Atropine sulfate is a competitive muscarinic acetylcholine receptor antagonist.IC50 value:Target: mAChRAtropine is a naturally occurring tropane alkaloid extracted from deadly nightshade (Atropa belladonna), Jimson weed (Datura stramonium), mandrake (Mandragora officinarum) and other plants of the family Solanaceae. Atropine is a competitive antagonist of the muscarinic acetylcholine receptors (acetylcholine being the main neurotransmitter used by the parasympathetic nervous system). Atropine dilates the pupils, increases heart rate, and reduces salivation and other secretions [1].
Clazosentan (Ro 61-1790) is a selective endothelin A (ETA) receptor antagonist. Clazosentan inhibits ET-1-mediated vasoconstriction. Clazosentan prevents cerebral vasospasm, vasospasm-related cerebral infarction[1][5].
L-693403 maleate is a high affinity and selective σ ligand. L-693403 maleate has the potential for physiological disease research[1].
LY377604 is a human β3-adrenergic receptor agonist with an EC50 of 2.4 nM and also a β1- and β2-adrenergic receptor antagonist.
ICI-204448 is a κ-opioid agonist with limited access to the CNS, ICI-204448 can displace the binding of the kappa-opioid ligand 3H-bremazocine from guinea pig cerebellum membranes[1].
Urapidil-d4 hydrochloride is the deuterium labeled Urapidil hydrochloride. Urapidil hydrochloride is an α1-adrenoceptor antagonist and 5-HT1A receptor agonist[1][2].
Avosentan(Ro 67-0565; SPP-301) is a potent, selective endothelin receptor(ETA receptor) antagonist.IC50 value:Target: ETA receptor
PF-03654746 Tosylate is a potent and selective histamine H3 receptor antagonist with high brain penetration. PF-03654746 Tosylate reduces allergen-induced nasal symptoms[1]. PF-03654746 Tosylate has potential for treatment of human cognitive disorders, improves cognitive efficacy and disease-modifying effects in Alzheimer's disease (AD)[2].
Neuropeptide Y (2-36) (porcine) is a neuropeptide Y5 receptor (NPY5R) agonist in rats with EC50 values of 1.2, 1.6 and 3.4 nM for receptor of Y5, Y2 and Y1 respectively. Neuropeptide Y (2-36) (porcine) can be used in studies related to obesity and eating disorders.
Ancarolol is a beta-adrenergic blocking agent.
Clencyclohexerol is a β-agonist. Clencyclohexerol can be used as a growth promoter in animals[1].
Ro 24-5913 (Cinalukast) is an orally active and potent LTD4 antagonist with an IC50 value of 6.4 nM. Ro 24-5913 can be used for the research of asthma[1].
Bupropion D9 is a deuterium labeled Bupropion. Bupropion is an atypical antidepressant of the aminoketone group and inhibits dopamine, norepinephrine reuptake and blocks several nicotinic receptors[1].
Histamine diphosphate is a potent agonist of histamine receptors and vasodilator. It can activate nitric oxide synthetase.
MRS 1754 is a selective antagonist radioligand for A2B adenosine receptor with very low affinity for A1 and A3 receptors of both humans and rats[1].
Namodenoson (CF-102) is a selective A3 adenosine receptor agonist (Ki = 0.33 nM). Displays 2500- and 1400-fold selectivity over A1 and A2A receptors respectively.
5-HT7 receptor ligand 1 (Compound 5c) is a 5-HT7 receptor ligand with a Ki of 8 nM. 5-HT7 receptor ligand 1 is not hepatotoxic and exhibit moderate potential interaction with other drugs metabolized by CYP3A4 or CYP2D6[1].
KRAS G12C inhibitor 28 is a KRAS G12C inhibitor with an IC50 of 57 nM. KRAS G12C inhibitor 28 has antitumor effects (WO2021113595A1; Example 1)[1].
Fenspiride, an orally active non-steroidal antiinflammatory agent, is an antagonist of H1-histamine receptor. Fenspiride inhibites phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4) and phosphodiesterase 5 (PDE5) activities with -log IC50 values of 3.44, 4.16 and approximately 3.8, respectively. Fenspiride can be used for the research of respiratory diseases[1][2][3].
PF-04634817 is a potent, orally bioavailble CCR2 and CCR5 chemokine receptor antagonist, for the treatment of diabetic nephropathies and diabetic macular oedema. Other Indication Phase 2 Discontinued
Zelminemab (AMG-301) is a human monoclonal antibody that inhibits PACAP type I (PAC1) receptor[1].
