Art. -Nr.: HY-187661

Pirandamine free base

Pirandamine free base is a selective serotonin (5-HT) (HY-B1473A) uptake inhibitor with an IC₅₀ of 250 nM. It exerts antidepressant-like effects by enhancing central serotonergic function, does not inhibit norepinephrine (HY-13715) uptake, and exhibits no central anticholinergic or monoamine oxidase inhibitory activity. Pirandamine free base is used in the study of depression.

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CAS. Nr.: 42408-79-7
Formel: C₁₇H₂₃NO
Molecular Weight:257.38

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (302 KB)

Pirandamine free base Chemical Structure

CAS. Nr.: 42408-79-7

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[3]

5-HT Receptor

250 nM (IC₅₀)

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In Vitro

Pirandamine free base potently inhibits ³H-5-HT uptake by the crude synaptosomal fraction of rat cerebral cortex after 5 min of incubation, with an IC₅₀ of 250 nM^[3].

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

In Vivo

Pirandamine free base (up to 10 mg/kg; i.p.; single administration) does not exhibit significant gastric acid secretion inhibitory activity in pylorus-ligated female Sprague Dawley rats^[1].
Pirandamine free base (up to 40 mg/kg; i.p.; single administration) does not reduce ulcer formation in female Sprague Dawley rats with 19 h pyloric ligation^[1].
Pirandamine (up to 40 mg/kg; subcutaneous injection; single administration) free base does not prevent Reserpine (HY-N0480)-induced gastric ulcer formation in male Sprague Dawley rats^[1].
Pirandamine free base (20 mg/kg; i.p.) exerts no inhibitory effect on norepinephrine uptake in the medulla oblongata of healthy male Sprague-Dawley rats^[2].
Pirandamine (3.13‑25 mg/kg; i.p.; single dose) free base reverses H75/12‑induced cerebral 5‑HT depletion in healthy male Swiss albino mice with an ED₅₀ value of 11 mg/kg, exhibiting potent 5‑HT uptake inhibitory activity^[2].
Pirandamine (10‑40 mg/kg; i.p.; single dose) free base fails to effectively reverse H77/77 (HY‑124331)‑induced cerebral norepinephrine depletion in healthy male Swiss albino mice, with an ED₅₀ value greater than 40 mg/kg, showing no obvious norepinephrine‑uptake‑inhibiting activity^[2].
Pirandamine (5-40 mg/kg; i.p.) free base dose-dependently enhances the hindlimb extensor reflex induced by 5-Hydroxytryptophan (5-HTP) (HY-N0122) in rats pretreated with spinal cord transection, Reserpine, and Pargyline (HY-A0091A), suggesting an increase in central 5-HT activity^[2].
Pirandamine (5‑20 mg/kg; i.p.; single dose) free base triggers mild behavioral responses at 5 mg/kg and achieves the maximum behavioral score of 4 at 10 mg/kg and 20 mg/kg in the L‑DOPA (HY‑N0304) potentiation assay using pargyline‑pretreated mice, which potentiates levodopa‑related behavioral symptoms^[2].
Pirandamine (10‑20 mg/kg; i.p.; single dose) free base only slightly relieves Reserpine‑evoked ptosis in mice^[2].
Pirandamine (23.0 mg/kg; i.p.; single dose) free base enhances apomorphine (HY‑12723)‑provoked gnawing behavior in mice with an ED₂₀ value of 23.0 mg/kg, displaying weak potentiation against dopamine‑dependent behavior^[2].
Pirandamine (25 mg/kg; i.p.) free base partially antagonizes Oxotremorine (HY-170032)-induced hypothermia in mice, but exerts no significant antagonistic effect on Oxotremorine-induced tremor, salivation, or lacrimation in mice, suggesting that it lacks central anticholinergic activity^[2].
Pirandamine free base (6.25-25 mg/kg; i.p.) dose-dependently potentiates 5-HTP-induced behavioral syndrome in mice, and exerts an extremely potent effect at 25 mg/kg^[3].
Pirandamine free base (40 mg/kg; i.p.) does not inhibit the uptake of ³H-norepinephrine in the mouse heart at intraperitoneal doses up to 40 mg/kg, with an ED₅₀ greater than 40 mg/kg^[3].
Pirandamine free base does not antagonize Reserpine-induced hypothermia in mice at intraperitoneal doses of 2.5 to 20 mg/kg^[3].
Pirandamine (5-20 mg/kg; i.p.) free base fails to prevent Guanethidine sulfate (HY-B0800)-induced ³H-norepinephrine depletion in the mouse heart at an intraperitoneal dose of up to 20 mg/kg, with an ED₅₀ greater than 20 mg/kg^[3].
Pirandamine (20 mg/kg followed by a subsequent 10 mg/kg dose; i.p.) free base suppresses H75/12‑triggered 5‑HT depletion in rat brain by 53%^[3].
Pirandamine (20 mg/kg; oral administration; once daily; for 9 consecutive days) free base does not alter NA-stimulated cAMP production in the cerebral cortex of male Sprague-Dawley rats^[4].

