2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. Histamine Receptor
  4. MK-3134

MK-3134 is an orally active, brain-penetrant and selective histamine H3 receptor inverse agonist. MK-3134 modulates histaminergic neurotransmission, decreases constitutive H3 receptor signaling, releases tonic inhibition of neurotransmitter release, potentiates neurotransmission, and may enhance cholinergic neurotransmission. MK-3134 can be used for the research of Alzheimer's disease.

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MK-3134

MK-3134 Chemical Structure

CAS No. : 862310-66-5

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MK-3134 Related Antibodies

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Description

MK-3134 is an orally active, brain-penetrant and selective histamine H3 receptor inverse agonist. MK-3134 modulates histaminergic neurotransmission, decreases constitutive H3 receptor signaling, releases tonic inhibition of neurotransmitter release, potentiates neurotransmission, and may enhance cholinergic neurotransmission. MK-3134 can be used for the research of Alzheimer's disease[1][2][3][4].

IC50 & Target[4]

H3 receptor

3.6 nM (Ki)

In Vitro

MK-3134 (Compound 5s) exhibits an IC50 of 0.33 nM against human H3[5].
MK-3134 (below 1 μM) is a highly selective nanomolar-affinity ligand for histamine H3 receptors, with no meaningful off-target activity at other histamine receptor subtypes or additional tested targets at concentrations below 1 μM[2].
MK-3134 binds to the human histamine H3 receptor with a Ki of 3.6 nM[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

MK-3134 Related Antibodies
Parmacokinetics
Species Dose Route CL AUC0-∞ Cmax F
Rat[5] 1 mg/kg i.v. 24 mL/min/kg / / /
Rat[5] 3 mg/kg p.o. / 1.66 μM·h 0.42 μM 33 %
Dog[5] 0.3 mg/kg i.v. 13 mL/min/kg / / /
Dog[5] 1 mg/kg p.o. / 1.3 μM·h 0.28 μM 46 %
Rhesus monkey[5] 0.3 mg/kg i.v. 26 mL/min/kg / / /
Rhesus monkey[5] 1 mg/kg p.o. / 0.15 μM·h 0.05 μM 11 %
In Vivo

MK-3134 (Compound 5s) (1-10 mg/kg; p.o.; singlle dose) significantly and dose-proportionally elevates tele-methylhistamine in the male SD rats brain[5].
MK-3134's (0.3-3 mg/kg; p.o.; single dose) brain penetration is significantly influenced by P-gp in mice model[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SD rats (male)[5]
Dosage: 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration: p.o.; single dose
Result: Significantly and dose-proportionally elevated tele-methylhistamine in the male SD rats brain.
Animal Model: mdr1a (+/+) and mdr1a (−/−) CF-1 mice (female)[5]
Dosage: 0.3 mg/kg; 1 mg/kg; 3 mg/kg
Administration: p.o.; single dose
Result: Significantly elevated brain penetration in mdr1a (−/−) CF-1 mice, with about 5-fold higher than those in mdr1a (+/+) CF-1 mice.
Clinical Trial
Molecular Weight

457.49

Formula

C25H26F3N3O2
CAS No.
SMILES

O=C1C2=C(C=CC=C2C(F)(F)F)N=C(C)N1C3=CC=C(C=C3)OC4CCN(C5CCC5)CC4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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MK-3134 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MK-3134862310-66-5MK3134MK 3134Histamine Receptorblood-brain barrierexecutive functionhistaminergic neurotransmissioncholinergic neurotransmissionattentionhistamine H3 receptorscopolamine-induced cognitive impairmentdonepezilpsychomotor functionalzheimer's diseaseInhibitorinhibitorinhibit

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