Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UNIPROT:P56851 (epididymal)
 11,273 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Since the synthesis and maturational processes of sperm are associated with characteristic alterations in different marker enzyme activities in testes and epididymis, it is possible to monitor these enzymes to investigate whether 3 antispermatogenic agents, WIN 18 446, alpha-chlorohydrin (AC), and cyproterone acetate (CA), have any characteristic effects on biochemical events associated with spermatogenesis and maturation of sperm; acid, neutral, and alkaline proteinases, particulate and soluble arylamidases, and sialidase were studied after treatment with 1 of the 3 agents in male albino rats (CIBA strain) by measuring these enzyme levels in rat testicular and epididymal tissues. After WIN treatment, sialidase activity as well as sialic acid content increased in the testis, whereas no such effect occurred in the epididymis at any dose. At low dose, AC (10 mg/kg/day for 7 days) and CA (50 mg/kg/day for 10 days) decreased the sialic acid content and the sialidase activity in the epididymis, whereas the sialic acid and sialidase activity in the testis remained unchanged. At higher dose levels, AC (25 mg) and CA (50 mg) both affected the tissues significantly, i.e., enhancing sialidase activity and lowering sialic acid content. Therefore, the effect of CA and AC is more prominent on the maturational phenomena than the testicular spermatogenesis. AC and CA deserve further investigation for use as a male contraceptive. The relationship between proteinase, sialidase, and arylamidase activities and different phases of spermatogenesis and maturation was established by these test results.
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PMID:Epididymal and testicular enzymes as monitors for assessment of male antifertility drugs. 49 33

The expression of genes encoding the cannabinoid CB(1) and CB(2) receptors and fatty acid amide hydrolase (FAAH) and the lipolytic activity of cannabinoid agonists were investigated in rat adipose tissue.RT-PCR studies indicated that the genes encoding CB(1) and CB(2) receptors and FAAH are not expressed in epididymal adipocytes. In functional studies, the non-selective cannabinoid receptor agonist WIN 55,212-2 concentration-dependently (0.01-30 micro M) induced glycerol release above baseline ( E(max) 96.1+/-6.2% of isoprenaline-induced lipolytic response). The selective CB(2) agonist JWH-015 (0.01-30 micro M) had no lipolytic activity while the endocannabinoid 2-arachidonoylglycerol and the stable anandamide derivative, R(+)-methanandamide had, only a weak lipolytic effect at the highest concentrations employed (10 and 30 micro M). The concentration/response relationship for WIN 55,212-2-mediated lipolytic activity, mimicked by the S(-)-enantiomer WIN 55,212-3, was shifted significantly to the right by the CB(1) antagonist AM 251 only at 10 micro M, but was not modified by the beta-adrenoceptor antagonist propranolol (1 micro M). The protein kinase inhibitor H-89, but not the two adenylyl cyclase inhibitors (+/-) N(6)- R-phenylisopropyladenosine (R-PIA, 1 micro M, a selective A(1) adenosine receptor agonist) or SQ 22,536 (50 micro M) significantly reduced the glycerol efflux induced by WIN 55,212-2. Our data suggest that the cannabinoid drug WIN 55,212-2 may exert lipolytic activity in male rat adipocytes via an intracellular mechanism, not activated by CB(1) or CB(2) receptor stimulation, significantly reversed by H-89 but not clearly linked to stimulation of adenylyl cyclase.
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PMID:CB1- and CB2-cannabinoid receptor-independent lipolysis induced by WIN 55,212-2 in male rat adipocytes. 1456 52

1. In the present study, the effects of anandamide and WIN 55,212-2, cannabinoid receptor agonists, were investigated on electrical field stimulation (EFS)-induced biphasic twitch responses obtained from the epididymal and prostatic portions of rabbit vas deferens strips. 2. Anandamide and WIN 55,212-2 dose-dependently inhibited both the first and second phases of the EFS-induced twitch responses recorded from epididymal and prostatic portions of the vas deferens over the concentration range 10(-9) to 3 x 10(-6) mol/L. 3. The cannabinoid CB1 receptor antagonist AM 251 (10(-6) mol/L) and the cannabinoid CB2 receptor antagonist AM 630 (10(-6) mol/L) had no effect on the inhibitory action of anandamide on the biphasic twitch responses in the prostatic and epididymal portions of the rabbit vas deferens. 4. In both the prostatic and epididymal portions of the rabbit vas deferens, AM 251 significantly, but not completely, reversed the inhibitory effect of WIN 55,212-2 on the first phase of the twitch response. In contrast, AM 630 did not have any effect on the inhibitory action of WIN 55,212-2 in the rabbit vas deferens strips. 5. The inhibitory effects of anandamide or WIN 55,212-2 on EFS-induced twitch responses of both the prostatic and epididymal portions of the rabbit vas deferens were not altered in the presence of 10(-5) mol/L naloxone. 6. These results suggest that cannabinoid receptors may have a modulatory role in the regulation of sympathetic transmission in the rabbit vas deferens. However, further investigation is required to characterize the receptors involved.
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PMID:Effects of cannabinoid receptor activation on rabbit bisected vas deferens strips. 1617 25

The effect of R-(+)-[2,3-dihydro-5-methyl-3-[(morpholiny)methyl]pyrolol[1,2,3-de]-1,4-benzoxazin-yl]-(1-naphthalenyl)methanone mesylate (WIN 55,212-2; a cannabinoid receptor agonist) was investigated on contractions of the bisected (epididymal and prostatic portions) rat vas deferens to assess the role of cannabinoid receptors in sympathetic ATP neurotransmission. WIN 55,212-2 inhibited the electrically induced contractions in both portions of the rat vas deferens. In the presence of the alpha1-adrenoreceptor antagonist prazosin, electrical stimulation produces a contraction mediated exclusively by ATP. In this condition, WIN 55,212-2 in the prostatic portion elicited a concentration-dependent inhibition that was antagonized by N-piperidinyl-[8-chloro-1-(2,4-dichlorophenyl)-1,4,5,6-tetrahydrobenzo[6,7]cyclohepta[1,2-c]pyrazole-3-carboxamide] (NESS 0327), a selective cannabinoid CB1 receptor antagonist. NESS 0327 caused a parallel dextral displacement of the WIN 55,212-2 concentration-response curve. It is suggested that activation of pre-junctional cannabinoid receptors on sympathetic nerves of the vas deferens modulates ATP neurotransmission.
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PMID:Modulation of ATP-mediated contractions of the rat vas deferens through presynaptic cannabinoid receptors. 1627 59