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

Animal Model:

Sprague-Dawley (male, 160-200 g)^[2]
Dosage:

20 mg/kg
Administration:

i.p.; single dose
Result:

Resulted in 106.0% of control ³H-norepinephrine levels in the medulla.
Resulted in 99.0% of control ³H-dihydroxymandelic acid/dihydroxyphenyl glycol (³H-DH) levels in the medulla.
Resulted in 111.7% of control ³H-normetanephrine (³H-OM) levels in the medulla.
Resulted in 110.8% of control ³H-vanillylmandelic acid/4-hydroxy-3-methoxyphenylglycol (³H-OMDH) levels in the medulla.
Did not inhibit ³H-norepinephrine uptake.

Animal Model:

Swiss albino (male, 18-20 g)^[2]
Dosage:

3.13; 12.5; 25 mg/kg
Administration:

i.p.; two doses, second dose half the first
Result:

At first dose 25 mg/kg, resulted in 108.4% of control brain 5-HT levels alone, and 97.7% of control brain 5-HT levels when co-administered with H75/12, achieving 76% inhibition of H75/12-induced depletion.
At first dose 12.5 mg/kg, resulted in 95.6% of control brain 5-HT levels alone, and 80.6% of control brain 5-HT levels when co-administered with H75/12, achieving 62% inhibition of H75/12-induced depletion.
At first dose 3.13 mg/kg, resulted in 99.4% of control brain 5-HT levels alone, and 59.8% of control brain 5-HT levels when co-administered with H75/12, achieving 4% inhibition of H75/12-induced depletion.
Exhibited an ED₅₀ of 11 mg/kg (i.p.) for reversing H75/12-induced brain 5-HT depletion.

Animal Model:

Swiss albino (male, 18-20 g)^[2]
Dosage:

10; 20; 40 mg/kg
Administration:

i.p.; two doses, second dose half the first
Result:

At first dose 40 mg/kg, resulted in 89.2% of control brain norepinephrine levels alone, and 60.2% of control brain norepinephrine levels when co-administered with H77/77, achieving 21% inhibition of H77/77-induced depletion.
At first dose 20 mg/kg, resulted in 94.4% of control brain norepinephrine levels alone, and 62.0% of control brain norepinephrine levels when co-administered with H77/77, achieving 17% inhibition of H77/77-induced depletion.
At first dose 10 mg/kg, resulted in 99.8% of control brain norepinephrine levels alone, and 55.6% of control brain norepinephrine levels when co-administered with H77/77, achieving 0% inhibition of H77/77-induced depletion.
Had an ED₅₀ greater than 40 mg/kg (i.p.) for reversing H77/77-induced brain norepinephrine depletion.

Animal Model:

Sprague-Dawley (spinalized, reserpine- and pargyline-pretreated)^[2]
Dosage:

5; 10; 20; 40 mg/kg
Administration:

i.p.; single dose
Result:

At 40 mg/kg, produced a mean extensor reflex rating of 3.83.
At 20 mg/kg, produced a mean extensor reflex rating of 3.25.
At 10 mg/kg, produced a mean extensor reflex rating of 2.25.
At 5 mg/kg, produced a mean extensor reflex rating of 2.33.
Potentiated the 5-HTP-induced extensor reflex relative to saline-treated controls at all doses.

