Terguride

Source: Wikipedia, the free encyclopedia.
Terguride
Clinical data
Trade namesTeluron
Other namesDironyl; Mysalfon; trans-Dihydrolisuride; Transdihydrolisuride; TDHL; SH-406; VUFB-6638; ZK-31224; N,N-Diethyl-N'-[(8α)-6-methylergolin-8-yl]urea
AHFS/Drugs.comInternational Drug Names
Routes of
administration		Oral
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Identifiers
  • 3-[(6aR,9S,10aR)-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinolin-9-yl]-1,1-diethylurea
JSmol)
  • CCN(CC)C(=O)N[C@H]1C[C@H]2[C@@H](CC3=CNC4=CC=CC2=C34)N(C1)C
  • InChI=1S/C20H28N4O/c1-4-24(5-2)20(25)22-14-10-16-15-7-6-8-17-19(15)13(11-21-17)9-18(16)23(3)12-14/h6-8,11,14,16,18,21H,4-5,9-10,12H2,1-3H3,(H,22,25)/t14-,16+,18+/m0/s1
  • Key:JOAHPSVPXZTVEP-YXJHDRRASA-N
  (verify)

Terguride (

hyperprolactinemia (high prolactin levels) in Japan.[1][2] Terguride is taken by mouth.[citation needed
]

Pharmacology

Pharmacodynamics

Terguride acts as an

serotonin 5-HT2A and 5-HT2B receptors, among other actions.[citation needed
]

As an antagonist of the 5-HT2B receptor, terguride is not associated with

cardiac valvulopathy.[3]

Activities of terguride at various sites[4][5][6][7]
Site Affinity (Ki [nM]) Efficacy (Emax [%]) Action
D1
 28 ? ?
D2S
 0.81 39 Partial agonist
D2L
 1.1 0 Silent antagonist
D3
 1.0 36 Partial agonist
D4
 8.1 0 Silent antagonist
D5
 23 ? ?
5-HT1A 3.5 71 Partial agonist
5-HT1B 257 37 Partial agonist
5-HT1D 16 62 Partial agonist
5-HT2A 4.8 49 Partial agonist
5-HT2B 7.1 0 Silent antagonist
5-HT2C 48 0 Silent antagonist
5-HT7 8–42 ? ?
α1A
 3.5 0 Silent antagonist
α1B
 35 ? ?
α1D
 3.9 ? ?
α2A
 0.30 0 Silent antagonist
α2B
 0.45 0 Silent antagonist
α2C
 0.76 0 Silent antagonist
α2D
 1.5 ? ?
β1
 661 ? ?
β2
 20 ? ?
H1
 339 ? ?
M1 >10,000 ? ?
Notes: All receptors are human except α2D-adrenergic, which is rat (no human counterpart), and 5-HT7, which was guinea pig.[4][7]

Research

pulmonary arterial hypertension.[9]
In May 2010 Pfizer purchased worldwide rights for the drug.[10] However, development was discontinued in 2011.

References

  1. ^ "List of 5HT3 receptor antagonists (5hydroxytryptamine receptor antagonists)". Archived from the original on 2016-03-03.
  2. ^ "Terguride - AdisInsight".
  3. S2CID 22768662
    .
  4. ^
    S2CID 6200455
    .
  5. S2CID 35238120
    .
  6. S2CID 19260572
    .
  7. ^ a b "PDSP Database - UNC". pdsp.unc.edu. Archived from the original on 13 April 2021. Retrieved 15 January 2022.
  8. PMID 25667920
    .
  9. ^ Presseportal (Swiss press portal, in German)
  10. ^ "TheDay.com 5/10/2010". Archived from the original on 2016-03-05. Retrieved 2010-05-21.