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CGMP SPECIFIC-PHOSPHODIESTERASE-TYPE-5

  • CGMP-specific phosphodiesterase type 5
  • Mammalian protein found in humans

    Cyclic guanosine monophosphate-specific phosphodiesterase type 5 is an enzyme (EC 3.1.4.17) from the phosphodiesterase class. It is found in various tissues

    CGMP-specific phosphodiesterase type 5

    CGMP-specific phosphodiesterase type 5

    CGMP-specific_phosphodiesterase_type_5

  • PDE5 inhibitor
  • Vasodilating drug

    A phosphodiesterase type 5 inhibitor (PDE5 inhibitor) is a vasodilating drug that works by blocking the degradative action of cGMP-specific phosphodiesterase

    PDE5 inhibitor

    PDE5 inhibitor

    PDE5_inhibitor

  • Type 5
  • Topics referred to by the same term

    Type 5 may refer to: Type 5 diabetes, an inherited form of diabetes CGMP-specific phosphodiesterase type 5 Hyper-IgM syndrome type 5 PDE5 inhibitor, a

    Type 5

    Type_5

  • Phosphodiesterase
  • Class of enzymes

    by cAMP or cGMP by inhibition of their degradation by PDE. Sildenafil (Viagra) is an inhibitor of cGMP-specific phosphodiesterase type 5, which enhances

    Phosphodiesterase

    Phosphodiesterase

    Phosphodiesterase

  • Sildenafil
  • Drug for erectile dysfunction and hypertension

    blood pressure. Sildenafil acts by blocking phosphodiesterase 5 (PDE5), an enzyme that promotes breakdown of cGMP, which regulates blood flow in the penis

    Sildenafil

    Sildenafil

    Sildenafil

  • Drug nomenclature
  • Systematic naming of drugs

    naming of drugs, especially pharmaceutical drugs. In general, drugs have 3 types of names: chemical names, for which IUPAC nomenclature is the most accepted

    Drug nomenclature

    Drug_nomenclature

  • Death during consensual sex
  • Circumstance of death

    dysfunction. One treatment for erectile dysfunction is cGMP-specific phosphodiesterase type 5 inhibitors, which enable patients to resume having sex despite

    Death during consensual sex

    Death_during_consensual_sex

  • PDE1
  • Enzyme

    isoforms exhibit different affinities for cAMP and cGMP. The existence of the Ca2+-stimulated Phosphodiesterase 1 was first demonstrated by Cheung (1970), Kakiuchi

    PDE1

    PDE1

  • Nitric oxide
  • Colorless gas with the formula NO

    protecting cyclic guanosine monophosphate (cGMP) from degradation by cGMP-specific phosphodiesterase type 5 (PDE5) in the corpus cavernosum, allowing for

    Nitric oxide

    Nitric oxide

    Nitric_oxide

  • Phosphodiesterase inhibitor
  • Drug

    (84% in humans), is another cGMP-specific phosphodiesterase inhibitor which inhibits PDE9, a cGMP preferring phosphodiesterase. PDE9 is expressed as high

    Phosphodiesterase inhibitor

    Phosphodiesterase inhibitor

    Phosphodiesterase_inhibitor

  • Discovery and development of phosphodiesterase 5 inhibitors
  • Drug discovery

    monophosphate (cGMP) which leads to several biological processes like effect on intracellular calcium level by the Ca2+ pathway. Phosphodiesterase 5 (PDE5) is

    Discovery and development of phosphodiesterase 5 inhibitors

    Discovery_and_development_of_phosphodiesterase_5_inhibitors

  • Pulmonary hypertension
  • Increased blood pressure in lung arteries

    The US FDA approved sildenafil, a selective inhibitor of cGMP-specific phosphodiesterase type 5 (PDE5), for the treatment of PAH in 2005. It is marketed

    Pulmonary hypertension

    Pulmonary hypertension

    Pulmonary_hypertension

  • Transducin
  • Heterotrimeric G protein involved in vertebrate phototransduction

    α-subunit activates cGMP phosphodiesterase. cGMP phosphodiesterase breaks down cGMP, an intracellular second messenger which opens cGMP-gated cation channels

    Transducin

    Transducin

    Transducin

  • Esterase
  • Class of enzymes which split esters into an acid and alcohol via hydrolysis

    many types of molecules, including nucleotides, proteins, and alkaloids. Phosphodiesterase (PDE), inactivates the second messenger cAMP cGMP specific phosphodiesterase

    Esterase

    Esterase

  • List of enzymes
  • 1.3.11) Category:EC 3.1.4 Phospholipase C (EC 3.1.4.3) CGMP specific phosphodiesterase type 5 (EC 3.1.4.17) Phospholipase D (EC 3.1.4.50) (3-methyl-2-oxobutanoate

    List of enzymes

    List_of_enzymes

  • Helicine arteries of penis
  • Arteries of the penis

    signal is terminated when cGMP is broken down by the enzyme cGMP specific phosphodiesterase type 5 (PDE5), the enzyme that is targeted by sildenafil and other

    Helicine arteries of penis

    Helicine arteries of penis

    Helicine_arteries_of_penis

  • Tadalafil
  • Medication used to treat erectile dysfunction

    citation needed] The inhibition of phosphodiesterase type 5 (PDE5) enhances erectile function by increasing the amount of cGMP.[medical citation needed] Tadalafil

    Tadalafil

    Tadalafil

    Tadalafil

  • GAF domain
  • Protein domain

    domain is named after some of the proteins it is found in: cGMP-specific phosphodiesterases, adenylyl cyclases and FhlA. The first structure of a GAF domain

    GAF domain

    GAF domain

    GAF_domain

  • PDE9A
  • Protein-coding gene in the species Homo sapiens

    High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A is an enzyme that in humans is encoded by the PDE9A gene. The protein encoded by this gene

    PDE9A

    PDE9A

    PDE9A

  • 7-Nitroindazole
  • Chemical compound

    for impotence, which inhibits cGMP specific phosphodiesterase type 5 (PDE5), which is responsible for degradation of cGMP, which is produced by guanylate

    7-Nitroindazole

    7-Nitroindazole

    7-Nitroindazole

  • Phosphodiesterase 3
  • Class of enzymes

    (March 1997). "Structure, localization, and regulation of cGMP-inhibited phosphodiesterase (PDE3)". The Journal of Biological Chemistry. 272 (11): 6823–6

    Phosphodiesterase 3

    Phosphodiesterase 3

    Phosphodiesterase_3

  • Ototoxic medication
  • The enzyme PDE-5, found in the corpus cavernosum smooth muscle, is responsible for degrading cyclic guanosine monophosphate (cGMP) to 5-GMP. Inhibitors

    Ototoxic medication

    Ototoxic medication

    Ototoxic_medication

  • Enzyme inhibitor
  • Molecule that blocks enzyme activity

    sildenafil (Viagra). This compound is a potent inhibitor of cGMP specific phosphodiesterase type 5, the enzyme that degrades the signalling molecule cyclic

    Enzyme inhibitor

    Enzyme inhibitor

    Enzyme_inhibitor

  • Cyclic guanosine monophosphate
  • Chemical compound

    Numerous cyclic nucleotide phosphodiesterases (PDE) can degrade cGMP by hydrolyzing cGMP into 5'-GMP. PDE 5, -6 and -9 are cGMP-specific while PDE1, -2, -3,

    Cyclic guanosine monophosphate

    Cyclic guanosine monophosphate

    Cyclic_guanosine_monophosphate

  • PDE6B
  • Protein-coding gene in the species Homo sapiens

    Rod cGMP-specific 3',5'-cyclic phosphodiesterase subunit beta is the beta subunit of the protein complex PDE6 that is encoded by the PDE6B gene. PDE6 is

    PDE6B

    PDE6B

    PDE6B

  • Avanafil
  • Chemical compound

    rights within the United States. Avanafil acts by inhibiting a specific phosphodiesterase type 5 enzyme found in various body tissues, primarily in the corpus

    Avanafil

    Avanafil

    Avanafil

  • Cyclic adenosine monophosphate
  • Cellular second messenger

    monophosphate (cGMP) 8-Bromoadenosine 3',5'-cyclic monophosphate (8-Br-cAMP) Acrasin specific to chemotactic use in Dictyostelium discoideum. phosphodiesterase 4 (PDE

    Cyclic adenosine monophosphate

    Cyclic adenosine monophosphate

    Cyclic_adenosine_monophosphate

  • Phosphodiesterase 2
  • Class of enzymes

    different substrate specificities. Some are cAMP selective hydrolases (PDE 4, -7 and -8), others are cGMP selective hydrolases (PDE 5, -6 and -9) and the

    Phosphodiesterase 2

    Phosphodiesterase 2

    Phosphodiesterase_2

  • Pulmonary edema
  • Fluid accumulation in the tissue and air spaces of the lungs

    hypertension. Sildenafil's mechanism of action is via phosphodiesterase inhibition which raises cGMP, resulting in pulmonary arterial vasodilation and inhibition