Animal Model:

Swiss albino (male, group size of 4 per dose)^[2]
Dosage:

5; 10; 20 mg/kg
Administration:

i.p.; single dose
Result:

At 5 mg/kg, produced a behavioural response score of 2.
At 10 mg/kg, produced a behavioural response score of 4.
At 20 mg/kg, produced a behavioural response score of 4.

Animal Model:

Swiss albino (male, 10 per group)^[2]
Dosage:

10; 20 mg/kg
Administration:

i.p.; single dose
Result:

At 20 mg/kg, produced a 19% reduction in reserpine-induced ptosis.
At 10 mg/kg, produced a 7% reduction in reserpine-induced ptosis.

Animal Model:

Swiss albino (male, 6 per group)^[2]
Dosage:

25 mg/kg
Administration:

i.p.; single dose
Result:

Reduced the oxotremorine-induced temperature decrease by 5.1°C at 30 minutes (compared to a 7.5°C decrease in saline controls).
Did not significantly antagonize oxotremorine-induced tremor, salivation, or lacrimation at 15 or 30 minutes.

Animal Model:

Male albino mice (23-25 g)^[3]
Dosage:

6.25; 12.5; 25 mg/kg
Administration:

i.p.
Result:

Produced a very strong (+4) potentiation of the 5-HTP-induced behavioural syndrome at 25 mg/kg.
Produced a strong (+3) potentiation of the 5-HTP-induced behavioural syndrome at 12.5 mg/kg.
Produced a moderate (+2) potentiation of the 5-HTP-induced behavioural syndrome at 6.25 mg/kg.

Animal Model:

Male albino mice (23-25 g)^[3]
Dosage:

40 mg/kg
Administration:

i.p.
Result:

Did not block ³H-NE uptake in mouse heart, with an ED₅₀ of >40 mg/kg i.p.

Animal Model:

Male albino mice (23-25 g)^[3]
Dosage:

2.5; 10; 20 mg/kg
Administration:

i.p.
Result:

Did not antagonize reserpine-induced hypothermia at any tested dose.

Animal Model:

Male albino mice (23-25 g)^[3]
Dosage:

5; 10; 20 mg/kg
Administration:

i.p.
Result:

Was ineffective at preventing guanethidine-induced displacement of ³H-NE in mouse heart, with 7-29% inhibition across tested doses and an ED₅₀ of >20 mg/kg i.p.

Animal Model:

Sprague-Dawley rats (150-160 g; male)^[3]
Dosage:

20 mg/kg (first dose); 10 mg/kg (second dose)
Administration:

i.p.
Result:

Did not affect brain 5-HT levels alone, but inhibited H75/12-induced depletion of rat brain 5-HT by 53%, increasing brain 5-HT levels from 0.31 μg/g (saline + H75/12) to 0.43 μg/g.

Animal Model:

Sprague-Dawley (male, initial body weight 140 g, final body weight ~200 g)^[4]
Dosage:

20 mg/kg
Administration:

p.o.; once daily; 9 days
Result:

Observed no alterations of noradrenaline (NA)-stimulated cyclic adenosine monophosphate (cAMP) formation in cerebral cortical slices.

Chemical Information

CAS. Nr. 42408-79-7
Molecular Weight 257.38
Formel C₁₇H₂₃NO
SMILES

O1CCC=2C=3C=CC=CC3CC2C1(C)CCN(C)C
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (302 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Lippmann W, et al. Effects of tandamine and pirandamine, selective blockers of biogenic amine uptake mechanisms, on gastric acid secretion and ulcer formation in the rat. Life Sci. 1977 Apr 15;20(8):1393-400.

[2]. Pugsley T, et al. Effects of tandamine and pirandamine, new potential antidepressants, on the brain uptake of norepinephrine and 5-hydroxytryptamine and related activities. Psychopharmacology. 1976 May 05;47(1):33-41.

[3]. Lippmann W, et al. Pirandamine, a relatively selective 5-hydroxytryptamine uptake inhibitor. Pharmacol Res Commun. 1976 Aug;8(4):387-405.

[4]. Kopanski C, et al. Effects of long-term treatment of rats with antidepressants on adrenergic-receptor sensitivity in cerebral cortex: Structure activity study. Neurochemistry international. 1983;5(5):649-59. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

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Pirandamine free base

Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen