Cat. No.: HY-16900G

Rolipram (GMP)

Rolipram GMP is Rolipram (HY-16900) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Rolipram is a PDE4 inhibitor, with blood-brain barrier permeability, that reverses β-amyloid-induced learning and memory impairment in rats. Rolipram elevates intracellular cAMP and clevels and regulates the cAMP/CREB signaling pathway, thereby alleviating neuroinflammation and apoptotic responses. Rolipram promotes neuronal differentiation of human bone marrow mesenchymal stem cells and inhibits Methamphetamine- and morphine-induced hyperlocomotion in mice. Rolipram also reduces the viability of glioblastoma stem-like cells and enhances Bevacizumab (HY-P9906)-induced cell death. Rolipram inhibits the expression of proinflammatory cytokines and enhances central noradrenergic transmission. Rolipram is mainly used in studies related to various central nervous system diseases including Alzheimer's disease, major depressive disorder, glioblastoma multiforme, and multiple sclerosis.

For research use only. We do not sell to patients.

CAS No.: 61413-54-5
Formula: C₁₆H₂₁NO₃
Molecular Weight:275.34

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

Rolipram (GMP) Chemical Structure

CAS No.: 61413-54-5

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Use of MCE Products

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

IC50: 3 nM (PDE4A), 130 nM (PDE4B), 240 nM (PDE4D)^[1]

All Phosphodiesterase (PDE) Isoforms :