PF-4479745 is a potent and selective 5-HT2C receptor agonist (EC50: 10 nM, ki: 15 nM). PF-4479745 can be used in the research of cardiovascular disease like hypertension[1].
Topiramate is an anticonvulsant that antagonizes GluR5 receptors and acts as a positive allosteric modulator of GABA receptor-mediated currents.Target: GluR5 receptor; GABA receptorTopiramate (Topamax) is a structurally novel broad-spectrum antiepileptic drug (AED) with established efficacy as monotherapy or adjunctive therapy in the treatment of adult and paediatric patients with generalised tonic-clonic seizures, partial seizures with or without generalised seizures, and seizures associated with Lennox-Gastaut syndrome [1]. topiramate has been believed to be a type of antiepileptic drug that blocks spread of seizures. Thus far, the mechanisms of its actions have been proven to include use-dependent inhibition of voltage-dependent Na+ channels in neurons, potentiation of GABA (gamma-amino-butyric acid)-induced Cl- influx, and inhibitory effects on inward currents by antagonizing kainate/alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptors [2].Topiramate (median average dosage 5.1 mg/kg/day) was also found to be useful as adjunctive therapy in the management of Lennox-Gastaut syndrome and significantly reduced the mean frequency of drop attacks by 14.8% compared with an increase of 5.1% with placebo. Further gains in seizure control were made in a nonblind extension of this trial where the mean topiramate dosage was 10 mg/kg/day. Nine of 11 patients in 1 pilot trial of children with otherwise intractable West syndrome, and 5 of 10 in another, achieved a > or =50% reduction in seizure rate with topiramate (target dosage up to 24 mg/kg/day) [3].Clinical indications: Epilepsy; Lennox Gastaut syndrome; Migraine; Seizure disorder Toxicity:abdominal pain; agitation; blurred vision; convulsions; depression; dizziness; double vision; drowsiness; impaired coordination; impaired mental activity; low blood pressure; reduced consciousness; severe diarrhea; sluggishness and speech problems.
Alcaftadine(R89674) is a H1 histamine receptor antagonist, which is used to prevent eye irritation brought on by allergic conjunctivitis.Target: H1 Histamine ReceptorAlcaftadine is a broad-spectrum antihistamine displaying a high affinity for histamine H1 and H2 receptors and a lower affinity for H4 receptors. alcaftadine was more effective than placebo and at least as effective as olopatadine 0.01% in preventing ocular itching at 15 minutes and at 16 hours after administration. Alcaftadine 0.025% ophthalmic solution has been approved by the U.S. Food and Drug Administration for prevention of itching associated with allergic conjunctivitis in patients over 2 years of age [1]. Alcaftadine is a safe and effective option for the prevention of ocular itching associated with allergic conjunctivitis, is dosed once daily, and is competitively priced among prescription medications for allergic conjunctivitis [2].
Rasarfin is a dual Ras and ARF6 inhibitor[1].
Neuropeptide Y (18-36) (porcine) is a competitive neuropeptide Y (NPY) cardiac receptor antagonist. Neuropeptide Y (18-36) (porcine) inhibits the binding of I-NPY to rat cardiac ventricular membranes in a concentration-dependent manner with an IC50 value of 158 nM and an Ki value of 140 nM. Neuropeptide Y (18-36) (porcine) can be used for the research of congestive heart failure[1].
CCR1 inhibitor 19e is a novel potent, selective CCR1 antagonist with IC50 of 6.8 nM, inhibits CCR1chemotaxis in THP-1 cells with IC50 of 28 nM.
[D-Trp34]-Neuropeptide Y is a potent and selective neuropeptide Y (NPY) Y5 receptor agonist. [D-Trp34]-Neuropeptide Y is a significantly less potent agonist at the NPY Y1, Y2, Y4, and y6 receptors. [D-Trp34]-Neuropeptide Y markedly increases food intake in rats[1][2].
S 25585 is a potent and selective neuropeptide Y (NPY) Y5 receptor antagonist. S 25585 reduces food intake but not through blockade of the NPY Y5 receptor[1].
TH-Z835 is a mutant selective KRAS (G12D) inhibitor with an IC50 of 1.6 μM. TH-Z835 inhibits both mantGMPPNP/GPPNP exchange and GPPNP/mantGMPPNP exchange[1].