    Pulmonary edema

    Pulmonary edema

    Pulmonary_edema

  • Cell signaling
  • System of communication

    Offermanns S (October 2005). "Mammalian G proteins and their cell type specific functions". Physiological Reviews. 85 (4): 1159–204. Bibcode:2005PhyRv

    Cell signaling

    Cell signaling

    Cell_signaling

  • Paraxanthine
  • Chemical compound

    than theophylline. Paraxanthine is a selective inhibitor of cGMP-preferring phosphodiesterase (PDE9) activity and is hypothesized to increase glutamate

    Paraxanthine

    Paraxanthine

    Paraxanthine

  • Riociguat
  • Chemical compound

    headache, and gastrointestinal disorders also occurred. Nitrates and phosphodiesterase inhibitors (including PDE5 inhibitors) increase the hypotensive (blood

    Riociguat

    Riociguat

    Riociguat

  • Progressive retinal atrophy
  • Genetic eye disease in dogs and cats

    years old. This type of PRA has an early onset of severe vision loss. It is caused by a defect in the gene for cGMP-phosphodiesterase, which leads to

    Progressive retinal atrophy

    Progressive_retinal_atrophy

  • Cyclic nucleotide
  • Cyclic nucleic acid

    regulatory needs. Some phosphodiesterases are cNMP-specific, while others can hydrolyze non-specifically. However, the cAMP and cGMP degradation pathways

    Cyclic nucleotide

    Cyclic nucleotide

    Cyclic_nucleotide

  • Visual phototransduction
  • Process by which light activates retinal cells

    bound GTP to GDP, and thus halts the action of phosphodiesterase, stopping the transformation of cGMP to GMP. This deactivation step of the phototransduction

    Visual phototransduction

    Visual_phototransduction

  • PDE6G
  • Protein-coding gene in the species Homo sapiens

    Retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gamma is an enzyme that in humans is encoded by the PDE6G gene. PDE6G has

    PDE6G

    PDE6G

    PDE6G

  • Photoreceptor cell
  • Type of neuroepithelial cell

    transducin then activates the enzyme cGMP-specific phosphodiesterase (PDE). PDE then catalyzes the hydrolysis of cGMP to 5' GMP. This is the second amplification

    Photoreceptor cell

    Photoreceptor cell

    Photoreceptor_cell

  • Sperm chemotaxis
  • Guidance of sperm

    hyperpolarization of the membrane. The cGMP signal is terminated by the hydrolysis of cGMP through phosphodiesterase (PDE) activity and inactivation of GC

    Sperm chemotaxis

    Sperm_chemotaxis

  • David Kass (physician)
  • American Physician-Scientist

    The lab discovered that inhibiting phosphodiesterase type 5A(PDE5A), which degraded Cyclic guanosine monophosphate(cGMP) and was inhibited by the drug sildenafil

    David Kass (physician)

    David Kass (physician)

    David_Kass_(physician)

  • Protein kinase A
  • Family of enzymes

    number of cAMP hydrolyzing phosphodiesterase (PDE) enzymes, which belong to the substrates activated by PKA. Phosphodiesterase quickly converts cAMP to

    Protein kinase A

    Protein kinase A

    Protein_kinase_A

  • Meiosis
  • Cell division producing haploid gametes

    on cumulus cells. cGMP diffuses into oocytes and halts meiosis by inhibiting phosphodiesterase 3A (PDE3A) and cyclic adenosine 3′,5′-monophosphate (cAMP)

    Meiosis

    Meiosis

    Meiosis

  • PRKAR1A
  • Protein-coding gene in the species Homo sapiens

    Genet. 41 (5): 925–32. PMC 1684338. PMID 3479018. "Entrez Gene: PRKAR1A protein kinase, cAMP-dependent, regulatory, type I, alpha (tissue specific extinguisher

    PRKAR1A

    PRKAR1A

    PRKAR1A

  • Chromosome 21
  • Human chromosome

    regulator protein PCP4 PDE9A: encoding enzyme high affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A PDXK: encoding enzyme Pyridoxal kinase PFKL: encoding

    Chromosome 21

    Chromosome 21

    Chromosome_21

  • Nitrovasodilator
  • Drug that causes vasodilation by releasing nitric oxide

    PDE5 inhibitors block deactivation of cGMP by the enzyme phosphodiesterase-5. In combination with the increased cGMP production caused by nitrovasodilators

    Nitrovasodilator

    Nitrovasodilator

    Nitrovasodilator

  • Sodium nitroprusside
  • Medication for lowering blood pressure

    is similar to that of phosphodiesterase 5 (PDE5) inhibitors such as sildenafil (Viagra) and tadalafil (Cialis), which elevate cGMP concentration by inhibiting