All Epigenetic Reader Domain Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	100 μM Compound: Rol	Antiproliferative activity against human A549 cells after 48 hrs by MTT assay Antiproliferative activity against human A549 cells after 48 hrs by MTT assay	[PMID: 34311158]
COS-7	IC₅₀	105 nM Compound: rolipram	Inhibition of PDE4B2 expressed in COS7 cells assessed as cAMP hydrolysis Inhibition of PDE4B2 expressed in COS7 cells assessed as cAMP hydrolysis	[PMID: 18222088]
HEK293	EC₅₀	131.5 nM Compound: 1	Inhibition of PDE4 expressed in HEK293 cells coexpressing G-protein coupled receptor and cyclic nucleotide gated ion channel by fluorescence assay Inhibition of PDE4 expressed in HEK293 cells coexpressing G-protein coupled receptor and cyclic nucleotide gated ion channel by fluorescence assay	[PMID: 19464886]
HEK293	EC₅₀	0.22 μM Compound: Rolipram	Inhibition of PDE4B expressed in HEK293 cells assessed as fold reduction in forskolin-stimulated cAMP production pretreated for 30 mins measured 4 hrs after forskolin challenge by luciferase reporter gene assay Inhibition of PDE4B expressed in HEK293 cells assessed as fold reduction in forskolin-stimulated cAMP production pretreated for 30 mins measured 4 hrs after forskolin challenge by luciferase reporter gene assay	[PMID: 22386978]
HEK293	EC₅₀	2.62 μM Compound: Rolipram	Inhibition of PDE4A4 (unknown origin) transfected in HEK293 cells assessed as forskolin-induced cAMP accumulation pretreated for 30 mins before forskolin challenge by luciferase reporter gene assay Inhibition of PDE4A4 (unknown origin) transfected in HEK293 cells assessed as forskolin-induced cAMP accumulation pretreated for 30 mins before forskolin challenge by luciferase reporter gene assay	10.1039/C2MD00273F
HEK293	EC₅₀	0.16 μM Compound: Rolipram	Inhibition of PDE4B1 (unknown origin) transfected in HEK293 cells assessed as forskolin-induced cAMP accumulation pretreated for 30 mins before forskolin challenge by luciferase reporter gene assay Inhibition of PDE4B1 (unknown origin) transfected in HEK293 cells assessed as forskolin-induced cAMP accumulation pretreated for 30 mins before forskolin challenge by luciferase reporter gene assay	10.1039/C2MD00273F
HEK293	EC₅₀	0.67 μM Compound: Rolipram	Inhibition of PDE4D3 (unknown origin) transfected in HEK293 cells assessed as forskolin-induced cAMP accumulation pretreated for 30 mins before forskolin challenge by luciferase reporter gene assay Inhibition of PDE4D3 (unknown origin) transfected in HEK293 cells assessed as forskolin-induced cAMP accumulation pretreated for 30 mins before forskolin challenge by luciferase reporter gene assay	10.1039/C2MD00273F
MCF7	IC₅₀	100 μM Compound: Rol	Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 34311158]
NCI-H460	IC₅₀	100 μM Compound: Rol	Antiproliferative activity against human NCI-H460 cells after 48 hrs by MTT assay Antiproliferative activity against human NCI-H460 cells after 48 hrs by MTT assay	[PMID: 34311158]
PBMC	IC₅₀	0.5 μM Compound: 1	Inhibition of TNF-alpha release from LPS-stimulated human mononuclear cells Inhibition of TNF-alpha release from LPS-stimulated human mononuclear cells	[PMID: 9784096]
PBMC	IC₅₀	0.15 μM Compound: Rolipram	Inhibition of LPS stimulated Tumor Necrosis Factor-alpha (TNF-alpha) release by human PBMC Inhibition of LPS stimulated Tumor Necrosis Factor-alpha (TNF-alpha) release by human PBMC	[PMID: 9873600]
PBMC	IC₅₀	0.16 μM Compound: Rolipram	Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha release in after 24 hrs by FACS Array analysis Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha release in after 24 hrs by FACS Array analysis	[PMID: 19303290]
PBMC	IC₅₀	0.23 μM Compound: Rolipram	Antiinflammatory activity in human PBMC assessed as inhibition of phytohemagglutininin-induced IL2 release after 24 hrs by FACS Array analysis Antiinflammatory activity in human PBMC assessed as inhibition of phytohemagglutininin-induced IL2 release after 24 hrs by FACS Array analysis	[PMID: 19303290]
PBMC	IC₅₀	0.5 μM Compound: Rolipram	Antiinflammatory activity in human PBMC assessed as inhibition of phytohemagglutininin-induced IL5 release after 48 hrs by FACS Array analysis Antiinflammatory activity in human PBMC assessed as inhibition of phytohemagglutininin-induced IL5 release after 48 hrs by FACS Array analysis	[PMID: 19303290]
PBMC	IC₅₀	0.88 μM Compound: Rolipram	Antiinflammatory activity in human PBMC assessed as inhibition of phytohemagglutininin-induced IL10 release after 48 hrs by FACS Array analysis Antiinflammatory activity in human PBMC assessed as inhibition of phytohemagglutininin-induced IL10 release after 48 hrs by FACS Array analysis	[PMID: 19303290]
PBMC	IC₅₀	60 nM Compound: Rolipram	Inhibition of LPS-induced TNFalpha production in human PBMC Inhibition of LPS-induced TNFalpha production in human PBMC	[PMID: 19049349]
PBMC	EC₅₀	0.13 μM Compound: rolipram	Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha production after 24 hrs by ELISA Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha production after 24 hrs by ELISA	[PMID: 22891752]
PBMC	IC₅₀	0.27 μM Compound: Rolipram	Inhibition of LPS-induced TNF-alpha production in rat PBMC Inhibition of LPS-induced TNF-alpha production in rat PBMC	[PMID: 24852119]
