A 5-HT2 receptor agonist
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Ro 60-0175

Item No. 29520

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(ɑS)-6-chloro-5-fluoro-ɑ-methyl-1H-indole-1-ethanamine, (2E)-2-butenedioate
CAS Number
169675-09-6
Molecular Formula
C11H12ClFN2 • C4H4O4
Formula Weight
342.8
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: soluble
λmax
223, 280 nm
SMILES
N[C@@H](C)CN1C=CC2=CC(F)=C(Cl)C=C21.OC(/C=C/C(O)=O)=O
InChi Code
InChI=1S/C11H12ClFN2.C4H4O4/c1-7(14)6-15-3-2-8-4-10(13)9(12)5-11(8)15;5-3(6)1-2-4(7)8/h2-5,7H,6,14H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1+/t7-;/m0./s1
InChi Key
CEPHEXXZGQBXGT-XZTIXWOLSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $95

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    Product Description

    Ro 60-0175 is an agonist of the serotonin (5-HT) receptor subtype 5-HT2 that stimulates increases in intracellular calcium levels in CHO-K1 cells expressing human 5-HT2A, 5-HT2B, and 5-HT2C receptors (EC50s = 447, 0.9, and 32 nM, respectively).1 It is selective for human 5-HT2A and 5-HT2C (Kis = 32 and 1 nM, respectively) over human 5-HT1A, 5-HT1D, 5-HT6, and 5-HT7, rat 5-HT1B and 5-HT3, and guinea pig 5-HT4 receptors (Kis = ≥1,995 nM), as well as adenosine A1 and A2, histamine H1-3, dopamine D1-5, α1-, α2-, and β1-adrenergic, M1-5 muscarinic, nicotinic, kainate, AMPA, and μ-, δ-, and κ-opioid receptors (IC50s = >1,000 nM), but does bind to β2-adrenergic receptors (IC50 = 251 nM). 2 In vivo, Ro 60-0175 increases plasma levels of corticosterone, oxytocin, and prolactin in rats (ED50s = 2.43, 4.19, and 4.03 mg/kg, respectively), effects that are not inhibited by the 5-HT2C antagonist SB-242084 (Item No. 10096) or the 5-HT2A antagonist MDL 100,907 (volinanserin; Item No. 15936).3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Porter, R.H.P., Benwell, K.R., Lamb, H., et al. Functional characterization of agonists at recombinant human 5-HT2A, 5-HT2B and 5-HT2C receptors in CHO-K1 cells. Br. J. Pharmacol. 128(1), 13-20 (1999).

    2. Martin, J.R., Bös, M., Jenck, F., et al. 5-HT2C receptor agonists: Pharmacological characteristics and therapeutic potential. J. Pharmacol. Exp. Ther. 286(2), 913-924 (1998).

    3. Damjanoska, K.J., Muma, N.A., Zhang, Y., et al. Neuroendocrine evidence that (S)-2-(chloro-5-fluoro-indol-l-yl)-1-methylethylamine fumarate (Ro 60-0175) is not a selective 5-hydroxytryptamine2C receptor agonist. J. Pharmacol. Exp. Ther. 304(3), 1209-1216 (2003).