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limited brain penetration

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-108625
    SHA 68
    1 Publications Verification

    		 Neuropeptide S Receptor Neurological Disease
    SHA 68 is a potent and selective non-peptide neuropeptide S receptor (NPSR) antagonist with IC50s of 22.0 and 23.8 nM for NPSR Asn 107 and NPSR Ile 107, respectively. SHA 68 has limited the blood-brain barrier (BBB) penetration and the activity in neuralgia .
    SHA 68
  • HY-110206
    AM6545

    		Cannabinoid Receptor Metabolic Disease
    AM6545 is a highly selective, brain-free (peripherally active) CB1 receptor antagonist (Ki=1.7 nM). AM6545 inhibits endocannabinoid signaling by competitively antagonizing CB1 receptors, inhibiting CB1-mediated appetite stimulation and inflammatory responses without affecting cAMP levels. AM6545 significantly reduces food intake and body weight in mice, while improving metabolic syndrome-related renal impairment (such as proteinuria, fibrosis) and insulin resistance. AM6545 can be used in the study of obesity and its complications .
    AM6545
  • HY-171195
    VU0631019

    		5-HT Receptor Metabolic Disease
    VU0631019 is a potent antagonist of 5-HT2B, with the IC50 of 29 nM. VU0631019 is predicted to have very limited potential for brain penetration in human subjects, as is predicted to be substrates for P-gp-mediated efflux in humans .
    VU0631019
  • HY-171194
    VU0530244

    		5-HT Receptor Metabolic Disease
    VU0530244 is a potent antagonist of 5-HT2B, with the IC50 of 17.3 nM. VU0530244 is predicted to have very limited potential for brain penetration in human subjects, as is predicted to be substrates for P-gp-mediated efflux in humans .
    VU0530244
  • HY-19057
    Vatinoxan

    MK-467; L-659066

    		 Adrenergic Receptor Cardiovascular Disease Neurological Disease
    Vatinoxan (MK-467) is an alpha 2-adrenergic receptor antagonist. The peripheral selectivity of Vatinoxan determines that it has limited penetration across the blood-brain barrier and therefore has low concentrations in the central nervous system. Vatinoxan antagonizes alpha 2-adrenergic receptor receptors by binding to them, thereby reducing or preventing cardiovascular effects caused by α2-adrenergic agonists. Vatinoxan can be used in studies of cardiovascular effects, sedation and analgesia .
    Vatinoxan

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