PBMC	IC₅₀	12.5 μM Compound: Rolipram	Anti-inflammatory activity in human PBMC assessed as suppression of LPS-induced TNF-alpha release preincubated for 30 mins followed by LPS stimulation for 18 hrs by TR-FRET assay Anti-inflammatory activity in human PBMC assessed as suppression of LPS-induced TNF-alpha release preincubated for 30 mins followed by LPS stimulation for 18 hrs by TR-FRET assay	[PMID: 27289320]
PBMC	IC₅₀	18.6 μM Compound: Rolipram	Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha secretion preincubated for 30 mins followed by LPS stimulation for 18 hrs by TR-FRET assay Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha secretion preincubated for 30 mins followed by LPS stimulation for 18 hrs by TR-FRET assay	[PMID: 28196708]
PBMC	IC₅₀	10.85 μM Compound: 1	Inhibition of LPS-induced TNFalpha production in human PBMC pre-incubated for 30 mins before LPS stimulation for 18 hrs by TR-FRET assay Inhibition of LPS-induced TNFalpha production in human PBMC pre-incubated for 30 mins before LPS stimulation for 18 hrs by TR-FRET assay	[PMID: 28888661]
PBMC	IC₅₀	0.13 μM Compound: Rolipram	Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha production after 24 hrs by ELISA Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha production after 24 hrs by ELISA	[PMID: 29432948]
PBMC	IC₅₀	30 μM Compound: IV	Cytotoxicity against human PBMC by MTS assay Cytotoxicity against human PBMC by MTS assay	[PMID: 29173945]
RAW264.7	IC₅₀	0.19 μM Compound: Rolipram	Inhibition of LPS-induced TNFalpha production in mouse RAW264.7 cells pretreated for 30 mins before LPS challenge by ELISA assay Inhibition of LPS-induced TNFalpha production in mouse RAW264.7 cells pretreated for 30 mins before LPS challenge by ELISA assay	10.1039/C2MD00273F
RAW264.7	CC₅₀	60 μM Compound: Rolipram	Cytotoxicity against mouse RAW264.7 cells measured after 24 hrs by CCK-8 method Cytotoxicity against mouse RAW264.7 cells measured after 24 hrs by CCK-8 method	[PMID: 40423264]
RAW264.7	IC₅₀	39.93 μM Compound: Rolipram	Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha release preincubated for 2 hrs followed by LPS stimulation and measured after 4 hrs by RT-PCR analysis Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha release preincubated for 2 hrs followed by LPS stimulation and measured after 4 hrs by RT-PCR analysis	[PMID: 40423264]
RAW264.7	IC₅₀	60 μM Compound: Rolipram	Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced NO release preincubated for 2 hrs followed by LPS stimulation and measured after 4 hrs by RT-PCR analysis Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced NO release preincubated for 2 hrs followed by LPS stimulation and measured after 4 hrs by RT-PCR analysis	[PMID: 40423264]
Sf21	IC₅₀	100 μM Compound: 7	Inhibition of His-tagged catalytic domain Trypanosoma brucei brucei PDEB1 expressed in baculovirus infected insect Sf21 cells Inhibition of His-tagged catalytic domain Trypanosoma brucei brucei PDEB1 expressed in baculovirus infected insect Sf21 cells	[PMID: 22023548]
Sf21	IC₅₀	95 nM Compound: 1	Inhibition of human full length PDE4A4 expressed in baculovirus infected sf21 cells Inhibition of human full length PDE4A4 expressed in baculovirus infected sf21 cells	[PMID: 23806553]
Sf9	IC₅₀	4 nM Compound: 1	Inhibition of recombinant human PDE4A expressed in Sf9 cells Inhibition of recombinant human PDE4A expressed in Sf9 cells	[PMID: 11052785]
Sf9	IC₅₀	2.3 μM Compound: Rolipram	Inhibition of human recombinant PDE4 catalytic domain expressed in baculovirus-infected insect Sf9 cells by modified two-step method Inhibition of human recombinant PDE4 catalytic domain expressed in baculovirus-infected insect Sf9 cells by modified two-step method	[PMID: 19303290]
Sf9	IC₅₀	0.092 μM Compound: rolipram	Inhibition of human recombinant PDE4D expressed in Sf9 cells Inhibition of human recombinant PDE4D expressed in Sf9 cells	[PMID: 19827751]
Sf9	IC₅₀	0.941 μM Compound: Rolipram	Inhibition of PDE4B1 (unknown origin) expressed in sf9 cells using cAMP as substrate preincubated for 15 mins before substrate addition measured after 1 hr by luminescence assay Inhibition of PDE4B1 (unknown origin) expressed in sf9 cells using cAMP as substrate preincubated for 15 mins before substrate addition measured after 1 hr by luminescence assay	[PMID: 23415088]
Sf9	IC₅₀	1 μM Compound: Rolipram	Inhibition of recombinant His-tagged PDE4B (unknown origin) expressed in Sf9 cells using cAMP as substrate incubated for 15 mins prior to substrate addition measured after 1 hr by luminescence-based assay Inhibition of recombinant His-tagged PDE4B (unknown origin) expressed in Sf9 cells using cAMP as substrate incubated for 15 mins prior to substrate addition measured after 1 hr by luminescence-based assay	[PMID: 23380174]
Sf9	IC₅₀	0.94 μM Compound: Rolipram	Inhibition of His-tagged recombinant human PDE4B1 expressed in baculovirus infected sf9 cells using cAMP as substrate preincubated for 15 mins followed by substrate addition measured after 1 hr by luminescence assay Inhibition of His-tagged recombinant human PDE4B1 expressed in baculovirus infected sf9 cells using cAMP as substrate preincubated for 15 mins followed by substrate addition measured after 1 hr by luminescence assay	10.1039/C2MD00273F
Sf9	IC₅₀	0.15 μM Compound: 4	Inhibition of human full length N-terminal GST-tagged PDE4B1 expressed in baculovirus infected Sf9 cells using cAMP as substrate incubated for 1 hr by fluorescence polarization assay Inhibition of human full length N-terminal GST-tagged PDE4B1 expressed in baculovirus infected Sf9 cells using cAMP as substrate incubated for 1 hr by fluorescence polarization assay	[PMID: 30822711]
