Indalpine

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Indalpine
Clinical data
Trade namesUpstène
Identifiers
  • 3-(2-Piperidin-4-ylethyl)-1H-indole
JSmol)
  • c2(c1ccccc1[nH]c2)CCC3CCNCC3
  • InChI=1S/C15H20N2/c1-2-4-15-14(3-1)13(11-17-15)6-5-12-7-9-16-10-8-12/h1-4,11-12,16-17H,5-10H2 checkY
  • Key:SADQVAVFGNTEOD-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Indalpine (

MAOI class antidepressants. The studies led to widespread recognition of a serotonin hypothesis of depression, contradicting theories that promoted the role of norepinephrine
.

History

While citalopram and zimelidine were developed in the early 1970s, it was Pharmuka's indalpine that was first to reach the market. Baron Shopsin was recruited as consultant to Pharmuka throughout a research and development process that resulted in the marketing of indalpine in France and then worldwide, in 1982. With FDA approval of Pharmuka's IND submission to conduct clinical studies with indalpine and viqueline, Shopsin carried out and published the first clinical trials with these drugs in depressed outpatients in the U.S.[3] Astra's SSRI zimelidine was marketed within a year (1983), but the next crop of SSRIs didn't become commercially available until the 1986 marketing of fluvoxamine in Belgium by Duphar, followed by approval in the United States later that year. Lilly's fluoxetine (Prozac) was approved in the US in 1987.

Meanwhile, zimelidine had been withdrawn soon after its marketing in 1983 due to the emergence of

positive allosteric modulator), both in different stages of development at the time.[citation needed
]

Recently, revision of this molecular motif yielded SERT inhibitors with nanomolar and subnanomolar IC50 values.[5]

References

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  3. ^ Shopsin B, Lefebvre C, Maulet C (1983). "Indalpine (LM-5008): An open study in depressed outpatients". Current Therapeutic Research. 34 (1): 239–252.
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