1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor Adrenergic Receptor
  3. LY 344864 hydrochloride

LY 344864 hydrochloride is a selective, orally active 5-HT1F receptor agonist with a Ki of 6 nM. LY 344864 hydrochloride is a full agonist producing an effect similar in magnitude to serotonin itself. LY 344864 hydrochloride can cross the blood brain barrier to some extent.

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LY 344864 hydrochloride Chemical Structure

LY 344864 hydrochloride Chemical Structure

CAS No. : 1217756-94-9

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Description

LY 344864 hydrochloride is a selective, orally active 5-HT1F receptor agonist with a Ki of 6 nM. LY 344864 hydrochloride is a full agonist producing an effect similar in magnitude to serotonin itself. LY 344864 hydrochloride can cross the blood brain barrier to some extent[1].

IC50 & Target[1]

human 5-HT1F Receptor

0.006 μM (Ki)

human 5-HT1A Receptor

0.530 μM (Ki)

human 5-HT1B Receptor

0.549 μM (Ki)

human 5-HT1D Receptor

0.575 μM (Ki)

human 5-HT1E Receptor

1.415 μM (Ki)

human 5-HT2B Receptor

1.695 μM (Ki)

Human 5-HT2C Receptor

3.499 μM (Ki)

Human 5-HT3A Receptor

3.935 μM (Ki)

Human 5-HT7 Receptor

4.851 μM (Ki)

rat α2-adrenergic receptor

3.69 μM (Ki)

rat α1-adrenergic receptor

5.06 μM (Ki)

In Vitro

LY 344864 binds to human 5-HT1F, 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT3A, 5-HT2B, 5-HT2C, 5-HT7, rat α1-adrenergic, rat α2-adrenergic receptors with Kis of 0.006, 0.530, 0.549, 0.575, 1.415, 3.935, 1.695, 3.499, 4.851, 5.06 and 3.69 μM, respectively[1].
LY 344864 is a inducer of mitochondrial biogenesis[2].

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

In Vivo

LY 344864 (0-10 ng/kg; p.o. or i.v.; once) inhibits neurogenic dural inflammation in rat migraine pain model[1].
LY 344864 (1 mg/kg; i.v.; once) can cross the blood brain barrier to some extent in rats[1].
LY 344864 (2 mg/kg; i.p.; daily for 14 days) attenuates dopaminergic neuron loss and improved behavioral endpoints in a Parkinson’s disease mouse model[2].

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

Animal Model: Male Wistar rats, migraine pain model[1]
Dosage: 1-10 ng/kg (oral), 0.3-2 ng/kg (intravenous)
Administration: Oral, 75 minutes before trigeminal stimulation or intravenous, 10 minutes before trigeminal stimulation
Result: When given intravenously 10 minutes before stimulation, inhibited inflammation with an ID50 (median infective dose) of 0.6 ng/kg. When administered orally 75 minutes before trigeminal stimulation, an ID50 of 1.2 ng/kg was obtained.
Animal Model: Male C57BL/6 mice, Parkinson’s disease model[2]
Dosage: 2 mg/kg
Administration: Intraperitoneal injection, daily for 14d beginning 7d post-lesion
Result: Attenuated TH-ir loss in the striatum and substantia nigra compared to vehicle-treated lesioned animals, also increased locomotor activity in 6-hydroxydopamine lesioned mice, while vehicle treatment had no effect.
Molecular Weight

387.88

Formula

C21H23ClFN3O

CAS No.
SMILES

O=C(NC1=CC2=C(NC3=C2C[C@H](N(C)C)CC3)C=C1)C4=CC=C(F)C=C4.[H]Cl

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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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.

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Product Name:
LY 344864 hydrochloride
Cat. No.:
HY-13788B
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