Sf9	IC₅₀	0.3 μM Compound: 4	Inhibition of human N-terminal GST-tagged PDE4D7 (2 to 748 residues) expressed in baculovirus infected Sf9 cells using cAMP as substrate after 1 hr by fluorescence polarization assay Inhibition of human N-terminal GST-tagged PDE4D7 (2 to 748 residues) expressed in baculovirus infected Sf9 cells using cAMP as substrate after 1 hr by fluorescence polarization assay	[PMID: 30822711]
Sf9	IC₅₀	0.94 μM Compound: Rolipram	Inhibition of recombinant His-tagged human PDE4B expressed in Sf9 cells using cAMP as substrate preincubated with enzyme for 15 mins followed by substrate addition and incubated for 1 hr by PDELight HTS cAMP phosphodiesterase Kit based luminometry Inhibition of recombinant His-tagged human PDE4B expressed in Sf9 cells using cAMP as substrate preincubated with enzyme for 15 mins followed by substrate addition and incubated for 1 hr by PDELight HTS cAMP phosphodiesterase Kit based luminometry	[PMID: 31035240]
Sf9	IC₅₀	288 nM Compound: CHEMBL63	Inhibition of recombinant human PDE4D7 catalytic domain expressed in baculovirus infected sf9 cells using cAMP as substrate Inhibition of recombinant human PDE4D7 catalytic domain expressed in baculovirus infected sf9 cells using cAMP as substrate	[PMID: 26908025]
Sf9	IC₅₀	1.03 μM Compound: Rolipram	Inhibition of recombinant human PDE4B expressed in baculovirus infected Sf9 cells using [3H] cAMP as substrate after 30 min by scintillation proximity assay Inhibition of recombinant human PDE4B expressed in baculovirus infected Sf9 cells using [3H] cAMP as substrate after 30 min by scintillation proximity assay	[PMID: 32209292]
T-cell	IC₅₀	10 μM Compound: Rolipram	Inhibitory concentration against T cell proliferation using concanavalin A stimulated mice spleen cells Inhibitory concentration against T cell proliferation using concanavalin A stimulated mice spleen cells	[PMID: 11229767]
U-251	IC₅₀	100 μM Compound: Rol	Antiproliferative activity against human U-251 cells after 48 hrs by MTT assay Antiproliferative activity against human U-251 cells after 48 hrs by MTT assay	[PMID: 34311158]
U-937	IC₅₀	0.93 μM Compound: Rolipram	Inhibition of phosphodiesterase type 4 isozyme (PDE4) from the U937 human cell line. Inhibition of phosphodiesterase type 4 isozyme (PDE4) from the U937 human cell line.	[PMID: 11123995]
U-937	IC₅₀	0.4 μM Compound: Rolipram	Inhibition of phosphodiesterase 4 from U937 cells Inhibition of phosphodiesterase 4 from U937 cells	[PMID: 9873600]
U-937	IC₅₀	3.5 μM Compound: Rolipram	Inhibition of Phosphodiesterase 4 from human U937 cells Inhibition of Phosphodiesterase 4 from human U937 cells	[PMID: 10999488]
U-937	IC₅₀	3.5 μM Compound: Rolipram	Inhibition of Phosphodiesterase 4 (PDE-4) from human U937 cells Inhibition of Phosphodiesterase 4 (PDE-4) from human U937 cells	[PMID: 12039574]
U-937	IC₅₀	3.5 μM Compound: Rolipram	Inhibition of human phosphodiesterase 4 from U937 cells Inhibition of human phosphodiesterase 4 from U937 cells	[PMID: 11814830]
U-937	EC₅₀	1.23 μM Compound: Rolipram	Arbitary maximal response for cAMP elevation from baseline level was evaluated in Human U-937 cells Arbitary maximal response for cAMP elevation from baseline level was evaluated in Human U-937 cells	[PMID: 9632360]
U-937	IC₅₀	1.23 μM Compound: 1	Ability to elevate intracellular levels of cAMP in human U937 cells Ability to elevate intracellular levels of cAMP in human U937 cells	10.1016/S0960-894X(97)00097-8
U-937	EC₅₀	1100 nM Compound: 1, Rolipram	cAMP elevation in U937 cells cAMP elevation in U937 cells	[PMID: 16263279]
U-937	IC₅₀	0.86 μM Compound: Rolipram	Inhibition of PDE4 in human U937 cells assessed as accumulation of [3H]adenosine by scintillation counting Inhibition of PDE4 in human U937 cells assessed as accumulation of [3H]adenosine by scintillation counting	[PMID: 19303290]
U-937	IC₅₀	0.41 μM Compound: rolipram	Inhibition of PDE4 from human U937 cells Inhibition of PDE4 from human U937 cells	[PMID: 19827751]
U-937	IC₅₀	880 nM Compound: (+/-)-Rolipram	Inhibition of PDE4 isolated from human U937 cells using [3H]-cAMP as substrate after 30 mins by liquid scintillation counting analysis Inhibition of PDE4 isolated from human U937 cells using [3H]-cAMP as substrate after 30 mins by liquid scintillation counting analysis	10.1039/C0MD00215A
U-937	IC₅₀	1.3 μM Compound: 1	Inhibition of PDE4B isolated from human U937 cells using [3H]-cAMP as substrate after 30 mins Inhibition of PDE4B isolated from human U937 cells using [3H]-cAMP as substrate after 30 mins	[PMID: 26320621]
U-937	IC₅₀	1.12 μM Compound: Rolipram	Anti-inflammatory activity in human U937 cells assessed as inhibition of LPS-induced TNFalpha production pre-incubated for 1 hr before LPS stimulation for 24 hrs by ELISA method Anti-inflammatory activity in human U937 cells assessed as inhibition of LPS-induced TNFalpha production pre-incubated for 1 hr before LPS stimulation for 24 hrs by ELISA method	[PMID: 28927905]
U-937	IC₅₀	1.17 μM Compound: Rolipram	Anti-inflammatory activity in human U937 cells assessed as inhibition of LPS-induced IL6 production pre-incubated for 1 hr before LPS stimulation for 24 hrs by ELISA method Anti-inflammatory activity in human U937 cells assessed as inhibition of LPS-induced IL6 production pre-incubated for 1 hr before LPS stimulation for 24 hrs by ELISA method	[PMID: 28927905]

