IDENTIFICATION OF ADENOSINE RECEPTORS IN HUMAN SPERMATOZOA

Meng-Ru Shen, Joel Linden, Shun‐Sheng ‐S Chen, Sheng-Nan Wu

Research output: Contribution to journalArticle

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Abstract

1. The effects of adenosine receptor agonists and antagonists on human sperm motility have been studied. Specific binding sites for adenosine and its analogues on human sperm were also investigated. 2. Agonists stimulated human sperm motility in a dose‐dependent manner with a potency order of 5'‐N‐ethylcarboxamidoadenosine (NECA, EC50= 0.3 μmol/L)>2‐[p‐(carboxyethyl)phenylethylamino]‐5'‐N‐ethylcarboxamidoadenosine(CGS‐21680, EC50= 10 μmol/L)> adenosine (EC50= 100 μmol/L). 3. NECA‐stimulated motility was competitively inhibited by various adenosine receptor antagonists. The potency order was 3,7‐dimethy‐l‐propargylxanthine>8‐(p‐sulfophenyl) theophylline > xanthine amino congener. 4. The radioligand [3H]‐NECA bound to sperm membrane in a saturable manner with a Bmax of 21.3 pmol/mg protein and equilibrium Kd of 4 μmol/L. Adenosine agonists and antagonists competed for [3H]‐NECA binding with the same rank order of potency as for the stimulation of human sperm motility. 5. GTPγs inhibited 63% of specific [3H]‐NECA binding with IC50 value of 11 nmol/L. This suggests that the [3H]‐NECA binding sites may be coupled to one or more G proteins. 6. These results indicate the presence of adenosine A2 receptors on human sperm which are responsible for adenosine‐mediated enhancement of sperm motility.

Original languageEnglish
Pages (from-to)527-534
Number of pages8
JournalClinical and Experimental Pharmacology and Physiology
Volume20
Issue number7-8
DOIs
Publication statusPublished - 1993 Jan 1

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Adenosine-5'-(N-ethylcarboxamide)
Purinergic P1 Receptors
Sperm Motility
Spermatozoa
Adenosine
Purinergic P1 Receptor Antagonists
Adenosine A2 Receptors
Binding Sites
Purinergic P1 Receptor Agonists
Xanthine
Theophylline
Guanosine Triphosphate
GTP-Binding Proteins
Inhibitory Concentration 50
Membranes
Proteins

All Science Journal Classification (ASJC) codes

  • Physiology
  • Pharmacology
  • Physiology (medical)

Cite this

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title = "IDENTIFICATION OF ADENOSINE RECEPTORS IN HUMAN SPERMATOZOA",
abstract = "1. The effects of adenosine receptor agonists and antagonists on human sperm motility have been studied. Specific binding sites for adenosine and its analogues on human sperm were also investigated. 2. Agonists stimulated human sperm motility in a dose‐dependent manner with a potency order of 5'‐N‐ethylcarboxamidoadenosine (NECA, EC50= 0.3 μmol/L)>2‐[p‐(carboxyethyl)phenylethylamino]‐5'‐N‐ethylcarboxamidoadenosine(CGS‐21680, EC50= 10 μmol/L)> adenosine (EC50= 100 μmol/L). 3. NECA‐stimulated motility was competitively inhibited by various adenosine receptor antagonists. The potency order was 3,7‐dimethy‐l‐propargylxanthine>8‐(p‐sulfophenyl) theophylline > xanthine amino congener. 4. The radioligand [3H]‐NECA bound to sperm membrane in a saturable manner with a Bmax of 21.3 pmol/mg protein and equilibrium Kd of 4 μmol/L. Adenosine agonists and antagonists competed for [3H]‐NECA binding with the same rank order of potency as for the stimulation of human sperm motility. 5. GTPγs inhibited 63{\%} of specific [3H]‐NECA binding with IC50 value of 11 nmol/L. This suggests that the [3H]‐NECA binding sites may be coupled to one or more G proteins. 6. These results indicate the presence of adenosine A2 receptors on human sperm which are responsible for adenosine‐mediated enhancement of sperm motility.",
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IDENTIFICATION OF ADENOSINE RECEPTORS IN HUMAN SPERMATOZOA. / Shen, Meng-Ru; Linden, Joel; Chen, Shun‐Sheng ‐S; Wu, Sheng-Nan.

In: Clinical and Experimental Pharmacology and Physiology, Vol. 20, No. 7-8, 01.01.1993, p. 527-534.

Research output: Contribution to journalArticle

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AU - Shen, Meng-Ru

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N2 - 1. The effects of adenosine receptor agonists and antagonists on human sperm motility have been studied. Specific binding sites for adenosine and its analogues on human sperm were also investigated. 2. Agonists stimulated human sperm motility in a dose‐dependent manner with a potency order of 5'‐N‐ethylcarboxamidoadenosine (NECA, EC50= 0.3 μmol/L)>2‐[p‐(carboxyethyl)phenylethylamino]‐5'‐N‐ethylcarboxamidoadenosine(CGS‐21680, EC50= 10 μmol/L)> adenosine (EC50= 100 μmol/L). 3. NECA‐stimulated motility was competitively inhibited by various adenosine receptor antagonists. The potency order was 3,7‐dimethy‐l‐propargylxanthine>8‐(p‐sulfophenyl) theophylline > xanthine amino congener. 4. The radioligand [3H]‐NECA bound to sperm membrane in a saturable manner with a Bmax of 21.3 pmol/mg protein and equilibrium Kd of 4 μmol/L. Adenosine agonists and antagonists competed for [3H]‐NECA binding with the same rank order of potency as for the stimulation of human sperm motility. 5. GTPγs inhibited 63% of specific [3H]‐NECA binding with IC50 value of 11 nmol/L. This suggests that the [3H]‐NECA binding sites may be coupled to one or more G proteins. 6. These results indicate the presence of adenosine A2 receptors on human sperm which are responsible for adenosine‐mediated enhancement of sperm motility.

AB - 1. The effects of adenosine receptor agonists and antagonists on human sperm motility have been studied. Specific binding sites for adenosine and its analogues on human sperm were also investigated. 2. Agonists stimulated human sperm motility in a dose‐dependent manner with a potency order of 5'‐N‐ethylcarboxamidoadenosine (NECA, EC50= 0.3 μmol/L)>2‐[p‐(carboxyethyl)phenylethylamino]‐5'‐N‐ethylcarboxamidoadenosine(CGS‐21680, EC50= 10 μmol/L)> adenosine (EC50= 100 μmol/L). 3. NECA‐stimulated motility was competitively inhibited by various adenosine receptor antagonists. The potency order was 3,7‐dimethy‐l‐propargylxanthine>8‐(p‐sulfophenyl) theophylline > xanthine amino congener. 4. The radioligand [3H]‐NECA bound to sperm membrane in a saturable manner with a Bmax of 21.3 pmol/mg protein and equilibrium Kd of 4 μmol/L. Adenosine agonists and antagonists competed for [3H]‐NECA binding with the same rank order of potency as for the stimulation of human sperm motility. 5. GTPγs inhibited 63% of specific [3H]‐NECA binding with IC50 value of 11 nmol/L. This suggests that the [3H]‐NECA binding sites may be coupled to one or more G proteins. 6. These results indicate the presence of adenosine A2 receptors on human sperm which are responsible for adenosine‐mediated enhancement of sperm motility.

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