    Sodium nitroprusside

    Sodium nitroprusside

    Sodium_nitroprusside

  • PDE6A
  • Protein-coding gene in the species Homo sapiens

    Rod cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha is an enzyme that in humans is encoded by the PDE6A gene. PDE6A encodes the cyclic-GMP (cGMP)

    PDE6A

    PDE6A

    PDE6A

  • Rhodopsin
  • Light-sensitive receptor protein

    cGMP phosphodiesterase. The cGMP phosphodiesterase hydrolyzes (breaks down) cGMP, lowering its local concentration so it can no longer activate cGMP-dependent

    Rhodopsin

    Rhodopsin

    Rhodopsin

  • Sulfoaildenafil
  • Chemical compound

    of designer analogues of USA FDA-approved inhibitors of type-5 cGMP-specific phosphodiesterase (PDE5), such as sildenafil and vardenafil, have been detected

    Sulfoaildenafil

    Sulfoaildenafil

    Sulfoaildenafil

  • PRKAR2A
  • Protein-coding gene in the species Homo sapiens

    LK, Scott JD (Apr 2001). "mAKAP assembles a protein kinase A/PDE4 phosphodiesterase cAMP signaling module". The EMBO Journal. 20 (8): 1921–30. doi:10

    PRKAR2A

    PRKAR2A

    PRKAR2A

  • GNAT1
  • Protein-coding gene in the species Homo sapiens

    protein (G protein) which stimulates the coupling of rhodopsin and cGMP-phosphodiesterase during visual impulses. The transducin alpha subunits in rods and

    GNAT1

    GNAT1

    GNAT1

  • Cyclic nucleotide–gated ion channel
  • Family of transport proteins

    activation of the enzyme phosphodiesterase, which hydrolyzes cGMP into 5’-GMP, decreasing the concentration of cGMP. In the absence of cGMP, the CNG channels

    Cyclic nucleotide–gated ion channel

    Cyclic nucleotide–gated ion channel

    Cyclic_nucleotide–gated_ion_channel

  • Endothelial NOS
  • Protein and coding gene in humans

    statins, angiotensin-converting enzyme inhibitors (ACEi) and phosphodiesterase type 5 (PDE-5) inhibitors (PDE5i). Statin treatment was more effective in

    Endothelial NOS

    Endothelial NOS

    Endothelial_NOS

  • Retina
  • Part of the eye

    causes the Ga-subunit of the protein to activate a phosphodiesterase (PDE6), which degrades cGMP, resulting in the closing of Na+ cyclic nucleotide-gated

    Retina

    Retina

    Retina

  • Ketotifen
  • Antihistamine medication

    respiratory conditions) and a phosphodiesterase inhibitor (a medication that blocks the enzymes that regulate the levels of cAMP and cGMP, which are molecules

    Ketotifen

    Ketotifen

    Ketotifen

  • Guanylate cyclase
  • Lyase enzyme that synthesizes cGMP from GTP

    tone, insulin secretion, and peristalsis. Once formed, cGMP can be degraded by phosphodiesterases, which themselves are under different forms of regulation

    Guanylate cyclase

    Guanylate cyclase

    Guanylate_cyclase

  • Cyclic di-AMP
  • Chemical compound

    decrease in phosphodiesterase. Phosphodiesterase (PDE) enzymes degrade cyclic di-AMP to the linear molecule 5'-pApA (phosphadenylyl adenosine). 5'-pApA is

    Cyclic di-AMP

    Cyclic di-AMP

    Cyclic_di-AMP

  • Adaptation (eye)
  • Response of the eye to light and dark

    increases the activity of phosphodiesterase which hydrolyses cGMP to further reduce its concentration. This reduces opening of the cGMP gated Na+ channels to

    Adaptation (eye)

    Adaptation_(eye)

  • Gustducin
  • G protein

    capabilities. Transducin removes the inhibition from cGMP Phosphodiesterase, which leads to the breakdown of cGMP. Similarly, α-gustducin binds the inhibitory

    Gustducin

    Gustducin

    Gustducin

  • Sperm guidance
  • Biological process

    hyperpolarization of the membrane. The cGMP signal is terminated by the hydrolysis of cGMP through phosphodiesterase (PDE) activity and inactivation of GC

    Sperm guidance

    Sperm_guidance

  • Nitroglycerin (medication)
  • Medication

    guanosine monophosphate (cGMP) from guanosine triphosphate (GTP). Among other roles, cGMP serves as a substrate for a cGMP-dependent protein kinase that

    Nitroglycerin (medication)

    Nitroglycerin (medication)

    Nitroglycerin_(medication)