In Vitro

Rolipram GMP (0.5-25 μM; 6-24 h) upregulates the expression of neural precursor cell genes in hBM-MSCs in a dose- and time-dependent manner, with the maximal effect observed at 1 μM for 12 h^[2].
Rolipram GMP (1-25 μM; 12 h) shows no toxicity to hBM-MSCs at concentrations ≤5 μM, but induces significant cytotoxicity at 10 μM and 25 μM^[2].
Rolipram GMP (1 μM; 12 h) significantly increases the neuronal differentiation rate, neurite length, and neurite number of hBM-MSCs following neuronal induction^[2].
Rolipram GMP (1 μM; 12 h) enhances neuron-specific gene expression and suppresses non-neuronal lineage gene expression in hBM-MSCs following neuronal induction^[2].
Treatment with Rolipram GMP (10 μM; 48 h) alone reduces the viability of CD133+/CD15+ human glioma stem cells (T2), and its cytotoxic effect is stronger when used in combination with bevacizumab than when either drug is used alone^[4].
Rolipram GMP downregulates antigen-driven proliferation and the gene expression of IL-5 and IFN-γ in human peripheral blood mononuclear cells, but does not affect the gene expression of IL-4^[5].

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

Real Time qPCR^[2]

Cell Line:

human bone marrow-mesenchymal stem cells (hBM-MSCs)
Concentration:

0.5 μM; 1 μM; 5 μM; 25 μM
Incubation Time:

6 h; 12 h; 24 h
Result:

Increased expression of neuroprogenitor genes Nestin and CD133 in a dose-dependent manner at ≤1 μM for 12 h, with peak expression at 1 μM.
Decreased expression of neuroprogenitor genes Nestin and CD133 at 25 μM for 12 h.
Peaked expression of neuroprogenitor genes Nestin and CD133 at 12 h, then declined at 24 h when treated with 1 μM.
Significantly increased expression of neuroprogenitor genes Nestin, Musashi, CD133, GFAP, BDNF, and Syn1 under the optimal condition of 1 μM for 12 h compared to untreated hBM-MSCs.

