brain-penetrant vasopressin 1a (hV1a) receptor antagonist, with Kis of 1 and 39 nM for human (hV1a) and mouse (mV1a) receptors. It is used for the research of autism.

SRX246 has no interaction at V1b and V2 receptors. SRX246 shows negligible binding at 64 other receptors classes, including 35 G-proteincoupled receptors. SRX246 is a potent and CNS-penetrant vasopressin 1a (V1a) receptor antagonist (Ki=0.3 nM for human V

YM 218 is a novel, potent, selective antagonist of nonpeptide vasopressin V1A receptor.

Conivaptan hydrochloride (Vaprisol) is an orally active vasopressin V2 and V1A receptor antagonist, used in the therapy of hypervolemic hyponatremia and euvolemic.

Pecavaptan is a vasopressin receptor antagonist.

Inarigivir soproxil (SB9200) is an agonist of innate immunity that demonstrates effective antiviral activity against resistant hepatitis C virus (HCV) variants, with EC50s of 2.2 and 1.0 μM for HCV 1a/1b in cells of genotype 1 HCV replicon systems.

JTK-853 is a novel, non-nucleoside inhibitor of Hepatitis C Virus (HCV) polymerase, exhibiting effective antiviral activity in HCV replicon cells with EC50s of 0.38 μM for genotype 1a H77 strain and 0.035 μM for genotype 1b Con1 strain.

TRPV1 antagonist 10 is a potent, orally active TRPV1 antagonist with an IC50 of 33.06 nM and serves as a moderate to weak inhibitor of URAT1 (IC50 = 22.51 μM) and GLUT9 (inhibition of 60.25% at 50 μM). It exhibits analgesic and urate-lowering properties and is applicable for research in hyperuricemia and inflammatory pain.

TRPV1 antagonist 11 (compound 2ac) is a highly potent TRPV1 antagonist with an IC50 of 29.3 nM. It also acts as a μ-opioid receptor (MOR) agonist with a Ki of 60.3 nM. This pyrimidinylpiperazine compound provides analgesic effects by antagonizing TRPV1 and activating MOR. In mouse models of formalin-induced pain, TRPV1 antagonist 11 demonstrates effective dose-dependent antinociceptive properties.

TRPV1 antagonist 6 (compound 51) is a modality-selective TRPV1 antagonist that exhibits antagonistic activity against capsaicin activation with an IC50 of 2.85 nM and demonstrates an inhibition rate of 28.48% against proton activation at a concentration of 3 µM.

TRPV1 antagonist 7 (Compound 36) is a selective TRPV1 inhibitor that effectively blocks capsaicin activation with an IC50 of 2.31 nM. It is useful for research in pain relief.

TRPV1 agonist-1 (Compound 13) is a non-irritant TRPV1 agonist that is effective when administered orally. It shows EC50 values of 4.5 nM for humans and 0.57 nM for rats. TRPV1 agonist-1 has the capability to improve swallowing function in rats and is applicable for research on dysphagia.

Paritaprevir (ABT450) is an inhibitor of non-structural protein 3/4A protease with EC50 values of 1 and 0.21 nM for HCV 1a and HCV 1b, respectively.

Asunaprevir (BMS-650032) is an effective hepatitis C virus (HCV) NS3 protease inhibitor.

TRPV1 antagonist 3 (Compound 7q) is a highly potent TRPV1 receptor antagonist with an IC50 of 2.66 nM against capsaicin. It exhibits selectivity in its mode of action, is orally bioavailable (60%), and can penetrate the central nervous system [1].