  • PRKAR1B
  • Protein-coding gene in the species Homo sapiens

    Am J Hum Genet. 41 (5): 925–32. PMC 1684338. PMID 3479018. "Entrez Gene: PRKAR1B protein kinase, cAMP-dependent, regulatory, type I, beta". Wong TH, Chiu

    PRKAR1B

    PRKAR1B

    PRKAR1B

  • Biochemical cascade
  • Series of chemical reactions resulting in a cell response

    – are soluble in water and are localized at the cytosol, including cAMP, cGMP, IP3, Ca2+, cADPR and S1P. Their main targets are protein kinases as PKA

    Biochemical cascade

    Biochemical_cascade

  • Biological functions of nitric oxide
  • Functions of nitric oxide in organisms

    tissue. Sildenafil (Viagra) works to inhibit the enzyme phosphodiesterase PDE5, which increases the cGMP concentration by inhibiting the conversion to GMP.

    Biological functions of nitric oxide

    Biological_functions_of_nitric_oxide

  • Retinitis pigmentosa
  • Gradual retinal degeneration leading to progressive sight loss

    maturation completes. A defect in cGMP-phosphodiesterase has also been documented; this leads to toxic levels of cGMP.[citation needed] Oxidative damage

    Retinitis pigmentosa

    Retinitis pigmentosa

    Retinitis_pigmentosa

  • Vasodilation
  • Widening of blood vessels

    Shawish MI, Ben-Eltriki M, Wright JM (December 2019). "Effect of phosphodiesterase 5 inhibitors on blood pressure". Cochrane Database of Systematic Reviews

    Vasodilation

    Vasodilation

    Vasodilation

  • PRKAR2B
  • Protein-coding gene in the species Homo sapiens

    cAMP-dependent protein kinase type II-beta regulatory subunit is an enzyme that in humans is encoded by the PRKAR2B gene. cAMP is a signaling molecule

    PRKAR2B

    PRKAR2B

    PRKAR2B

  • GRB2
  • Protein-coding gene in the species Homo sapiens

    Pyne NJ (May 2003). "The inhibitory gamma subunit of the type 6 retinal cGMP phosphodiesterase functions to link c-Src and G-protein-coupled receptor kinase

    GRB2

    GRB2

    GRB2

  • G protein-coupled receptor kinase 2
  • Enzyme

    Pyne NJ (May 2003). "The inhibitory gamma subunit of the type 6 retinal cGMP phosphodiesterase functions to link c-Src and G-protein-coupled receptor kinase

    G protein-coupled receptor kinase 2

    G protein-coupled receptor kinase 2

    G_protein-coupled_receptor_kinase_2

  • PRKG1
  • Protein-coding gene in the species Homo sapiens

    and kinase-directed regulation of phosphorylation of a cGMP-binding phosphodiesterase by cGMP". The Journal of Biological Chemistry. 265 (25): 14971–8

    PRKG1

    PRKG1

    PRKG1

  • Commonly prescribed drugs
  • Type of drugs

    ISBN 978-1-60913-345-0. Li, Heng; Zuo, Jianping; Tang, Wei (17 October 2018). "Phosphodiesterase-4 Inhibitors for the Treatment of Inflammatory Diseases". Frontiers

    Commonly prescribed drugs

    Commonly_prescribed_drugs

  • Thaddeus Dryja
  • retinitis pigmentosa caused by mutations in the α subunit of rod cGMP phosphodiesterase". Nature Genetics. 11 (4): 468–471. doi:10.1038/ng1295-468. ISSN 1061-4036

    Thaddeus Dryja

    Thaddeus_Dryja

  • ADCY8
  • Protein-coding gene in the species Homo sapiens

    to increased cAMP-phosphodiesterase activity in transgenic mice with a cardiac-directed expression of the human adenylyl cyclase type 8 (AC8)" (PDF). FASEB

    ADCY8

    ADCY8

    ADCY8

  • PLCB3
  • Protein-coding gene in the species Homo sapiens

    1-Phosphatidylinositol-4,5-bisphosphate phosphodiesterase beta-3 is an enzyme that in humans is encoded by the PLCB3 gene. The gene codes for the enzyme

    PLCB3

    PLCB3

    PLCB3

  • RAR-related orphan receptor alpha
  • Protein-coding gene in the species Homo sapiens

    Reports. 15 (5): 518–28. doi:10.1002/embr.201338271. PMC 4210094. PMID 24737872. Du J, Huang C, Zhou B, Ziegler SF (April 2008). "Isoform-specific inhibition

    RAR-related orphan receptor alpha

    RAR-related orphan receptor alpha

    RAR-related_orphan_receptor_alpha

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