Real Time qPCR^[2]

Cell Line:

human bone marrow-mesenchymal stem cells (hBM-MSCs)
Concentration:

1 μM
Incubation Time:

12 h (pretreatment, followed by neuronal differentiation)
Result:

Showed significantly higher expression of neuronal-specific marker genes CD133, NF-M, MAP-2, KCNH5, SCN3A, and CACNA1A compared to dMSCs.
Exhibited significantly decreased expression of adipogenic (Adiponectin, FABP4), chondrogenic (MMP13), and osteogenic (ALP) marker genes compared to undifferentiated hBM-MSCs, similar to dMSCs.

In Vivo

Rolipram GMP (0.1-0.5 mg/kg; i.p.; once daily; 24 days) dose-dependently reverses Aβ25-35-induced learning and long-term memory deficits in rats, alongside reversing associated hippocampal reductions in pCREB and Bcl-2, and increases in NF-κB p65 and Bax^[1].
Rolipram GMP (0.5 mg/kg; i.p.; once daily; 14 days) reverses Aβ1-42-induced hippocampal changes in pCREB, NF-κB p65, Bcl-2, and Bax in rats, confirming effects observed with Aβ25-35^[1].
Rolipram GMP (1.0-10 mg/kg; i.p.; single dose; 15 minutes pre-methamphetamine) significantly suppresses methamphetamine-induced hyperlocomotion in male ddY mice, with 10 mg/kg producing nearly complete inhibition^[3].
Rolipram GMP (10-100 mg/kg/day; p.o.; daily; 5-14 days) induces dose-dependent toxic effects in female rats, including cardiac, vascular, gastrointestinal, and salivary gland changes, with lethal effects at 100 mg/kg/day within 5 days^[5].
Rolipram GMP (0.02-400 mg/kg; systemic; single dose) induces a characteristic behavioral syndrome and mild hypothermia in rats, with effects linked to enhanced central adrenergic signal transduction^[5].

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

Animal Model:

Rat^[5]
Dosage:

0.02 mg/kg; 400 mg/kg
Administration:

systemic; single dose
Result:

Elicited a head twitch reaction, inhibited spontaneous motility, increased maintenance activity (forepaw shaking, grooming, head twitches), caused vocalization on touch, salivation, increased respiration rate, stimulated the hind limb flexor reflex in the spinal cord, and induced slight hypothermia.
Did not have behavioral effects blocked by cyproheptadine, pizotifen, or phenoxybenzamine.

Chemical Information

CAS No. 61413-54-5
Molecular Weight 275.34
Formula C₁₆H₂₁NO₃
SMILES

O=C1NCC(C2=CC=C(OC)C(OC3CCCC3)=C2)C1
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

Handling Instructions (2659 KB)

References

[1]. Wang C, et al. The phosphodiesterase-4 inhibitor rolipram reverses Aβ-induced cognitive impairment and neuroinflammatory and apoptotic responses in rats. Int J Neuropsychopharmacol. 2012;15(6):749-766. [Content Brief]

[2]. Joe IS, et al. PDE4 Inhibition by Rolipram Promotes Neuronal Differentiation in Human Bone Marrow Mesenchymal Stem Cells. Cell Reprogram. 2016;18(4):224-229. [Content Brief]

[3]. Mori T, et al. Effects of rolipram, a selective inhibitor of phosphodiesterase 4, on hyperlocomotion induced by several abused drugs in mice. Jpn J Pharmacol. 2000;83(2):113-118. [Content Brief]

[4]. Ramezani S, et al. Rolipram potentiates bevacizumab-induced cell death in human glioblastoma stem-like cells. Life Sci. 2017;173:11-19. [Content Brief]

[5]. Zhu J, et al. The antidepressant and antiinflammatory effects of rolipram in the central nervous system. CNS Drug Rev. 2001;7(4):387-398. [Content Brief]

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Rolipram (GMP)

All Phosphodiesterase (PDE) Isoforms

All Epigenetic Reader Domain Isoforms